sign in sign up
<<
Home , Levomefolic acid, Mitotic inhibitor, Nuclear DNA, Reversine

Inhibitors, Agonists, Screening Libraries www.MedChemExpress.com

Cell Cycle/DNA Damage

Cell Cycle includes many processes necessary for successful self-replication, and consists of DNA synthesis (S) and (M) phases separated by gap phases in the order G1–S–G2–M. S phase and M phase are usually separated by gap phases called G1 and G2, when cell-cycle progression can be regulated by various intracellular and extracellular signals. In order to move from one phase of its life cycle to the next, a cell must pass through numerous checkpoints. At each checkpoint, specialized proteins determine whether the necessary conditions exist. Progression through G1 phase is controlled by pRB proteins, and phosphorylation of pRB proteins by CDKs releases E2F factors, promoting the transition to S phase. The G2/M transition that commits cells to division is a default consequence of initiating the cell cycle at the G1/S transition, many proteins, such Wee1, PLK1 and cdc25, is involved the regulation of this process. The best-understood checkpoints are those activated by DNA damage and problems with DNA replication. DNA damage response (DDR) is a series of regulatory events including DNA damage, cell-cycle arrest, regulation of DNA replication, and repair or bypass of DNA damage to ensure the maintenance of genomic stability and cell viability. instability arises if cells initiate mitosis when are only partially replicated or are damaged by a double-strand DNA break (DSB). To prevent cells with damaged DNA from entering mitosis, ATR inhibits cyclin B/Cdk1 activation by stimulating the Cdk1 inhibitory kinase Wee1 and inhibiting Cdc25C via Chk1, besides, ATM and ATR also initiate DNA repair by phosphorylating several other substrates. In cells, the cell cycle regulators as well as other elements of the DDR pathway have been found to protect tumor cells from different stresses and to promote tumor progression. Thus, cell cycle proteins that directly regulate cell cycle progression (such as CDKs), as well as checkpoint kinases, Aurora kinases and PLKs, are promising targets in cancer therapy.

References: [1] Rhind N, et al. Cold Spring Harb Perspect Biol. 2012 Oct; 4(10): a005942. [2] Duronio RJ, et al. Cold Spring Harb Perspect Biol. 2013 Mar; 5(3): a008904. [3] Liu W, et al. Mol Cancer. 2017 Mar 14;16(1):60.

www.MedChemExpress.com 1

2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Inhibitors, Agonists, Screening Libraries www.MedChemExpress.com

Target List in Cell Cycle/DNA Damage

• 3 • /Analog 104

• APC 7 • p97 111

• ATM/ATR 9 • PAK 113

• Aurora Kinase 12 • PARP 116

• Casein Kinase 17 • PERK 122

• CDK 20 • Polo-like Kinase (PLK) 124

• Checkpoint Kinase (Chk) 34 • PPAR 128

• CRISPR/Cas9 37 • RAD51 137

• Deubiquitinase 39 • ROCK 139

• DNA Alkylator/Crosslinker 43 • Sirtuin 144

• DNA-PK 48 • SRPK 149

• DNA/RNA Synthesis 52 • Telomerase 151

• Eukaryotic Initiation Factor (eIF) 60 • TOPK 153

• G-quadruplex 62 • Topoisomerase 155

• Haspin Kinase 64 • Wee1 163

• HDAC 66

• HSP 77

• IRE1 83

• Kinesin 86

• LIM Kinase (LIMK) 89

• / 91

• Mps1 101

www.MedChemExpress.com 3 Antifolate

Antifolates are compounds that antagonise the actions of folic acid ( B9). Folic acid's primary function in the body is as a cofactor to various involved in serine, , and biosynthesis. Consequently inhibit , DNA/RNA synthesis and repair and protein synthesis. Some such as Proguanil, Pyrimethamine and Trimethoprim selectively inhibit 's actions in microbial organisms such as bacteria, protozoa and fungi. The majority of antifolates work by inhibiting (DHFR). Many are primarily DHFR inhibitors, but is an inhibitor of , and inhibits both and a third . Antifolates act specifically during DNA and RNA synthesis, and thus are cytotoxic during the S-phase of the cell cycle. Thus, they have a greater toxic effect on rapidly dividing cells.

4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Antifolate Inhibitors & Modulators

Calcium N5-methyltetrahydrofolate Cycloguanil D6 (NSC173328) Cat. No.: HY-17557 (Chlorguanide triazine D6) Cat. No.: HY-12784S

Bioactivity: N5-methyltetrahydrofolate(NSC173328) is the calcium Bioactivity: Cycloguanil D6 is the deuterium labeled Cycloguanil, which is salt of , which has been proposed for a dihydrofolate reductase inhibitor. treatment of cardiovascular disease and advanced such as breast and colorectal cancers.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg, 10 mg

Cycloguanil D6 Nitrate Diaveridine (Chlorguanide triazine D6 Nitrate) Cat. No.: HY-12784S1 (EGIS-5645) Cat. No.: HY-B1902

Bioactivity: Cycloguanil D6 Nitrate is the deuterium labeled Cycloguanil, Bioactivity: Diaveridine (EGIS-5645) is a dihydrofolate reductase ( DHFR) which is a dihydrofolate reductase inhibitor. inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.

Purity: >98% Purity: 98.48% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg Size: 10mM x 1mL in DMSO, 250 mg, 1 g, 5 g

EC0489 Cat. No.: HY-114306 (leucovorin) Cat. No.: HY-17556

Bioactivity: EC0489, a conjugate of folic acid and desacetyl Bioactivity: Folinic acid is an adjuvant used in cancer hydrazide, is a high-affinity for the folate involving the drug . Target: Antifolate Folinic (FR). Refractory or metastatic Tumor [1]. Small molecule-drug acid is a 5-formyl derivative of . It is readily converted to other reduced folic acid derivatives conjugate (SMDC) [2]. (e.g., tetrahydrofolate), and, thus, has vitamin activity that… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 500 mg, 250 mg Size: 100 mg

Folinic acid Calcium Folinic acid calcium salt pentahydrate (Leucovorin Calcium; Calcium Folinate) Cat. No.: HY-13664 (Leucovorin calcium salt pentahydrate) Cat. No.: HY-B0080

Bioactivity: Leucovorin Calcium is a reduced folic acid. IC50 Value: 30 μM Bioactivity: Folinic Acid is a reduced folic acid, which is used in for zcSHMT and70 μM for zmSHMT [2] Target: Antifolate in combination with other chemotherapy drugs. Target: Folate vitro: Increasing concentrations of leucovorin (N5-CHO-THF) analog Approved: 2008 Folinic acid (calcium salt pentahydrate) inhibit both zcSHMT and hcSHMT activities substantially, yet is the calcium salt form of folinic acid, which is one of the to a lesser extent than zmSHMT. The IC50 of leucovorin is… forms of folate found naturally in foods. is… Purity: 99.73% Purity: 99.73% Clinical Data: Launched Clinical Data: Launched Size: 100 mg, 500 mg Size: 100 mg, 200 mg, 500 mg

Levoleucovorin Calcium Levomefolate calcium (Calcium levofolinate; CL307782) Cat. No.: HY-13667 Cat. No.: HY-17383

Bioactivity: Levoleucovorin calcium is the calcium salt of Levoleucovorin, Bioactivity: Levomefolate is an artificial form of folate. IC50 Value: which is the enantiomerically active form of folinic acid. Target: Antifolate The calcium salt of IC50 value: Target: Levoleucovorin is used to treat or prevent L-5-methyltetrahydrofolic acid which belongs to the group of toxic effects of methotrexate in people who have received folate (Vitamin B9, Folacin). It is a coenzymated methotrexate to treat bone cancer. Levoleucovorin is also used… form of folic acid and a more bioavailable alternative in… Purity: 95.24% Purity: 95.17% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10 mg, 50 mg 100 mg, 500 mg, 1 g, 2 g

www.MedChemExpress.com 5

LY 254155 LY309887 Cat. No.: HY-14523 Cat. No.: HY-10818

Bioactivity: LY 254155, an antifolate, inhibits hGARFT and binds to Bioactivity: LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase ( GARFT), with a K of 6.5 nM, and has mFBP with Kis of 2.1±0.2 and 1.7±0.1 nM, respectively. i antitumor activity.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 250 mg, 500 mg

Methotrexate Pemetrexed (Amethopterin; CL14377; WR19039) Cat. No.: HY-14519 (LY231514) Cat. No.: HY-10820

Bioactivity: Methotrexate is a folate antagonist, with median IC50 of 78 nM Bioactivity: Pemetrexed is a novel antifolate, the Ki values of the in in vitro assay. pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase ( TS), dihydrofolate reductase ( DHFR), and glycinamide ribonucleotide formyltransferase ( GARFT), respectively. Purity: 99.75% Purity: 99.30% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 50 mg, 100 mg

Pemetrexed disodium Pemetrexed disodium hemipenta hydrate (LY231514 disodium) Cat. No.: HY-10820A (LY231514 (disodium hemipenta hydrate)) Cat. No.: HY-13781

Bioactivity: Pemetrexed disodium is a novel antifolate that inhibits the Bioactivity: Pemetrexed disodium hemipenta hydrate is a novel antifolate,

folatedependent thymidylate synthase, dihydrofolate the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, reductase, and glycinamide ribonucleotide and 65 nM for inhibits thymidylate synthase ( TS), formyltransferase with K s of 1.3, 7.2, and 65 nM, i dihydrofolate reductase ( DHFR), and glycinamide respectively. ribonucleotide formyltransferase ( GARFT), respectively. Purity: 99.77% Purity: 99.78% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in Water, 50 mg, 100 mg, 200 mg 100 mg, 500 mg

Pralatrexate Pyrimethamine Cat. No.: HY-10446 (Pirimecidan; Pirimetamin; RP 4753) Cat. No.: HY-18062

Bioactivity: (Folotyn) is an antifolate, and structurally a Bioactivity: Pyrimethamine(RP4753) is a medication used for protozoal folate analog. Its IC50 is < 300 nM in some cell lines. infections; interferes with tetrahydrofolic acid synthesis IC50 Value: < 300 nM Target: Antifolate Pralatrexate is an from folic acid by inhibiting the enzyme dihydrofolate antifolate (a folate analogue metabolic inhibitor) designed to reductase (DHFR). IC50 Value: 15.4 nM () accumulate preferentially in cancer cells. Based on… [1] Target: DHFR; antifolate in vitro: Three susceptibility… Purity: 99.23% Purity: 99.90% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 100 mg, 500 mg

Trimethoprim Cat. No.: HY-B0510

Bioactivity: Trimethoprim is a bacteriostatic antibiotic used mainly in the prophylaxis and treatment of urinary tract infections.

Purity: 99.98% Clinical Data: Launched Size: 10mM x 1mL in DMSO, 5 g, 10 g

6 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] APC promoting complex

APC (Anaphase-Promoting Complex) is an E3 ubiquitin ligase that marks target cell cycle proteins for degradation by the 26S proteasome. The APC/C is a large complex of 11–13 subunit proteins, including a cullin (Apc2) and RING (Apc11) subunit much like SCF. The APC/C's main function is to trigger the transition from to anaphase by tagging specific proteins for degradation. The two proteins of most importance that get degraded in this process as substrates of the APC/C are securin and S and M cyclins. Securin releases separase, a protease, after being degraded which in turn triggers the cleavage of cohesin, the protein complex that binds sister chromatids together. During metaphase, sister chromatids are linked by intact cohesin complexes. When securin undergoes ubiquitination by the APC/C and releases separase, which degrades cohesin, sister chromatids become free to move to opposite poles for anaphase. The APC/C also targets the mitotic cyclins for degradation, resulting in the inactivation of M-CdK (mitotic cyclin-dependent kinase) complexes, promoting exit from mitosis and cytokinesis.

www.MedChemExpress.com 7 APC Inhibitors & Modulators

TAME TAME hydrochloride Cat. No.: HY-13255 Cat. No.: HY-13255A

Bioactivity: TAME is a serine protease inhibitor and can be also utilized Bioactivity: TAME hydrochloride is a serine protease inhibitor and can be as a substrate for the serine proteases trypsin, plasmin, and also utilized as a substrate for the serine proteases trypsin, thrombin [1] [2] [3]. TAME is an inhibitor of plasmin, and thrombin [1] [2] [3]. TAME hydrochloride is an anaphase-promoting complex (APC), which binds to the … inhibitor of anaphase-promoting complex (APC), which bi…

Purity: 99.11% Purity: 99.10% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 50 mg, 100 mg

8 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] ATM/ATR Ataxia telangiectasia mutated;ATM and RAD3 related

ATM/ATR are members of the PI3 family of serine-threonine kinases and function as essential links between the sensors and effectors of the DNA damage response. The roles of ATM and ATR partially overlap and are cooperative; however they are also known to play distinct roles in protecting the cell from DNA damage. ATM is mostly responsible for sending signals from DSBs (double-strand breaks) induced by ionizing radiation while the closely related ATR responds to UV damage or stalled replication forks. ATM and ATR are known to phosphorylate common as well as specific substrates to activate checkpoint signaling. The G1, S, and G2 cell cycle checkpoints are primarily regulated by the ATM (ataxia telangiectasia, mutated) and ATR (ATM and Rad3-related) protein kinases.

www.MedChemExpress.com 9 ATM/ATR Inhibitors & Modulators

ATM Inhibitor-1 ATR inhibitor 1 Cat. No.: HY-112614 Cat. No.: HY-111451

Bioactivity: ATM Inhibitor-1 is a highly potent, selective and orally Bioactivity: ATR inhibitor 1 is a ATR inhibitor extracted from patent active ATM inhibitor, with an IC of 0.7 nM, shows weak [1] 50 WO2015187451A1, compound I-l, has a Ki value below 1 µΜ . activity against mTOR (IC 50, 21 μM), DNAPK (IC 50, 2.8 μM),

PI3Kα (IC 50, 3.8 μM), PI3Kβ (IC 50, 10.3 μM), PI3Kγ … Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size:

AZ20 AZ32 Cat. No.: HY-15557 Cat. No.: HY-112305

Bioactivity: AZ20 is a potent and selective inhibitor of ATR with an IC50 Bioactivity: AZ32 is an orally bioavailable and blood-brain barrier-penetrating ATM inhibitor with an IC of <6.2 of 5 nM, and has 8-fold selectivity against mTOR (IC 50=38 50 nM). nM for ATM enzyme, and an IC50 of 0.31 μM for ATM in cell.

Purity: 99.84% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

AZD0156 AZD1390 Cat. No.: HY-100016 Cat. No.: HY-109566

Bioactivity: AZD0156 is an oral, potent and selective ATM inhibitor with Bioactivity: AZD1390 is an ATM inhibitor.

an IC50 of 0.58 nM.

Purity: 99.60% Purity: 99.81% Clinical Data: Phase 1 Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

BAY-1895344 BAY-1895344 hydrochloride Cat. No.: HY-101566 Cat. No.: HY-101566A

Bioactivity: BAY-1895344 is a potent, orally available and selective ATR Bioactivity: BAY-1895344 hydrochloride is a potent, orally available and [1] selective ATR inhibitor, with IC of 7 nM. Anti-tumor inhibitor, with IC50 of 7 nM. Anti-tumor activity . 50 activity [1].

Purity: >98% Purity: 99.04% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Berzosertib Ceralasertib (VE-822; VX-970) Cat. No.: HY-13902 (AZD6738) Cat. No.: HY-19323

Bioactivity: Berzosertib (VE-822) is an ATR inhibitor with a Ki value of Bioactivity: Ceralasertib (AZD6738) is a potent inhibitor of ATR kinase with an IC50 of 1 nM. less than 0.2 nM. It also inhibits ATM with a Ki of 34 nM.

Purity: 99.67% Purity: 99.76% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg 5 mg, 10 mg, 50 mg, 100 mg

10 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

CGK733 CP-466722 Cat. No.: HY-15520 Cat. No.: HY-11002

Bioactivity: CGK733 is a potent ATM/ATR inhibitor, used for the research Bioactivity: CP-466722 is a rapidly reversible inhibitor of ATM, with an

of cancer. IC50 of 4.1 μM, and has no effects on PI3K or closely related PI3K-like protein kinase (PIKK) family members.

Purity: 99.93% Purity: 98.40% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 50 mg

ETP-46464 KU 59403 Cat. No.: HY-15521 Cat. No.: HY-18650

Bioactivity: ETP-46464 is an effective mTOR and ATR inhibitor with Bioactivity: KU 59403 is a potent ATM inhibitor, with an IC50 of 3 nM. IC50s of 0.6 and 14 nM, respectively.

Purity: 99.13% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

KU-55933 KU-60019 Cat. No.: HY-12016 Cat. No.: HY-12061

Bioactivity: KU-55933 is a potent ATM inhibitor with an IC50 and Ki of Bioactivity: KU-60019 is an improved ATM kinase-specific inhibitor with IC of 6.3 nM. 12.9 and 2.2 nM, respectively, and is highly selective for ATM 50 as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.

Purity: 99.88% Purity: 98.05% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

VE-821 Wortmannin Cat. No.: HY-14731 (SL-2052; KY-12420) Cat. No.: HY-10197

Bioactivity: VE-821 is a potent ATP-competitive inhibitor of ATR with Ki/ Bioactivity: Wortmannin is a multi-target inhibitor. Wortmannin inhibits PI3K [1], MLCK [1], DNA-PK [2], ATM [2], ATR [2], IC50 of 13 nM/26 nM. [3] and Polo-like kinase 3 ( Plk3 ) with IC50s of 3 nM, 200 nM, 16 nM, 150 nM, 1.8 μM and 48 nM, respectively. Purity: 99.47% Purity: 99.85% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg

www.MedChemExpress.com 11 Aurora Kinase

Aurora kinases are serine/threonine kinases that are essential for cell proliferation. Aurora kinase helps the dividing cell dispense its genetic materials to its daughter cells. More specifically, Aurora kinases play a crucial role in cellular division by controlling chromatid segregation. Defects in this segregation can cause genetic instability, a condition which is highly associated with tumorigenesis. Three Aurora kinases have been identified in mammalian cells to date, Aurora A, Aurora B, Aurora C. Besides being implicated as mitotic regulators, these three kinases have generated significant interest in the cancer research field due to their elevated expression profiles in many human cancers. The human Aurora kinases present a similar domain organization, with a N-terminal domain of 39 to 129 residues in length, a protein kinase domain and a short C-terminal domain containing 15 to 20 residues. The N-terminal domain of three proteins share low sequence conservation, which determines selectivity during protein-protein interactions.

12 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Aurora Kinase Inhibitors & Modulators

Alisertib AMG 900 (MLN 8237) Cat. No.: HY-10971 Cat. No.: HY-13253

Bioactivity: Alisertib (MLN 8237) is an oral active and selective Aurora A Bioactivity: AMG 900 is a potent and highly selective pan-Aurora kinases

kinase inhibitor with an IC50 of 1.2 nM. inhibitor with IC50 of 5 nM, 4 nM and 1 nM for Aurora A, B and C, respectively.

Purity: 99.84% Purity: 98.19% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg 5 mg, 10 mg, 50 mg, 100 mg

AT9283 Aurora A inhibitor I Cat. No.: HY-50514 Cat. No.: HY-70061

Bioactivity: AT9283 is a multitargeted kinase inhibitor which potently Bioactivity: Aurora A inhibitor I is a potent and highly selective Aurora inhibits aurora kinase A/B, JAK2/3 ( IC =1.2 nM, 1.1 nM). 50 A inhibitor with with an IC50 of 3.4 nM.

Purity: 99.13% Purity: 98.74% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Aurora B inhibitor 1 Aurora inhibitor 1 Cat. No.: HY-U00304 Cat. No.: HY-111506

Bioactivity: Aurora B inhibitor 1 is an Aurora B (Aurora-1) inhibitor Bioactivity: Aurora inhibitor 1 is a potent Aurora inhibitor with an IC50 extracted from patent WO2007059299A1, compound 1-3, has a K i of ≤ 4 nM and ≤13 nM for Aurora A and Aurora B kinase, value of <0.010 uM. respectively [1].

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 500 mg, 100 mg, 250 mg

AZD1152 Barasertib-HQPA (Barasertib) Cat. No.: HY-10127 (AZD2811; INH-34; AZD1152-HQPA) Cat. No.: HY-10126

Bioactivity: AZD1152 is a pro-drug of Barasertib-hQPA, which is a highly Bioactivity: AZD1152-HQPA is a highly selective Aurora selective Aurora B inhibitor with IC of 0.37 nM in a 50 B inhibitor with an IC50 of 0.37 nM in a cell-free assay. cell-free assay, and shows 3700-fold selectivity for Aurora B over Aurora A.

Purity: 98.95% Purity: 99.64% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

BI-847325 CCT 137690 Cat. No.: HY-18955 Cat. No.: HY-10804

Bioactivity: BI-847325 is an ATP competitive dual inhibitor of MEK and Bioactivity: CCT 137690 is a potent and orally available aurora kinase

aurora kinases ( AK) with IC50 values of 4 and 15 nM for inhibitor with IC50s of 15, 25, and 19 nM for aurora A, B and human MEK2 and AK-C, respectively. C, respectively.

Purity: 98.42% Purity: 98.33% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 13

CCT129202 CCT241736 Cat. No.: HY-12049 Cat. No.: HY-18161

Bioactivity: CCT129202 is an aurora kinase inhibitor with IC50s of 42, Bioactivity: CCT241736 is a potent and orally bioavailable dual FLT3 and 198, and 227 nM for aurora A, B and C, respectively. Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM; Aurora-B Kd, 48 nM),

FLT3 kinase ( Kd, 6.2 nM), and FLT3 mutants includ… Purity: 95.0% Purity: 99.86% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

CYC-116 Danusertib Cat. No.: HY-10558 (PHA-739358) Cat. No.: HY-10179

Bioactivity: CYC-116 is a potent aurora A and aurora B inhibitor with Bioactivity: Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor

Kis of 8 and 9 nM, respectively. with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.

Purity: 98.17% Purity: 99.44% Clinical Data: Phase 1 Clinical Data: Phase 2 Size: 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

ENMD-2076 ENMD-2076 Tartrate Cat. No.: HY-10987A Cat. No.: HY-10987

Bioactivity: ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of Bioactivity: ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, 50 KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, respectively. PDGFRα, respectively.

Purity: 99.23% Purity: 98.59% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

GSK-1070916 Hesperadin (GSK-1070916A) Cat. No.: HY-70044 Cat. No.: HY-12054

Bioactivity: GSK-1070916 is a potent and selective ATP-competitive Bioactivity: Hesperadin is an ATP-competitive inhibitor of aurora B inhibitor of aurora B and aurora C with K s of 0.38 and i kinase with an IC50 of 250 nM. 1.5 nM, respectively, and is >250- fold selective over Aurora A.

Purity: 99.55% Purity: 98.48% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg 5 mg, 10 mg, 50 mg, 100 mg

Ilorasertib JNJ-7706621 (ABT-348) Cat. No.: HY-16018 Cat. No.: HY-10329

Bioactivity: Ilorasertib (ABT-348) is an ATP-competitive multitargeted Bioactivity: JNJ-7706621 is a potent aurora kinase inhibitor, and also

kinase inhibitor with IC50s for inhibiting binding Aurora B (7 inhibits CDK1 and CDK2, with IC50s of 9, 3, 11, and 15 nM nM), C (1 nM), and A (120 nM), and also inhibits RET tyrosine for CDK1, CDK2, Aurora-A and Aurora-B, respectively.

kinase, PDGFRβ, and Flt1 with IC50s of 7 nM, 3 nM and 32 nM. Purity: >98% Purity: 98.80% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

14 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

KW-2449 LY3295668 Cat. No.: HY-10339 (AK-01) Cat. No.: HY-114258

Bioactivity: KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, Bioactivity: LY3295668 is a potent, orally active and highly specific T315I Aurora-A kinase inhibitor, with K values of 0.8 nM and 1038 ABL and Aurora kinase with IC50s of 6.6, 14, 4 and 48 nM, i respectively. nM for AurA and AurB, respectively.

Purity: 99.85% Purity: 99.61% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

MK-5108 MK-8745 (VX-689) Cat. No.: HY-13252 Cat. No.: HY-13819

Bioactivity: MK-5108 is a highly potent and specific inhibitor of Aurora A Bioactivity: MK-8745 is an aurora A kinase inhibitor with an IC50 of 0.6 kinase with an IC value of 0.064 nM. 50 nM.

Purity: 99.11% Purity: 99.28% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

MLN8054 NU6140 Cat. No.: HY-10180 Cat. No.: HY-107419

Bioactivity: MLN8054 is a potent, selective and orally available aurora A Bioactivity: NU6140 is a selective CDK2-cyclin A inhibitor ( IC50, 0.41 kinase inhibitor with an IC of 4 nM. 50 μM), exhibits 10- to 36-fold selectivity over other CDKs [1]. NU6140 also potently inhibits Aurora A and Aurora B, with [2] IC50s of 67 and 35 nM, respectively . Enhances … Purity: 98.0% Purity: 99.0% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg 5 mg, 10 mg, 50 mg, 100 mg

PF-03814735 PHA-680632 Cat. No.: HY-14574 Cat. No.: HY-10178

Bioactivity: PF-03814735 is a potent, orally available and reversible Bioactivity: PHA-680632 is an aurora kinase inhibitor with IC50s of 27, aurora A and aurora B inhibitor with IC s of 0.8 and 0.5 50 135 and 120 nM for aurora A, B and C, respectively. nM, respectively.

Purity: 99.77% Purity: 98.02% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

Reversine SCH-1473759 Cat. No.: HY-14711 Cat. No.: HY-10482

Bioactivity: Reversine is a novel class of ATP-competitive Aurora kinase Bioactivity: SCH-1473759 is an aurora inhibitor with IC50s of 4 and 13 nM inhibitor with IC s of 400, 500 and 400 nM for Aurora A, 50 for aurora A and B, respectively. Aurora B and Aurora C, respectively.

Purity: 99.25% Purity: 98.20% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 2 mg, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 15

SCH-1473759 hydrochloride SNS-314 Cat. No.: HY-10483 (SNS-314 Mesylate) Cat. No.: HY-12003

Bioactivity: SCH-1473759 hydrochloride is an aurora inhibitor with IC50s Bioactivity: SNS-314 is a potent and selective aurora kinase inhibitor with IC s of 9, 31, and 6 nM for aurora A, B and C, of 4 and 13 nM for aurora A and B, respectively. 50 respectively.

Purity: 99.67% Purity: 99.81% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg 5 mg, 10 mg, 50 mg, 100 mg

TAK-632 TAK-901 Cat. No.: HY-15767 Cat. No.: HY-12201

Bioactivity: TAK-632 is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 Bioactivity: TAK-901 is a multi-targeted aurora inhibitor with IC50s of 21 and 8.3 nM for CRAF, BRAFV600E, BRAFWT, respectively. and 15 nM for aurora A and B, respectively.

Purity: 99.13% Purity: 99.80% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Tozasertib XL228 (VX 680; MK-0457) Cat. No.: HY-10161 Cat. No.: HY-15749

Bioactivity: Tozasertib (VX 680; MK-0457) is an inhibitor of Aurora A/B/C Bioactivity: XL228 is a multi-targeted tyrosine kinase inhibitor with IC50s kinases with K s of 0.6, 18, 4.6 nM, respectively. i of 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src and Lyn, respectively.

Purity: 99.85% Purity: 99.61% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 250 mg 5 mg, 10 mg, 50 mg, 100 mg

ZM-447439 Cat. No.: HY-10128

Bioactivity: ZM-447439 is an aurora kinase inhibitor with IC50s of 110 and 130 nM for aurora A and B, respectively.

Purity: 98.59% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

16 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Casein Kinase

Casein Kinases (CKs) are serine/threonine-selective enzymes that function as regulators of signal transduction pathways in most eukaryotic cell types.

www.MedChemExpress.com 17 Casein Kinase Inhibitors & Modulators

Casein Kinase II Inhibitor IV Casein Kinase II Inhibitor IV Hydrochloride Cat. No.: HY-111378 Cat. No.: HY-111378A

Bioactivity: Casein Kinase II Inhibitor IV is a small-molecule inducer of Bioactivity: Casein Kinase II Inhibitor IV Hydrochloride is a epidermal keratinocyte differentiation. small-molecule inducer of epidermal keratinocyte differentiation.

Purity: 98.08% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

CK1-IN-1 D4476 Cat. No.: HY-111820 (Casein Kinase I Inhibitor) Cat. No.: HY-10324

Bioactivity: CK1-IN-1 is a casein kinase 1 (CK1) inhibitor extracted from Bioactivity: D4476 is a potent, selective and cell-permeable inhibitor of casein kinase 1( CK1) with an IC value of 0.3 μM in vitro. patent WO2015119579A1, compound 1c, has IC50s of 15 nM, 16 nM, 50 73 nM for CK1δ, and CK1ε, p38σ MAPK, respectively [1].

Purity: 98.00% Purity: 99.64% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

DMAT Ellagic acid (Casein kinase II Inhibitor; CK2 Inhibitor) Cat. No.: HY-15535 Cat. No.: HY-B0183

Bioactivity: DMAT is a potent and specific CK2 inhibitor with an IC50 Bioactivity: Ellagic acid is a natural antioxidant, and acts as a potent and ATP-competitive CK2 inhibitor, with an IC of 40 nM and value of 130 nM. 50

a Ki of 20 nM.

Purity: 98.0% Purity: 99.92% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 1 g, 5 g 10 mg, 50 mg

Emodin IC261 (Frangula ) Cat. No.: HY-14393 Cat. No.: HY-12774

Bioactivity: Emodin is a broad-spectrum anticancer agent. Emodin inhibits Bioactivity: IC261 is a selective, ATP-competitive CK1 inhibitor, with casein kinase II (CKII) activity with IC of 2 μM. 50 IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively.

Purity: 98.0% Purity: 99.67% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 200 mg 5 mg, 10 mg, 50 mg

LH846 Longdaysin Cat. No.: HY-15704 Cat. No.: HY-18285

Bioactivity: LH846 is a selective inhibitor of CKIδ, with an IC50 of 290 nM, Bioactivity: Longdaysin is a CK1α, CK1δ, and extracellular signal-regulated kinase 2 (ERK2) inhibitor with IC50s of 5.6 and less potently inhibits CKIα and CKIε, with IC50s of 2.5 μM [1] [2] and 1.3 μM, respectively. µM, 8.8 µM, and 52 µM, respectively .

Purity: 98.02% Purity: 99.92% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

18 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

NCC007 PF-4800567 Cat. No.: HY-128677 Cat. No.: HY-12470

Bioactivity: NCC007 is a dual casein kinase Iα (CKIα) and δ (CKIδ) inhibitor Bioactivity: PF-4800567 is a potent and selective inhibitor of casein kinase 1ϵ ( CK1ϵ), with an IC of 32 nM, which is greater with IC50s of 1.8 and 3.6 μM, respectively, and can be used in 50 [1] research of modulating mammalian circadian rhythms . than 20-fold selectivity over CK1δ ( IC50, 711 nM).

Purity: >98% Purity: 98.38% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

PF-670462 Silmitasertib Cat. No.: HY-15490 (CX-4945) Cat. No.: HY-50855

Bioactivity: PF-670462 is a potent and selective inhibitor of casein kinase Bioactivity: Silmitasertib (CX-4945) is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC values of 1 nM (CK1ε and CK1δ), with IC50s of 7.7 nM and 14 nM, 50 respectively. against CK2α and CK2α'.

Purity: 99.96% Purity: 99.92% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

Silmitasertib sodium salt SR-3029 (CX-4945 (sodium salt)) Cat. No.: HY-50855B Cat. No.: HY-100011

Bioactivity: Silmitasertib sodium salt is an orally bioavailable, highly Bioactivity: SR-3029 is a potent and ATP competitive CK1δ and CK1ε selective and potent CK2 inhibitor, with IC values of 1 nM 50 inhibitor, with IC50s of 44 nM and 260 nM, respectively, and against CK2α and CK2α'. Kis of 97 nM for both kinases.

Purity: 99.98% Purity: 99.58% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg

TA-01 TBB Cat. No.: HY-100114 (NSC 231634; Casein Kinase II Inhibitor I) Cat. No.: HY-14394

Bioactivity: TA-01 is a potent CK1 and p38 MAPK inhibitor, with IC50s Bioactivity: TBB is a cell-permeable and ATP-competitive CK2 inhibitor with an IC of 0.15 μM for rat liver CK2. of 6.4 nM, 6.8 nM, 6.7 nM for CK1ε, CK1δ and p38 MAPK, 50 respectively.

Purity: 99.93% Purity: 98.27% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 10 mg, 50 mg

TTP 22 Cat. No.: HY-15479

Bioactivity: TTP 22 is a potent CK2 inhibitor, with an IC50 of 100 nM and

a Ki of 40 nM.

Purity: 97.01% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

www.MedChemExpress.com 19 CDK Cyclin dependent kinase

CDKs (Cyclin-dependent kinases) are serine-threonine kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. CDKs are relatively small proteins, with molecular weights ranging from 34 to 40 kDa, and contain little more than the kinase domain. In fact, yeast cells can proliferate normally when their CDK gene has been replaced with the homologous human gene. By definition, a CDK binds a regulatory protein called a cyclin. Without cyclin, CDK has little kinase activity; only the cyclin-CDK complex is an active kinase. There are around 20 Cyclin-dependent kinases (CDK1-20) known till date. CDK1, 4 and 5 are involved in cell cycle, and CDK 7, 8, 9 and 11 are associated with transcription. CDK levels remain relatively constant throughout the cell cycle and most regulation is post-translational. Most knowledge of CDK structure and function is based on CDKs of S. pombe (Cdc2), S. cerevisia (CDC28), and vertebrates (CDC2 and CDK2). The four major mechanisms of CDK regulation are cyclin binding, CAK phosphorylation, regulatory inhibitory phosphorylation, and binding of CDK inhibitory subunits (CKIs).

20 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] CDK Inhibitors & Modulators

(+)-BAY-1251152 (-)-BAY-1251152 Cat. No.: HY-103019 Cat. No.: HY-103019B

Bioactivity: (+)-BAY-1251152 is a CDK9 inhibitor extracted from patent WO Bioactivity: (-)-BAY-1251152 is an enanthiomer of BAY-1251152 with rotation 2014076091 A1, example 1. (-). BAY-1251152 is a potent and highly selective PTEF/CDK9 inhibitor.

Purity: 99.66% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg 2 mg, 5 mg, 10 mg, 50 mg

(±)-BAY-1251152 5-Iodo-indirubin-3'-monoxime Cat. No.: HY-103019A Cat. No.: HY-111930

Bioactivity: (±)-BAY-1251152 is a racemic mixture of BAY-1251152. Bioactivity: 5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 BAY-1251152 is a potent and highly selective PTEF/CDK9 and CDK1/cyclin B inhibitor, competing with ATP for binding to inhibitor. the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively [1]. Purity: 99.73% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 500 mg, 250 mg 2 mg, 5 mg, 10 mg, 50 mg

Abemaciclib Metabolites M2 (LY2835219) Cat. No.: HY-16297A Cat. No.: HY-128669

Bioactivity: Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with Bioactivity: Abemaciclib Metabolites M2 is a metabolite of abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC s in the IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively. 50 range of 1-3 nM. Anti-cancer activity [1].

Purity: 99.69% Purity: >98% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size:

Abemaciclib methanesulfonate AMG 925 (LY2835219 (methanesulfonate)) Cat. No.: HY-16297 Cat. No.: HY-15889

Bioactivity: Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a Bioactivity: AMG 925 is a potent, selective, and orally available FLT3/ selective CDK4/6 inhibitor with IC s of 2 nM and 10 nM for 50 CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, CDK4 and CDK6, respectively. respectively.

Purity: 99.95% Purity: 99.33% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

AMG 925 HCl AT7519 Cat. No.: HY-15889A Cat. No.: HY-50940

Bioactivity: AMG 925 HCl is a potent, selective, and orally available Bioactivity: AT7519 as a potent inhibitor of CDKs, with IC50s of 210, 47, FLT3/ CDK4 dual inhibitor with IC s of 2±1 nM and 3±1 nM, 50 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and respectively. CDK9, respectively.

Purity: 98.01% Purity: 98.15% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 21

AT7519 Hydrochloride AT7519 trifluoroacetate Cat. No.: HY-50943 Cat. No.: HY-50940A

Bioactivity: AT7519 Hydrochloride is a potent inhibitor of CDKs, with Bioactivity: AT7519 trifluoroacetate as a potent inhibitor of CDKs, with

IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively. CDK4 to CDK6, and CDK9, respectively.

Purity: 99.99% Purity: 98.16% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Atuveciclib Atuveciclib Racemate (BAY-1143572) Cat. No.: HY-12871B (BAY-1143572 Racemate) Cat. No.: HY-12871

Bioactivity: Atuveciclib (BAY-1143572) is a potent and highly selective, Bioactivity: Atuveciclib Racemate (BAY-1143572 Racemate) is the racemate oral PTEFb/ CDK9 inhibitor. Atuveciclib (BAY-1143572) mixture of Atuveciclib. Atuveciclib is a potent and highly

inhibits CDK9/ CycT1 with an IC50 of 13 nM. selective, oral P-TEFb/ CDK9 inhibitor which supresses CDK9/ CycT1 with an IC50 of 13 nM.

Purity: 99.42% Purity: 98.48% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 1 mg, 5 mg, 10 mg, 25 mg

Atuveciclib S-Enantiomer AUZ 454 (BAY-1143572 S-Enantiomer) Cat. No.: HY-12871C (K03861) Cat. No.: HY-15004

Bioactivity: Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) is a Bioactivity: AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 potent and selective CDK9 inhibitor, which inhibits CDK9/ nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with

CycT1 with an IC50 of 16 nM. binding of activating cyclins.

Purity: 97.00% Purity: 99.99% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg

AZD-5438 AZD4573 Cat. No.: HY-10012 Cat. No.: HY-112088

Bioactivity: AZD-5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 Bioactivity: AZD4573 is a CDK9 inhibitor with an IC50 of <3 nM nM/6 nM/20 nM in cell-free assays. AZD-5438 shows less extracted from patent US 20160376287 A1, example 14. inhibition activity against GSK3β, CDK5 and CDK6.

Purity: 99.84% Purity: 99.80% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

BGG463 BI-1347 Cat. No.: HY-100600 Cat. No.: HY-120350

Bioactivity: BGG463 is a CDK2 inhibitor. Bioactivity: BI-1347 is a potent CDK8 inhibitor extracted from patent [1] WO2017202719A1, product I-003, has an IC50 of 1.1 nM .

Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

22 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

BMS-265246 BS-181 Cat. No.: HY-15275 Cat. No.: HY-13266

Bioactivity: BMS-265246 is a potent and selective CDK1/2 inhibitor for Bioactivity: BS-181 is a highly selective CDK7 inhibitor with an IC50 of CDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM and 9 nM, 21 nM, showing 40-fold selective over CDK1, 2, 4, 5, 6, or 9. respectively.

Purity: 97.47% Purity: 99.62% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

BS-181 hydrochloride BSJ-03-123 Cat. No.: HY-13266A Cat. No.: HY-111556

Bioactivity: BS-181 hydrochloride is a highly selective CDK7 inhibitor Bioactivity: BSJ-03-123 is a potent and novel CDK6-selective small-molecule

with IC50 of 21 nM, and > 40-fold selective for CDK7 than degrader. CDK1, 2, 4, 5, 6, or 9.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Ca2+ channel agonist 1 CC-671 Cat. No.: HY-41076 Cat. No.: HY-108709

Bioactivity: Ca 2+ channel agonist 1 is an agonist of N-type Ca2+ channel Bioactivity: CC-671 is a dual TTK protein kinase/ CDC2-like kinase ( CLK2) inhibitor with IC s of 0.005 and 0.006 μM for TTK and CLK2, and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 50 μM, respectively, and is used as a potential treatment for respectively. motor nerve terminal dysfunction. Purity: 99.00% Purity: 98.86% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

CCT-251921 CDK-IN-2 Cat. No.: HY-19984 (CDK inhibitor II) Cat. No.: HY-13033

Bioactivity: CCT-251921 is a potent, selective, and orally bioavailable Bioactivity: CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of

CDK8 inhibitor with an IC50 of 2.3 nM. <8 nM, extracted from reference 1, example 4. IC50 Value: <8 nM [1] Target: CDK9 In vitro: In vivo:

Purity: 98.70% Purity: 97.54% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 2 mg, 5 mg, 10 mg, 50 mg

CDK4/6-IN-2 CDK4/6/1 Inhibitor Cat. No.: HY-114339 Cat. No.: HY-112280

Bioactivity: CDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor extracted Bioactivity: CDK4/6/1 Inhibitor is a CDK4/6 inhibitor with IC50s of 3 and from patent US20180000819A1, Compound 1, has IC s of 2.7 and 50 1 nM, respectively. 16 nM for CDK4 and CDK6, respectively [1].

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 23

CDK8-IN-1 CDK8-IN-3 Cat. No.: HY-103492 Cat. No.: HY-111463

Bioactivity: CDK8-IN-1 is a potent and selective CDK8 inhibitor with an Bioactivity: CDK8-IN-3 is an inhibitor of CDK8 extracted from patent

IC50 of 3 nM. WO2016041618A1, compound example 1.7.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 250 mg, 500 mg

CDK8-IN-4 CDK8/19-IN-1 Cat. No.: HY-111465 Cat. No.: HY-111427

Bioactivity: CDK8-IN-4 is an inhibitor of CDK8 extracted from patent Bioactivity: CDK8/19-IN-1 is a potent, selective and oral bioavailable CDK8/19 dual inhibitor, with IC s of 0.46 nM, 0.99 nM and WO2014090692A1, compound example 16, with an IC50 of 0.2 nM. 50 270 nM for CDK8, CDK19 and CDK9, respectively.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 250 mg, 500 mg

CDK9 Antagonist-1 CDK9-IN-1 Cat. No.: HY-112811 Cat. No.: HY-13231

Bioactivity: CDK9 Antagonist-1 (compounds 11c) is a potent and selective Bioactivity: CDK9-IN-1 is a novel, selective CDK9 inhibitor for the CDK9 degrader based on PROTAC, with an IC of 17 μM in MCF-7 50 treatment of HIV infection, with an IC50 of 39 nM for cell lines. Natural product Wogonin binds ubiquitin E3 ligase CDK9/CycT1, extracted from reference, compound 87. cereblon (CRBN) via a linker to form PROTAC [1]. Purity: >98% Purity: 95.48% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 100 mg, 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

CDK9-IN-2 CDK9-IN-8 Cat. No.: HY-16462 Cat. No.: HY-102039

Bioactivity: CDK9-IN-2 is a special cyclin-dependent kinase 9 ( CDK9) Bioactivity: CDK9-IN-8 is a highly effective and selective CDK9 inhibitor

inhibitor, extracted from patent WO/2012131594A1, compound with an IC50 of 12 nM. CDKI(8), has an IC50 of 5 nM and 7 nM in H929 multiple myeloma(MM) cell line (72 hours) and A2058 skin cell line (72 hours), respectively. Purity: 99.83% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 500 mg, 250 mg 5 mg, 10 mg, 50 mg

CDKI-73 CLK1-IN-1 Cat. No.: HY-12445 Cat. No.: HY-103082

Bioactivity: CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM; shows Bioactivity: CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 (

selective toxicity to CLL cells(LD50=80 nM) versus normal B CLK1) inhibitor, with an IC 50 of 2 nM. cell and normal CD34+ cell(LD50>20 uM). IC50 value: 4 nM/80 nM(Ki/LD50) [1] Target: CDK9 inhibitor in vitro: CDKI-73 was cytotoxic to all of the CLL samples tested (n = 38) with a… Purity: 99.58% Purity: 99.03% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

24 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

CMPD 7 CT7001 hydrochloride Cat. No.: HY-112261 (ICEC0942 hydrochloride) Cat. No.: HY-103712A

Bioactivity: CMPD 7 is a potent and selective CDK12 inhibitor with an IC50 Bioactivity: CT7001 hydrochloride is a selective CDK7 inhibitor, with IC s of 41 nM and 578 nM for CDK7/CycH/MAT1 and of 491 nM in enzymatic assay. 50 CDK2/cycE1, respectively.

Purity: >98% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Cucurbitacin E CVT-313 (α-Elaterin; α-Elaterine) Cat. No.: HY-N0417 (Cdk2 Inhibitor III) Cat. No.: HY-15339

Bioactivity: Cucurbitacin E is a natural compound which from the climbing Bioactivity: CVT-313 is a potent, selective, reversible, and

stem of Cucumic melo L. Cucurbitacin E significantly ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. suppresses the activity of the cyclin B1/ CDC2 complex.

Purity: 99.30% Purity: 99.52% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 5 mg, 10 mg, 50 mg

CYC065 Dinaciclib Cat. No.: HY-101212 (SCH 727965) Cat. No.: HY-10492

Bioactivity: CYC065 is a second-generation, orally available Bioactivity: Dinaciclib is a potent inhibitor of CDK, with IC50s of 1, 1, ATP-competitive inhibitor of CDK2/ CDK 9 kinases. 3, and 4 nM for CDK2, CDK5, CDK1, and CDK9, respectively.

Purity: 98.58% Purity: 99.73% Clinical Data: Phase 1 Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

EHT 5372 Flavopiridol Cat. No.: HY-111380 (L868275; HMR-1275; ) Cat. No.: HY-10005

Bioactivity: EHT 5372 is a strong inhibitor of DYRK’s family kinases, with Bioactivity: Flavopiridol is a broad spectrum and competitive inhibitor of CDKs, inhibiting CDK1, CDK2, CDK4 with IC s of 30, 170, 100 IC50s of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively. 50 nM, respectively.

Purity: >98% Purity: 99.70% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 250 mg, 500 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

Flavopiridol Hydrochloride (HL 275; NSC 649890; MDL 107826A; FMF-04-159-2 FLAVOPIRIDOL HCL; Alvocidib Hydrochloride) Cat. No.: HY-10006 Cat. No.: HY-127104

Bioactivity: Flavopiridol Hydrochloride is a broad inhibitor of CDK, Bioactivity: FMF-04-159-2 is a covalent CDK14 inhibitor. FMF-04-159-2

competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 inhibits CDK14 and CDK2 with IC50s of 39.6 nM and 256 nM in with IC s of 30, 170, 100 nM, respectively. 50 NanoBRET assay, respectively [1].

Purity: 99.00% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 250 mg, 500 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 25

FN-1501 GSK 3 Inhibitor IX Cat. No.: HY-111361 (6-Bromoindirubin-3'-oxime; BIO; MLS 2052) Cat. No.: HY-10580

Bioactivity: FN-1501 is a potent inhibitor of FLT3 and CDK, with IC50s of Bioactivity: GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC s of 5 nM/320 D1, CDK6/cyclin D1 and FLT3, respectively; FN-1501 has 50 anticancer activity. nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively. Purity: 98.41% Purity: 99.66% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

GSK3186899 IIIM-290 (DDD-853651) Cat. No.: HY-112622 Cat. No.: HY-111356

Bioactivity: GSK3186899 is an inhibitor of cdc-2-related kinase 12 ( Bioactivity: IIIM-290 is a potent and oral CDK inhibitor with IC50s of 90 CRK12), with an EC of 1.4 μM for L. donovani in an 50 and 94 nM for CDK2/A and CDK9/T1. intra-macrophage assay.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 251 mg, 500 mg, 250 mg

Indirubin-3'-monoxime-5-sulphonic acid Indirubin-5-sulfonate Cat. No.: HY-111931 Cat. No.: HY-111932

Bioactivity: Indirubin-3'-monoxime-5-sulphonic acid is a potent and Bioactivity: Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) selective inhibitor of CDK1, CDK5, and GSK-3β with IC s of 50 inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM 5 nM, 7 nM, and 80 nM, respectively [1]. and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively [1] Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 250 mg, 500 mg

JH-XI-10-02 JNJ-7706621 Cat. No.: HY-111518 Cat. No.: HY-10329

Bioactivity: JH-XI-10-02 is a potent and selective degrader of CDK8, with Bioactivity: JNJ-7706621 is a potent aurora kinase inhibitor, and also

an IC50 of 159 nM, based on PROTAC. JH-XI-10-02 causes inhibits CDK1 and CDK2, with IC50s of 9, 3, 11, and 15 nM proteasomal degradation, does not affect CDK8 mRNA levels. for CDK1, CDK2, Aurora-A and Aurora-B, respectively. JH-XI-10-02 shows no effect on CDK19 [1]. Purity: >98% Purity: 98.80% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 100 mg, 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

JSH-150 Kenpaullone Cat. No.: HY-X0150 (9-Bromopaullone; NSC-664704) Cat. No.: HY-12302

Bioactivity: JSH-150 is a highly selective and potent CDK9 inhibitor with Bioactivity: Kenpaullone is a potent inhibitor of CDK1/cyclin B and

an IC 50 of 1 nM. GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits

CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively. Purity: 92.04% Purity: 98.07% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 50 mg

26 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

KH-CB19 LDC000067 Cat. No.: HY-12828 (LDC067) Cat. No.: HY-15878

Bioactivity: KH-CB19 is a potent and highly specific inhibitor of the Bioactivity: LDC000067 is a highly specific CDK9 inhibitor with an IC50 CDC2-like kinase isoforms 1 and 4 (CLK1/CLK4). IC50 value: 20 value of 44±10 nM in vitro. nM (CLK1) [1] Target: CLK1/4 inhibitor in vitro: KH-CB19 showed potent inhibition of CLK1 with an IC50 of 20 nM, and for the pure isomer KH-CB19, almost 100-fold selectivity… Purity: 99.31% Purity: 98.14% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg 10 mg, 50 mg

LDC4297 Lerociclib Cat. No.: HY-12653 (G1T38) Cat. No.: HY-112272

Bioactivity: LDC4297 is a potent and selective CDK7 inhibitor with an IC50 Bioactivity: Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC s of 1 nM, 2 nM for CDK4/CyclinD1 and of 0.13 nM. 50 CDK6/CyclinD3, respectively.

Purity: 99.14% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Lerociclib dihydrochloride LY2857785 (G1T38 dihydrochloride) Cat. No.: HY-112272A Cat. No.: HY-12293

Bioactivity: Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent Bioactivity: LY2857785 is a type I reversible and competitive ATP kinase

and selective inhibitor of CDK4/ CDK6, with IC50s of 1 nM inhibitor against CDK9 ( IC50 11 nM) and other transcription

and 2 nM for CDK4/ CyclinD1 and CDK6/ CyclinD3, respectively. kinases CDK8 ( IC50 16 nM), and CDK7 ( IC50 246 nM).

Purity: 98.45% Purity: 98.59% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

LY3177833 MBQ-167 Cat. No.: HY-100023 Cat. No.: HY-112842

Bioactivity: LY3177833 is an CDC7 and pMCM2 inhibitor extracted from Bioactivity: MBQ-167 is a dual Rac/Cdc42 inhibitor, with IC50s of 103 nM patent US 20140275131and patent WO 2014143601 A1 compound for Rac 1/2/3 and 78 nM for Cdc42 in MDA-MB-231 cells, example 4; has IC values of 3.3 nM and 290 nM, respectively. 50 respectively.

Purity: 99.90% Purity: 99.26% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

MC180295 Milciclib ((rel)-MC180295) Cat. No.: HY-119940 (PHA-848125) Cat. No.: HY-10424

Bioactivity: MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin Bioactivity: Milciclib (PHA-848125) is a potent, dual inhibitor of CDK and

T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, selective for CDK9 over other CDKs. MC180295 also inhibits 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has pot… cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively. Purity: 98.47% Purity: 98.61% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 27

ML167 MSC2530818 (CID44968231; NCGC00188654) Cat. No.: HY-15951 Cat. No.: HY-101611

Bioactivity: ML167 is a highly selective Cdc2-like kinase 4 ( Clk4) Bioactivity: MSC2530818 is a potent, selective and orally available CDK8

inhibitor with IC50 of 136 nM, >10-fold selectivity for inhibitor with an IC50 of 2.6 nM for CDK8. closely related kinases Clk1, Clk2, Clk3 and Dyrk1A/1B.

Purity: 98.51% Purity: 99.59% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

NG 52 Nimbolide (Compound 52) Cat. No.: HY-15154 Cat. No.: HY-116035

Bioactivity: NG 52 (Compound 52 ) is a potent, cell-permeable, reversible, Bioactivity: Nimbolide is a triterpene derived from the leaves and flowers selective, and ATP-compatible inhibitor of the cell of neem ( Azadirachta indica L). Nimbolide induces apoptosis cycle-regulating kinase, Cdc28p (IC50 = 7 μM), and the related through inactivation of NF-κB. Nimbolide inhibits CDK4/ Pho85p kinase (IC50 = 2 μM). CDK6 kinase activity. Nimbolide suppresses the NF-κB, Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways [1]. Purity: 99.93% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg

NU2058 NU6140 (O6-(Cyclohexylmethyl)) Cat. No.: HY-19316 Cat. No.: HY-107419

Bioactivity: NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and Bioactivity: NU6140 is a selective CDK2-cyclin A inhibitor ( IC50, 0.41 26 μM for CDK2 and CDK1. IC50 value: 17μM (CDK2), 26μM (CDK1) μM), exhibits 10- to 36-fold selectivity over other CDKs [1]. Target: CDK in vitro: NU2058 is a competitive inhibitor of NU6140 also potently inhibits Aurora A and Aurora B, with CDK2 with respect to ATP (Ki value CDK2, 12 3 μM) that binds [2] in the ATP binding pocket in a different orientation from… IC50s of 67 and 35 nM, respectively . Enhances … Purity: 99.01% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg 5 mg, 10 mg, 50 mg, 100 mg

NU6300 NVP-2 Cat. No.: HY-18930 Cat. No.: HY-12214A

Bioactivity: NU6300 is the first covalent ATP-competitive CDK2 inhibitor. Bioactivity: NVP-2 is a CDK9 inhibitor with an IC50 of 0.5 nM. IC50 value: Target: CDK2 in vitro: NU6300 is a covalent CDK2 inhibitor that illustrates the potential of using vinyl sulfones to mediate irreversible inhibition. NU6300 blocks the inhibitor binding site. The effect was time dependent and… Purity: 97.03% Purity: 99.29% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

NVP-LCQ195 ON-013100 (LCQ-195; AT9311) Cat. No.: HY-15241 Cat. No.: HY-112822

Bioactivity: NVP-LCQ195 (AT9311; LCQ195) is a small molecule heterocyclic Bioactivity: ON-013100, an antineoplastic drug, acts a mitotic inhibitor inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM. that could inhibit Cyclin D1 expression.

Purity: 98.99% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

28 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

ON123300 Cat. No.: HY-12624 (PD 0332991) Cat. No.: HY-50767

Bioactivity: ON123300 is a potent inhibitor of CDK4, with an IC50 of 3.8 Bioactivity: Palbociclib (PD 0332991) is a selective CDK4 and CDK6 nM, with little inhibitory activity against CDKs 1,2,5 and 8. inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib is a drug for the treatment of ER-positive and HER2-negative .

Purity: >98% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: Launched Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g

Palbociclib hydrochloride Palbociclib isethionate (PD 0332991 hydrochloride) Cat. No.: HY-50767A (PD 0332991 isethionate) Cat. No.: HY-A0065

Bioactivity: Palbociclib hydrochloride is a highly selective CDK4/6 Bioactivity: Palbociclib isethionate is a highly selective inhibitor of CDK4/6 with IC s of 11 nM/16 nM, inhibitor with IC50s of 11 nM and 16 nM, respectively. 50 respectively.

Purity: 99.94% Purity: 99.99% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

PF-06873600 PHA-767491 Cat. No.: HY-114177 (CAY10572) Cat. No.: HY-13461

Bioactivity: PF-06873600 is a selective and orally bioavailable inhibitor Bioactivity: PHA-767491 is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM of cyclin-dependent kinase (CDK), with K values of 0.09 nM, i and 34 nM, respectively. 0.13 nM and 0.16 nM for CDK2, CDK4 and CDK6, respectively. PF-06873600 has potential antineoplastic activity [1] [2]. Purity: 99.98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

PHA-767491 hydrochloride PHA-793887 (CAY-10572 hydrochloride) Cat. No.: HY-13461A Cat. No.: HY-11001

Bioactivity: PHA-767491 hydrochloride is a dual Cdc7/Cdk9 inhibitor, with Bioactivity: PHA-793887 is a potent, ATP-competitive CDK inhibitor, can

IC50s of 10 nM and 34 nM, respectively. inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC50s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen

synthase kinase 3β with an IC50 of 79 nM. Purity: 99.91% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

PROTAC CDK9 Degrader-1 Purvalanol A Cat. No.: HY-103628 (NG-60) Cat. No.: HY-18299A

Bioactivity: PROTAC CDK9 Degrader-1 is a selective CDK9 degrader. Bioactivity: Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1,

and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.

Purity: 99.04% Purity: 98.66% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 29

Purvalanol B R547 (NG 95) Cat. No.: HY-18299 Cat. No.: HY-10014

Bioactivity: Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitor Bioactivity: R547 is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki with IC50 values of 6, 6, 9, > 10,000, and 6 nM for of 2 nM/3 nM/1 nM. cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively.

Purity: 97.0% Purity: 98.42% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 10 mg, 50 mg

RGB-286638 RGB-286638 free base Cat. No.: HY-15504 Cat. No.: HY-15504A

Bioactivity: RGB-286638 is a CDK inhibitor that inhibits the kinase Bioactivity: RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2,

cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TA… 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TA…

Purity: >98% Purity: 99.55% Clinical Data: Phase 1 Clinical Data: Phase 1 Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Ribociclib hydrochloride (LEE011) Cat. No.: HY-15777 (LEE011 (hydrochloride)) Cat. No.: HY-15777A

Bioactivity: Ribociclib (LEE011) is a highly specific CDK4/6 inhibitor Bioactivity: Ribociclib hydrochloride (LEE011 hydrochloride) is a highly specific CDK4/6 inhibitor with IC values of 10 nM and 39 with IC50s of 10 nM and 39 nM, respectively. 50 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

Purity: 99.85% Purity: 99.83% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Ribociclib succinate Ribociclib succinate hydrate (LEE011 (succinate)) Cat. No.: HY-15777B (LEE011 (succinate hydrate)) Cat. No.: HY-15777C

Bioactivity: Ribociclib succinate (LEE011 succinate) is a highly specific Bioactivity: Ribociclib succinate hydrate (LEE011 succinate hydrate) is a

CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, highly specific CDK4/6 inhibitor with IC50 values of 10 nM respectively, and is over 1,000-fold less potent against the and 39 nM, respectively, and is over 1,000-fold less potent cyclin B/CDK1 complex. against the cyclin B/CDK1 complex.

Purity: 99.93% Purity: 99.00% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

Riviciclib Riviciclib hydrochloride (P276-00 (free base)) Cat. No.: HY-16559A (P276-00) Cat. No.: HY-16559

Bioactivity: Riviciclib (P276-00 free base) is a potent cyclin-dependent Bioactivity: Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1,

CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively [1] [2]. Riviciclib shows antitu… and 79 nM, respectively [1] [2]. Riviciclib hydrochlor… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 500 mg, 250 mg

30 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Ro-3306 Roniciclib Cat. No.: HY-12529 (BAY 1000394) Cat. No.: HY-13914

Bioactivity: Ro-3306 is a potent and selective inhibitor of CDK1, with Kis Bioactivity: Roniciclib is an orally bioavailable pan-cyclin dependent kinase (CDK) inhibitor, with IC s of 5-25 nM for CDK1, CDK2, of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and 50 CDK2/cyclin E, respectively. CDK3, CDK4, CDK7 and CDK9.

Purity: 96.77% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

SB1317 SEL120-34A (TG02) Cat. No.: HY-15166 Cat. No.: HY-111388

Bioactivity: SB1317 is a potent inhibitor of CDK2, JAK2, and FLT3 for Bioactivity: SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC s of 4.4 nM and 10.4 the treatment of cancer, with IC50 of 13, 73, and 56 nM for 50 CDK2, JAK2 and FLT3, respectively. nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.

Purity: 99.96% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

SEL120-34A HCl SEL120-34A monohydrochloride Cat. No.: HY-111388B Cat. No.: HY-111388A

Bioactivity: SEL120-34A HCl is a potent, selective, orally available, Bioactivity: SEL120-34A monohydrochloride is an ATP-competitive and

ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC s of 4.4 nM and nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor 50 activity. 10.4 nM, respectively, with a Kd of 3 nM for CD… Purity: 99.80% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Seliciclib Senexin A (Roscovitine; CYC202; R-roscovitine) Cat. No.: HY-30237 Cat. No.: HY-15681

Bioactivity: (Roscovitine) is a potent and selective CDKs Bioactivity: Senexin A is a CDK8 inhibitor with an IC50 of 280 nM. inhibitor with IC50s of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5, Cdc2, and CDK2, respectively.

Purity: 99.94% Purity: 99.93% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg, 200 mg 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

Simurosertib SNS-032 (TAK-931) Cat. No.: HY-100888 (BMS-387032) Cat. No.: HY-10008

Bioactivity: Simurosertib (TAK-931) is a selective cycle 7 (CDC7) kinase Bioactivity: SNS-032 (BMS-387032) is a selective inhibitor of CDK2,

inhibitor, with an IC50<0.3 nM. CDK7, and CDK9 with IC50s of 38 nM, 62 nM and 4 nM, respectively.

Purity: 99.07% Purity: 98.50% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

www.MedChemExpress.com 31

SU9516 SY-1365 Cat. No.: HY-18629 Cat. No.: HY-128587

Bioactivity: SU9516 is a potent CDK2 inhibitor, with an IC50 of 22 nM, and Bioactivity: SY-1365 is a highly selective covalent inhibitor of CDK7. SY-1365 possesses therapeutic potential in both hematological also shows inhibitory effects on CDK1 and CDK4, with IC50s of and solid tumors [1]. 40, 200 nM, respectively.

Purity: 99.76% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg, 100 mg 5 mg, 10 mg, 50 mg

T025 THAL-SNS-032 Cat. No.: HY-112296 Cat. No.: HY-123937

Bioactivity: T025 is an orally available and highly potent Cdc2-like kinase Bioactivity: THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting

(CLK) inhibitor with Kds of 4.8, 0.096, 6.5, and 0.61 nM of a CDK-binding SNS-032 ligand linked to a thalidomide for CLK1, CLK2, CLK3, and CLK4, respectively. derivative that binds the E3 ubiquitin ligase Cereblon (CRBN) [1].

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 100 mg, 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg

THZ1 THZ1 Hydrochloride Cat. No.: HY-80013 Cat. No.: HY-80013A

Bioactivity: THZ1 is a selective and potent covalent CDK7 inhibitor with Bioactivity: THZ1 Hydrochloride is a selective and potent CDK7 inhibitor

an IC50 of 3.2 nM. with an IC50 of 3.2 nM.

Purity: 98.82% Purity: 98.70% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

THZ1-R THZ2 Cat. No.: HY-19988 Cat. No.: HY-12280

Bioactivity: THZ1-R is a non- reactive analog of THZ1 which Bioactivity: THZ2 is a potent and selective CDK7 inhibitor with an IC50 of displays diminished activity for CDK7 inhibition. THZ1-R 13.9 nM. binds to CDK7 with a Kd of 142 nM.

Purity: 97.96% Purity: 99.03% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

THZ531 Trilaciclib Cat. No.: HY-103618 (G1T28) Cat. No.: HY-101467

Bioactivity: THZ531 is a covalent inhibitor of both CDK12 and CDK13 with Bioactivity: Trilaciclib is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM IC s of 158 nM and 69 nM, respectively. 50 for CDK4 and CDK6, respectively.

Purity: 99.86% Purity: 98.46% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg, 50 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

32 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Trilaciclib hydrochloride Voruciclib hydrochloride (G1T28 hydrochloride) Cat. No.: HY-101467A Cat. No.: HY-12422A

Bioactivity: Trilaciclib hydrochloride is a CDK4/6 inhibitor with IC50s of Bioactivity: Voruciclib hydrochloride is a clinical stage oral CDK9 1 nM and 4 nM for CDK4 and CDK6, respectively. inhibitor. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell (DLBCL) [1].

Purity: 99.24% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 500 mg, 250 mg 5 mg, 10 mg, 50 mg, 100 mg

Wogonin XL413 Cat. No.: HY-N0400 Cat. No.: HY-15260

Bioactivity: Wogonin is a naturally occurring mono-flavonoid, can inhibit Bioactivity: XL413 is a potent, selective and ATP competitive inhibitor of

the activity of CDK8 and Wnt, and exhibits Cdc7, with an IC50 of 3.4 nM, and also shows potent effect anti-inflammatory and anti-tumor effects. with IC50s of 215, 42 nM on CK2, PIM1, respectively, and an

EC50 of 118 nM on pMCM. Purity: 99.98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

XL413 hydrochloride Cat. No.: HY-15260A

Bioactivity: XL413 hydrochloride is a potent, selective and ATP competitive

inhibitor of Cdc7, with an IC50 of 3.4 nM, and also shows

potent effect with IC50s of 215, 42 nM on CK2, PIM1,

respectively, and an EC50 of 118 nM on pMCM. Purity: 99.72% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 33 Checkpoint Kinase (Chk)

Checkpoint Kinases (Chk) are protein kinases that are involved in cell cycle control. Two checkpoint kinase subtypes have been identified, Chk1 and Chk2. Chk1 is a central component of genome surveillance pathways and is a key regulator of the cell cycle and cell survival. Chk1 is required for the initiation of DNA damage checkpoints and has recently been shown to play a role in the normal (unperturbed) cell cycle. Chk1 impacts various stages of the cell cycle including the S phase, G2/M transition and M phase. In addition to mediating cell cycle checkpoints, Chk1 also contributes to DNA repair processes, gene transcription, embryo development, cellular responses to HIV infection and somatic cell viability. Chk2 is a protein kinase that is activated in response to DNA damage and is involved in cell cycle arrest. In response to DNA damage and replication blocks, cell cycle progression is halted through the control of cell cycle regulators. The protein encoded by this gene is a cell cycle checkpoint regulator and putative tumor suppressor.

34 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Checkpoint Kinase (Chk) Inhibitors & Modulators

AZD-7762 BML-277 Cat. No.: HY-10992 (Chk2 Inhibitor II) Cat. No.: HY-13946

Bioactivity: AZD-7762 is a potent ATP-competitive checkpoint kinase ( Chk) Bioactivity: BML-277 is a selective checkpoint kinase 2 ( Chk2) inhibitor

inhibitor in with an IC50 of 5 nM for Chk1. with an IC50 of 15 nM.

Purity: 99.90% Purity: 98.02% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg

CCT241533 CCT241533 hydrochloride Cat. No.: HY-14715 Cat. No.: HY-14715B

Bioactivity: CCT241533 is a potent and selective ATP competitive inhibitor Bioactivity: CCT241533 hydrochloride is a potent and selective CHK2 of CHK2 with an IC of 3 nM and K of 1.16 nM. 50 i inhibitor with an IC50 of 3 nM and a Ki of 1.16 nM.

Purity: >98% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

CCT244747 CCT245737 Cat. No.: HY-18175 Cat. No.: HY-18958

Bioactivity: CCT244747 is a potent, orally bioavailable and highly Bioactivity: CCT245737 is a orally active and seletive Chk1 inhibitor, selective CHK1 inhibitor, with an IC of 7.7 nM; CCT244747 50 with an IC50 of 1.3 nM.

also abrogates G2 checkpoint with an IC50 of 29 nM.

Purity: 99.0% Purity: 99.24% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

CHIR-124 CHK-IN-1 Cat. No.: HY-13263 Cat. No.: HY-U00345

Bioactivity: CHIR-124 is a potent and selective Chk1 inhibitor with IC50 Bioactivity: CHK-IN-1 is an inhibitor of CHK1 and CHK2, with of 0.3 nM, and also potently targets PDGFR and FLT3 with anti-proliferative activities.

IC50s of 6.6 nM and 5.8 nM.

Purity: 98.77% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 50 mg, 100 mg

CHK1 inhibitor CHK1-IN-2 Cat. No.: HY-104022 Cat. No.: HY-111369

Bioactivity: CHK1 inhibitor is an inhibitor of CHK1. Bioactivity: CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an

IC50 of 6 nM.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 250 mg, 500 mg

www.MedChemExpress.com 35

CHK1-IN-3 GDC-0575 Cat. No.: HY-128601 (ARRY-575, RG7741) Cat. No.: HY-112167

Bioactivity: CHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an Bioactivity: GDC-0575 (ARRY-575, RG7741) is a highly-selective oral [1] small-molecule Chk1 inhibitor with an IC of 1.2nM. IC50 of 0.4 nM . 50

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 100 mg, 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

GDC-0575 dihydrochloride PF 477736 (ARRY-575 dihydrochloride; RG7741 dihydrochloride) Cat. No.: HY-112167A (PF 00477736) Cat. No.: HY-10032

Bioactivity: GDC-0575 dihydrochloride is an orally bioavailable CHK1 Bioactivity: PF 477736 is a potent, selective ATP-competitive inhibitor of Chk1, with a K of 0.49 nM, 100-fold selectivity versus Chk2 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity. i

( Ki, 47 nM).

Purity: 99.83% Purity: 98.07% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

Prexasertib Prexasertib dihydrochloride (LY2606368) Cat. No.: HY-18174 (LY2606368 (dihydrochloride)) Cat. No.: HY-18174A

Bioactivity: Prexasertib (LY2606368) is a potent, selective and Bioactivity: Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a ATP-competitive checkpoint kinase 1 (Chk1) inhibitor, with an potent and selective ATP competitive inhibitor of the Chk1

IC50 and a Ki of <1 nM and 0.9 nM, respectively. protein kinase, with IC50s of <1 nM and 8 nM for CHK1 and

CHK2, respectively, and a Ki of 0.9 nM against purified CHK1. Purity: 97.91% Purity: 99.41% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Prexasertib Mesylate Hydrate Rabusertib (LY2606368 Mesylate Hydrate; LY2940930) Cat. No.: HY-18174B (LY2603618; IC-83) Cat. No.: HY-14720

Bioactivity: Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a Bioactivity: Rabusertib (LY2603618) is a potent and selective inhibitor of

potent, selective, ATP competitive CHK1 and CHK2 inhibitor, Chk1 with an IC50 of 7 nM. with a Ki of 0.9 nM for CHK1 and IC50s of <1 nM, 8 nM for CHK1 and CHK2, respectively. Prexasertib Mesylate Hydrate inhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2… Purity: >98% Purity: 99.69% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

SCH900776 (MK-8776) Cat. No.: HY-15532

Bioactivity: SCH900776 is a potent, selective and oral inhibitor of

checkpoint kinase1 ( Chk1) with an IC50 of 3 nM. It shows 50- and 500-fold selectivity over CDK2 andChk2, respectively.

Purity: 99.65% Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

36 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] CRISPR/Cas9

CRISPR/Cas9 (Clustered Regularly-Interspaced Short Palindromic Repeats/Cas9) is a bacterial immune system that has been adapted for genome editing in mammalian cells. Cas9 is a programmable nuclease that generates double-stranded breaks (DSB) in DNA dictated by binding of a ~20 recombinant “guide RNA” (gRNA) to the target site. DSB’s produced by Cas9 are most often repaired through the cell’s error-prone non-homologous end joining (NHEJ) pathway, resulting in small insertions or deletions (indels). The vast majority of indels shift the reading frame, introducing a premature stop codon or resulting in nonsense mediated decay of the mRNA-effectively “knocking out” a gene. The CRISPR/Cas9 system has substantially advanced efforts in specific gene editing and has been successfully applied to modify the episomal of human and other organisms. The CRISPR/Cas9 system utilizes a prokaryotic RNA-guided programmable nuclease that can make a double-strand DNA break (DSB) at a specific site under the guidance of a leading RNA. This DSB process depends on the co-expression of two basic components: a guide RNA (gRNA) and Cas9 nuclease. Making a specific DSB can trigger DNA repair via either error-prone non-homologous end joining (NHEJ) or homology-directed repair (HDR). In the presence of the CRISPR/Cas9 system, the NHEJ inhibitor SCR7 is proven to increase the efficiency of Cas9-mediated HDR by at least by 7-fold in mammalian cells. Genome editing via CRISPR/Cas9 has become an efficient and reliable way to make precise, targeted changes to the genome of living cells.

www.MedChemExpress.com 37 CRISPR/Cas9 Inhibitors & Modulators

Brefeldin A KU-57788 (BFA; Cyanein; Decumbin) Cat. No.: HY-16592 (NU7441) Cat. No.: HY-11006

Bioactivity: Brefeldin A is a specific inhibitor of protein trafficking which Bioactivity: KU-57788 is a potent and selective inhibitor of DNA-PK with

blocks the protein transport from the endoplasmic reticulum to an IC50 of 13 nM, with selectivity over a range of kinases the Golgi complex. including mTOR, PI 3-K, ATM and ATR.

Purity: 99.79% Purity: 99.35% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

L755507 Cat. No.: HY-19334 (Oncodazole; R17934) Cat. No.: HY-13520

Bioactivity: L755507 is a potent, selective agonist of β3-AR with an IC50 Bioactivity: Nocodazole is a rapidly-reversible inhibitor of of 35 nM. microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, activates CRISPR/Cas9. Purity: 98.0% Purity: 98.68% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg 10 mg, 50 mg, 100 mg

RS-1 SCR7 Cat. No.: HY-19793 Cat. No.: HY-12742

Bioactivity: RS-1 is a RAD51 activator, and also increases Bioactivity: SCR7 is a DNA Ligase IV inhibitor with anticancer activity and CRISPR/Cas9-mediated knock-in efficiencies. is also a CRISPR HDR enhancer which increases the efficiency of Cas9-mediated HDR [1] [2].

Purity: 99.55% Purity: 99.75% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

Zidovudine (Azidothymidine; AZT; ZDV) Cat. No.: HY-17413

Bioactivity: Zidovudine is a nucleoside reverse transcriptase inhibitor ( NRTI), widely used to treat HIV infection. Zidovudine increases CRISPR/Cas9-mediated editing frequency.

Purity: 99.96% Clinical Data: Launched Size: 10mM x 1mL in DMSO, 100 mg, 500 mg

38 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Deubiquitinase DUBs

Deubiquitinases (DUBs) are a large group of proteases that cleave ubiquitin from proteins and other molecules. Ubiquitin is attached to proteins in order to regulate the degradation of proteins via the proteasome and lysosome; coordinate thecellular localisation of proteins; activate and inactivate proteins; and modulate protein-protein interactions. DUBs can reverse these effects by cleaving the peptide or isopeptide bond between ubiquitin and its substrate protein. In humans there are nearly 100 DUB genes, which can be classified into two main classes: cysteine proteases and metalloproteases. The cysteine proteases comprise ubiquitin-specific proteases (USPs), ubiquitin C-terminal hydrolases (UCHs), Machado-Josephin domain proteases (MJDs) and ovarian tumour proteases (OTU). The metalloprotease group contains only the Jab1/Mov34/Mpr1 Pad1 N-terminal+ (MPN+) (JAMM) domain proteases. DUBs play several roles in the ubiquitin pathway. One of the best characterised functions of DUBs is the removal of monoubiqutin and polyubiquitin chainsfrom proteins.

www.MedChemExpress.com 39 Deubiquitinase Inhibitors & Modulators

6-Thioguanine b-AP15 (Thioguanine2-Amino-6-purinethiol) Cat. No.: HY-13765 (NSC 687852) Cat. No.: HY-13989

Bioactivity: 6-Thioguanine (Thioguanine) is an anti- and Bioactivity: b-AP15 is a specific inhibitor of the deubiquitinating enzymes immunosuppressant agent, acts as an inhibitor of SARS and MERS UCHL5 and Usp14. coronavirus papain-like proteases ( PLpros) and also potently

inhibits USP2 activity, with IC50s of 25 μM and 40 μM for Plpros and recombinant human USP2, respectively. Purity: 98.0% Purity: 98.93% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 500 mg

BAY 11-7082 C527 (BAY 11-7821) Cat. No.: HY-13453 Cat. No.: HY-12988

Bioactivity: BAY 11-7082 is a NF-κB inhibitor which decreases NF-κB by Bioactivity: C527 is a is a pan DUB , with a high

inhibiting TNF-α-induced phosphorylation of IκB-α. BAY 11-7082 potency for the USP1/UAF1 complex ( IC50=0.88 μM). inhibits ubiquitin-specific protease USP7 and USP21 with

IC50s of 0.19 μM and 0.96 μM, respectively.

Purity: 99.42% Purity: 98.92% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Degrasyn DUBs-IN-1 (WP1130) Cat. No.: HY-13264 Cat. No.: HY-50736

Bioactivity: Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB) Bioactivity: DUBs-IN-1 is an active inhibitor of ubiquitin-specific

inhibitor, directly inhibiting DUB activity of USP9x, USP5, proteases (USPs), with an IC50 of 0.24 μM for USP8. USP14, and UCH37. Degrasyn has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.

Purity: 99.70% Purity: 99.46% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

DUBs-IN-2 DUBs-IN-3 Cat. No.: HY-50737A Cat. No.: HY-50737

Bioactivity: DUBs-IN-2 is a potent deubiquitinase inhibitor with an IC50 of Bioactivity: DUBs-IN-3 is a potent deubiquitinase (USP) enzyme inhibitor extracted from reference compound 22c with an IC of 0.56 μM 0.28 μM for USP8. 50 for USP8.

Purity: 99.08% Purity: 99.40% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

EOAI3402143 FT671 Cat. No.: HY-111408 Cat. No.: HY-107985

Bioactivity: EOAI3402143 is a deubiquitinase ( DUB) inhibitor, which Bioactivity: FT671 is a potent, non-covalent and selective USP7 inhibitor

inhibits dose-dependently inhibits Usp9x/ Usp24 and Usp5. with an IC50 of 52 nM and binds to the USP7 catalytic domain

with a Kd of 65 nM.

Purity: 99.12% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

40 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

FT827 GNE-6640 Cat. No.: HY-111350 Cat. No.: HY-112937

Bioactivity: FT827 is a selective and covalent ubiquitin-specific protease Bioactivity: GNE-6640 is a selective and non-covalent inhibitor of

7 ( USP7) inhibitor with an IC50 of 52 nM. ubiquitin epecific peptidase 7 (USP7), with IC50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP43 and Ub-MDM2, respectively. Purity: 98.48% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

GNE-6776 HBX 19818 Cat. No.: HY-107986 Cat. No.: HY-17540

Bioactivity: GNE-6776 is a selective USP7 inhibitor. Bioactivity: HBX 19818 is a specific inhibitor of ubiquitin-specific

protease 7 (USP7), with an IC50 of 28.1 μM.

Purity: 98.03% Purity: 96.84% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

IU1 IU1-47 Cat. No.: HY-13817 Cat. No.: HY-122243

Bioactivity: IU1 is a special Usp14 inhibitor with IC50 of 4-5 μM. Bioactivity: IU1-47 is a potent USP14 inhibitor with an IC50 of 0.6 μM. IU1-47 induces tau elimination in cultured neurons [1].

Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

LDN-57444 MF-094 Cat. No.: HY-18637 Cat. No.: HY-112438

Bioactivity: LDN-57444 is a reversible, competitive and site-directed Bioactivity: MF-094 is a potent and selective USP30 inhibitor with an IC50 inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1), with of 120 nM. an IC50 of 0.88 μM and a Ki of 0.40 μM; LDN-57444 also

suppresses UCH-L3 activity, with an IC50 of 25 μM. Purity: 97.73% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

ML-323 ML364 Cat. No.: HY-17543 Cat. No.: HY-100900

Bioactivity: ML-323 is a reversible, potent USP1-UAF1 inhibitor with IC50 Bioactivity: ML364 is an inhibitor of ubiquitin specific peptidase 2 of 76 nM in a Ub-Rho assay. The measured inhibition constants (USP2), and can be used for the research of breast cancer, extracted from patent WO 2016134026 A1, compound Figure 10G. of ML-323 for the free enzyme ( Ki) is 68 nM.

Purity: 99.61% Purity: 99.81% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 41

NSC632839 P 22077 Cat. No.: HY-100708 Cat. No.: HY-13865

Bioactivity: NSC632839 is a nonselective isopeptidase inhibitor, which Bioactivity: P 22077 is a cell-permeable ubiquitin-specific protease 7 inhibits USP2, USP7, and SENP2 with EC s of 45±4 μM, 50 (USP7) inhibitor with an EC50 of 8.01 μM. It also inhibits 37±1 μM, and 9.8±1.8 μM, respectively. USP47 with an EC50 of 8.74 μM.

Purity: 98.43% Purity: 99.97% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

P005091 PR-619 (P5091) Cat. No.: HY-15667 Cat. No.: HY-13814

Bioactivity: P005091 is a selective and potent inhibitor of Bioactivity: PR-619 is a broad-range DUB inhibitor with EC50 of 3.93, ubiquitin-specific protease 7 (USP7) with an 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, EC of 4.2 μM. 50 and USP5, respectively.

Purity: 99.94% Purity: 98.81% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg

SJB2-043 SJB3-019A Cat. No.: HY-15757 Cat. No.: HY-80012

Bioactivity: SJB2-043 is an inhibitor of the native USP1/UAF1 complex with Bioactivity: SJB3-019A is a potent and novel USP1 inhibitor, 5 times more

IC50 of 544 nM. potent than SJB2-043 in promoting ID1 degradation and cytoxicity in K562 cells with IC50 of 0.0781 μM.

Purity: 97.37% Purity: 99.00% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

USP7-IN-1 USP7-IN-3 Cat. No.: HY-16709 Cat. No.: HY-112128

Bioactivity: USP7-IN-1 is a selective and reversible inhibitor of Bioactivity: USP7-IN-3 (Compound 5) is a potent and selective allosteric [1] ubiquitin-specific protease 7 (USP7), with an IC50 of 77 μM, ubiquitin-specific protease 7 ( USP7) inhibitor . and can be used for the research of cancer.

Purity: 99.77% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

USP7/USP47 inhibitor VLX1570 Cat. No.: HY-13487 Cat. No.: HY-12471

Bioactivity: USP7/USP47 inhibitor is a selective ubiquitin-specific protease Bioactivity: VLX1570 is a competitive inhibitor of proteasome

7/47 (USP7/USP47) inhibitor, with EC50s of 0.42 μM and 1.0 deubiquitinases ( DUBs) with an IC50 of approximate 10 μM. μM, respectively.

Purity: 98.17% Purity: 98.00% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

42 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] DNA Alkylator/Crosslinker

DNA alkylator/crosslinker is a molecule that alkylates DNA or can cross link with DNA. DNA alkylator/crosslinker can have mutagenic, pharmaceutical, or other effects. Alkylation is the transfer of an alkyl group from one molecule to another. The alkyl group may be transferred as an alkyl carbocation, a free radical, a carbanion or a carbene. Alkylating agents are widely used in chemistry because the alkyl group is probably the most common group encountered in organic molecules. Selective alkylation, or adding parts to the chain with the desired functional groups, is used, especially if there is no commonly available biological precursor. Alkylation with only one carbon is termed . In medicine, alkylation of DNA is used in chemotherapy to damage the DNA of cancer cells. Alkylation is accomplished with the class of drugs called alkylating antineoplastic agents. Crosslinking of DNA occurs when various exogenous or endogenous agents react with two different positions in the DNA. This can either occur in the same strand (intrastrand crosslink) or in the opposite strands of the DNA (interstrand crosslink). Crosslinks also occur between DNA and protein. DNA replication is blocked by crosslinks, which causes replication arrest and cell death if the crosslink is not repaired. The RAD51 family plays a role in repair.

www.MedChemExpress.com 43 DNA Alkylator/Crosslinker Inhibitors & Modulators

Altretamine hydrochloride (ENT-50852 hydrochloride; RB-1515 (ENT-50852; RB-1515; WR-95704) Cat. No.: HY-B0181 hydrochloride; WR-95704 hydrochloride) Cat. No.: HY-B0181A

Bioactivity: Altretamine is an alkylating antineoplastic agent. Bioactivity: Altretamine hydrochloride is an alkylating antineoplastic agent.

Purity: 99.61% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 500 mg 100 mg, 500 mg

Bendamustine D4 hydrochloride (SDX-105 D4) Cat. No.: HY-13567S (SDX-105; EP-3101) Cat. No.: HY-B0077

Bioactivity: Bendamustine D4 is the deuterium labeled Bendamustine. Bioactivity: Bendamustine hydrochloride is a DNA cross-linking agent that Bendamustine is a DNA cross-linking agent that causes DNA causes DNA breaks, with alkylating and antimetabolite breaks, with alkylating and antimetabolite properties. properties.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 25 mg, 100 mg, 200 mg, 500 mg

Busulfan Calicheamicin Cat. No.: HY-B0245 (Calicheamicin γ1) Cat. No.: HY-19609

Bioactivity: is a potent alkylator with selective immunosuppressive Bioactivity: Calicheamicin is a cytotoxic agent that causes double-strand effect on bone marrow. DNA breaks.

Purity: 98.0% Purity: 98.44% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 1 mg, 5 mg, 10 mg

Carboplatin (NSC 241240) Cat. No.: HY-17393 Cat. No.: HY-13585

Bioactivity: (NSC 241240) is a DNA synthesis inhibitor which Bioactivity: Carmustine is an antitumor chemotherapeutic agent, which works binds to DNA, inhibits replication and transcription and by akylating DNA and RNA. induces cell death. Carboplatin (NSC 241240) is a derivative of CDDP and a potent anti-cancer agent.

Purity: 99.93% Purity: 99.85% Clinical Data: Launched Clinical Data: Launched Size: 100 mg, 200 mg, 500 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

Chlorambucil (CB-1348; WR-139013) Cat. No.: HY-13593 (CDDP; cis-Diaminodichloroplatinum) Cat. No.: HY-17394

Bioactivity: is an alkylating agent with antitumor activity. Bioactivity: Cisplatin is a antineoplastic chemotherapy drug which works by cross-linking with DNA and causing DNA damage in cancer cells.

Purity: 98.79% Purity: 99.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 500 mg 100 mg, 500 mg

44 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Cyclophosphamide hydrate Cat. No.: HY-17420 (Cyclophosphamide monohydrate) Cat. No.: HY-17420A

Bioactivity: Cyclophosphamide is a synthetic alkylating agent chemically Bioactivity: Cyclophosphamide hydrate is a synthetic alkylating agent related to the nitrogen mustards with antineoplastic and chemically related to the nitrogen mustards with immunosuppressive activities. antineoplastic and immunosuppressive activities.

Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 100 mg, 200 mg, 500 mg Size: 100 mg, 200 mg, 500 mg

Fotemustine (S10036) Cat. No.: HY-B0733 Cat. No.: HY-17419

Bioactivity: is a DNA-alkylating agent, with antitumor activity. Bioactivity: Ifosfamide is an alkylating chemotherapeutic agent with activity against a wide range of tumors.

Purity: >98% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 5 mg, 10 mg, 50 mg Size: 200 mg, 500 mg

Lomustine (CCNU; NSC 79037) Cat. No.: HY-13669 (L-PAM) Cat. No.: HY-17575

Bioactivity: (CCNU) is a DNA alkylating agent, with antitumor Bioactivity: Melphalan is an effective DNA alkylating agent, with potent activity. antitumor activity.

Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 200 mg, 500 mg 50 mg, 100 mg, 500 mg

Methylnitronitrosoguanidine Miriplatin (MNNG) Cat. No.: HY-128612 (SM-11355) Cat. No.: HY-16325A

Bioactivity: Methylnitronitrosoguanidine (MNNG) is an alkylating agent with Bioactivity: Miriplatin is a chemotherapy agent which belongs to the class toxic and mutagenic effects [1]. of alkylating agents.

Purity: 98.0% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 50 mg, 100 mg

Miriplatin hydrate (SM-11355 (hydrate)) Cat. No.: HY-16325 (Ametycine) Cat. No.: HY-13316

Bioactivity: Miriplatin hydrate is a chemotherapy agent which belongs to Bioactivity: Mitomycin C is an antitumor drug and antibiotic that shows the class of alkylating agents. extraordinary ability to inhibit DNA synthesis. Mitomycin C is a DNA cross-linking agent, which induces DNA damaging.

Purity: >98% Purity: 99.45% Clinical Data: Launched Clinical Data: Launched Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

www.MedChemExpress.com 45

Oxaliplatin Palifosfamide Cat. No.: HY-17371 (Isophosphoramide mustard; IPM; ZIO-201) Cat. No.: HY-14798

Bioactivity: is a DNA synthesis inhibitor. It causes DNA Bioactivity: Palifosfamide is a novel DNA alkylator and the active crosslinking damage, prevents DNA replication and metabolite of ifosfamide, with antitumor activity. transcription and causes cell death.

Purity: 99.86% Purity: 95.0% Clinical Data: Launched Clinical Data: Phase 3 Size: 50 mg, 100 mg, 200 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

Procarbazine Hydrochloride RITA Cat. No.: HY-13733 (NSC 652287) Cat. No.: HY-13424

Bioactivity: Hydrochloride is an alkylating agent, with Bioactivity: RITA is an inhibitor of p53-HDM-2 interaction, binds to

anticancer activity. p53dN, with a Kd of 1.5 nM, and also induces DNA-DNA cross-links.

Purity: 95.0% Purity: 99.57% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 5 mg, 10 mg, 50 mg

Satraplatin SJG-136 (BMS182751; BMY45594; JM216) Cat. No.: HY-17576 (NSC-694501) Cat. No.: HY-14573

Bioactivity: is an alkylating agent, with potent antitumor Bioactivity: SJG-136 is a DNA cross-linking agent, with an XL50 of 45 nM effect. for pBR322 DNA; SJG-136 has potent antitumor activity.

Purity: 99.26% Purity: 98.0% Clinical Data: Phase 3 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg

Streptozocin (; U 9889) Cat. No.: HY-13753 (NSC 362856; CCRG 81045; TMZ) Cat. No.: HY-17364

Bioactivity: Streptozocin is a potent DNA-methylating agent, with IC50s Bioactivity: Temozolomide (NSC 362856; CCRG 81045) is an oral DNA of 11.7, 904 and 1024 μg/mL in HL60, K562 and C1498 cells alkylating agent used to treat some brain cancers. respectively.

Purity: 99.58% Purity: 99.96% Clinical Data: Launched Clinical Data: Launched Size: 100 mg, 500 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g

Thio-TEPA Cat. No.: HY-17574 (NSC 39069; Treosulphan) Cat. No.: HY-16503

Bioactivity: Thio-TEPA is a DNA alkylating agent, with antitumor activity. Bioactivity: Treosulfan (NSC 39069;Treosulphan) is an alkylating agent with activity in and other solid tumor types.

Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

46 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Uramustine VAL-083 (Uracil mustard) Cat. No.: HY-13544 (Dianhydrodulcitol; Dianhydrogalactitol) Cat. No.: HY-16513

Bioactivity: is an oral alkylating agent, effective in the Bioactivity: VAL-083 is an alkylating agent that creates N7 methylation on treatment of lymphosarcoma, chronic lymphatic leukaemia, and DNA, with antitumor activity. thrombocythemia.

Purity: 98.48% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

www.MedChemExpress.com 47 DNA-PK DNA-dependent protein kinase

DNA-PKcs (DNA-dependent protein kinase, catalytic subunit) is an enzyme that in humans is encoded by the PRKDC gene. DNA-PKcs belongs to the phosphatidylinositol 3-kinase-related kinase protein family. DNA-PKcs is the catalytic subunit of a nuclear DNA-dependent serine/threonine protein kinase called DNA-PK. The second component is the autoimmune antigen Ku. On its own, DNA-PKcs is inactive and relies on Ku to direct it to DNA ends and trigger its kinase activity. DNA-PKcs is required for the non-homologous end joining (NHEJ) pathway of DNA repair. Many proteins have been identified as substrates for the kinase activity of DNA-PK. Autophosphorylation of DNA-PKcs appears to play a key role in NHEJ and is thought to induce a conformational change that allows end processing enzymes to access the ends of the double-strand break. DNA-PK also cooperates with ATR and ATM to phosphorylate proteins involved in the DNA damage checkpoint.

48 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] DNA-PK Inhibitors & Modulators

(R)-Nedisertib AZD-7648 ((R)-M3814) Cat. No.: HY-101570A Cat. No.: HY-111783

Bioactivity: (R)-Nedisertib ((R)-M3814) is a less active R-enantiomer of Bioactivity: AZD-7648 is a potent and selective DNA-PK inhibitor. [1] Nedisertib, with an IC50 in the range of 7-30 nM for DNA-PK Anti-tumor activity . [1].

Purity: 92.39% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 500 mg, 250 mg 5 mg, 10 mg, 25 mg, 50 mg

CC-115 CC-115 hydrochloride Cat. No.: HY-16962 Cat. No.: HY-16962A

Bioactivity: CC-115 is a potent and dual DNA-PK and mTOR kinase Bioactivity: CC-115 hydrochloride is a potent and dual DNA-PK and mTOR

inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. blocks both mTORC1 and mTORC2 signaling. CC-115 blocks both mTORC1 and mTORC2 signaling.

Purity: 96.64% Purity: 97.22% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Compound 401 KU-57788 Cat. No.: HY-19341 (NU7441) Cat. No.: HY-11006

Bioactivity: Compound 401 is a synthetic inhibitor of DNA-PK ( IC50 = 0.28 Bioactivity: KU-57788 is a potent and selective inhibitor of DNA-PK with an IC of 13 nM, with selectivity over a range of kinases μM) that also targets mTOR but not PI3K in vitro. 50 including mTOR, PI 3-K, ATM and ATR.

Purity: 99.97% Purity: 99.35% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

LTURM34 LY3023414 Cat. No.: HY-101667 Cat. No.: HY-12513

Bioactivity: LTURM34 is a specific DNA-PK inhibitor with an IC50 of 0.034 Bioactivity: LY3023414 potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC s of 6.07 nM, 77.6 μM. 50 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. LY3023414 potently inhibits mTORC1/ 2 at low nanomolar… Purity: 99.24% Purity: 99.77% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Nedisertib NU 7026 (M3814) Cat. No.: HY-101570 (DNA-PK Inhibitor II; LY293646) Cat. No.: HY-15719

Bioactivity: Nedisertib (M3814) is a potent and selective inhibitor of Bioactivity: NU 7026 is a novel specific DNA-PK inhibitor with IC50 of DNA-dependent Protein Kinase ( DNA-PK), with an IC50 of <3 0.23±0.01 μM, also inhibits PI3K with IC50 of 13±3 μM. nM.

Purity: 99.43% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

www.MedChemExpress.com 49

PI-103 PI-103 Hydrochloride Cat. No.: HY-10115 Cat. No.: HY-10115A

Bioactivity: PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 Bioactivity: PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, 50 p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. DNA-PK with an IC50 of 2 nM. PI-103 also inhibits DNA-PK with an IC50 of 2 nM.

Purity: 99.86% Purity: 99.78% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

PIK-75 PIK-90 (PIK-75 Hydrochloride) Cat. No.: HY-13281 Cat. No.: HY-12030

Bioactivity: PIK-75 is a DNA-PK and PI3K inhibitor, which inhibits DNA-PK, Bioactivity: PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α,

p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. p110γ and DNA-PK with IC50s of 11, 18 and 13 nM, PIK-75 inhibits p110α >200-fold more potently than p110β respectively.

(IC 50=1.3 μM). Purity: 99.91% Purity: 99.06% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

Rac-Nedisertib SF2523 (Rac-M3814) Cat. No.: HY-101570B Cat. No.: HY-101146

Bioactivity: Rac-Nedisertib (Rac-M3814) is a racemate of Nedisertib, a Bioactivity: SF2523 is a highly selective and potent inhibitor of PI3K with [1] IC s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, potent DNA-PK inhibitor, with an IC50 of <3 nM . 50 PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.

Purity: 91.45% Purity: 99.37% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

STL127705 Torin 2 Cat. No.: HY-122727 Cat. No.: HY-13002

Bioactivity: STL127705 (Compound L) is a Ku 70/80 heterodimer protein Bioactivity: Torin 2 is an mTOR inhibitor with EC50 of 0.25 nM for inhibitor, inhibits Ku70/80-DNA interaction, with an IC of 50 inhibiting cellular mTOR activity, and exhibits 800-fold

3.5 μM. STL127705 also inhibits Ku-dependent activation of selectivity over PI3K (EC 50: 200 nM). Torin 2 also inhibits DNA-PKCS kinase ( IC , 2.5 μM) [1]. 50 DNA-PK with an IC50 of 0.5 nM in the cell free assay. Tori… Purity: >98% Purity: 99.93% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

VX-984 Wortmannin (M9831) Cat. No.: HY-19939S (SL-2052; KY-12420) Cat. No.: HY-10197

Bioactivity: VX-984 is a potent DNA-PK inhibitor. Bioactivity: Wortmannin is a multi-target inhibitor. Wortmannin inhibits PI3K [1], MLCK [1], DNA-PK [2], ATM [2], ATR [2], [3] and Polo-like kinase 3 ( Plk3 ) with IC50s of 3 nM, 200 nM, 16 nM, 150 nM, 1.8 μM and 48 nM, respectively. Purity: >98% Purity: 99.85% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg

50 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

YU238259 Cat. No.: HY-19977

Bioactivity: YU238259 is an inhibitor of homology-dependent DNA repair ( HDR), used for cancer research.

Purity: 98.01% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 51 DNA/RNA Synthesis

RNA synthesis, which is also called DNA transcription, is a highly selective process. Transcription by RNA polymerase II extends beyond RNA synthesis, towards a more active role in mRNA maturation, surveillance and export to the cytoplasm. Single-strand breaks are repaired by DNA ligase using the complementary strand of the double helix as a template, with DNA ligase creating the final to fully repair the DNA.DNA ligases discriminate against substrates containing RNA strands or mismatched base pairs at positions near the ends of the nickedDNA. (BLM) exerts its genotoxicity by generating free radicals, whichattack C-4′ in the deoxyribose backbone of DNA, leading to opening of the ring and strand breakage; it is an S-independentradiomimetic agent that causes double-strand breaks in DNA. First strand cDNA is synthesized using random hexamer primers and M-MuLV Reverse Transcriptase (RNase H). Second strand cDNA synthesis is subsequently performed using DNA Polymerase I and RNase H. The remaining overhangs are converted into blunt ends using exonuclease/polymerase activity. After adenylation of the 3′ ends of DNA fragments, NEBNext Adaptor with hairpin loop structure is ligated to prepare the samples for hybridization. Cell cycle and DNA replication are the top two pathways regulated by BET bromodomain inhibition. Cycloheximide blocks the translation of mRNA to protein.

52 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] DNA/RNA Synthesis Inhibitors & Modulators

2-(Methylamino)-1H-purin-6(7H)-one 3,7,4'-Trihydroxyflavone (N2-methylguanine) Cat. No.: HY-101412 (5-Deoxykampferol) Cat. No.: HY-111806

Bioactivity: 2-(Methylamino)-1H-purin-6(7H)-one (N2-Methylguanine) is a Bioactivity: 3,7,4'-Trihydroxyflavone, isolated from Rhus javanica var. modified nucleoside. 2-(Methylamino)-1H-purin-6(7H)-one is an roxburghiana, is a flavonoid with DNA strand-scission activity endogenous methylated nucleoside found in human fluids. [1].

Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 5 mg

5-Methoxyflavone 6-Thio-2'-Deoxyguanosine Cat. No.: HY-107790 (6-thio-dG; β-TGdR) Cat. No.: HY-18762

Bioactivity: 5-Methoxyflavone, belonged to Flavonoid family, is a DNA Bioactivity: 6-Thio-2'-Deoxyguanosine is a nucleoside analogue that can be polymerase-beta inhibitor and neuroprotective agent against incorporated into de novo-synthesized telomeres by telomerase. beta-amyloid toxicity. possess central nervous system (CNS)

depressant effect mediated through the ionotropic GABA A receptors. Purity: 99.98% Purity: 97.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 25 mg 5 mg, 10 mg, 25 mg, 50 mg

Acelarin Actinomycin D (NUC-1031) Cat. No.: HY-100885 (; Actinomycin IV) Cat. No.: HY-17559

Bioactivity: Acelarin (NUC-1031) is a ProTide transformation and Bioactivity: Actinomycin D inhibits DNA repair with an IC50 of 0.42 μM. enhancement of the widely-used nucleoside analogue, .

Purity: 99.68% Purity: 99.89% Clinical Data: Phase 2 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Adenine alpha-Amanitin (6-Aminopurine; Vitamin B4) Cat. No.: HY-B0152 (α-Amanitin; α-Amatoxin) Cat. No.: HY-19610

Bioactivity: is a purine derivative and a with a variety Bioactivity: alpha-Amanitin is the principal toxin of several deadly of roles in biochemistry. Target: Nucleoside poisonous mushrooms, exerting its toxic function by inhibiting antimetabolite/analog Adenine is a nucleobase with a variety RNA-polymerase II. of roles in biochemistry including cellular respiration, in the form of both the energy-rich triphosphate (ATP)… Purity: 98.76% Purity: 99.79% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 2 mg, 5 mg 1 g, 5 g

Anisomycin Beaucage reagent (Flagecidin; Wuningmeisu C) Cat. No.: HY-18982 Cat. No.: HY-100951

Bioactivity: Anisomycin is a potent protein synthesis inhibitor which Bioactivity: Beaucage reagent is found to be potent in causing DNA interferes with protein and DNA synthesis by inhibiting cleavage. peptidyl transferase or the 80S ribosome system. Anisomycin is a JNK activator, which increases phospho-JNK.

Purity: 98.20% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 250 mg, 1 g

www.MedChemExpress.com 53

Bleomycin sulfate BMH-21 Cat. No.: HY-17565 Cat. No.: HY-12484

Bioactivity: Bleomycin sulfate is a DNA synthesis inhibitor with potent Bioactivity: BMH-21 is a small molecule DNA intercalator that binds antitumor activity. ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription; does not cause phosphorylation of H2AX.

Purity: 98.0% Purity: 98.96% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10 mg, 50 mg, 100 mg 10 mg, 50 mg

Branaplam (LMI070; NVS-SM1) Cat. No.: HY-19620 Cat. No.: HY-B0016

Bioactivity: Branaplam (LMI070) is a highly potent, selective and orally Bioactivity: Capecitabine is an oral prodrug that is converted to its active small molecule SMN2 splicing modulator. active metabolite, 5-FU, by thymidine phosphorylase.

Purity: 99.67% Purity: 99.97% Clinical Data: Phase 2 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 g, 5 g

Carboplatin CeMMEC1 (NSC 241240) Cat. No.: HY-17393 Cat. No.: HY-111445

Bioactivity: Carboplatin (NSC 241240) is a DNA synthesis inhibitor which Bioactivity: CeMMEC1 is an inhibitor of BRD4, and also has high affinity

binds to DNA, inhibits replication and transcription and for TAF1, with an IC50 of 0.9 μM for TAF1, and a Kd of 1.8 induces cell death. Carboplatin (NSC 241240) is a derivative μM for TAF1 (2). of CDDP and a potent anti-cancer agent.

Purity: 99.93% Purity: 98.03% Clinical Data: Launched Clinical Data: No Development Reported Size: 100 mg, 200 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

CeMMEC13 Chebulinic acid Cat. No.: HY-101088 Cat. No.: HY-N2033

Bioactivity: CeMMEC13 is a potent inhibitor of TAF1 (2) bromodomain, with Bioactivity: Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 an IC50 of 2.1 μM. phosphorylation, inhibit H+ K+-ATPase activity.

Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

COH29 CX-5461 (RNR Inhibitor COH29) Cat. No.: HY-19931 Cat. No.: HY-13323

Bioactivity: COH29 is a potent ribonucleotide reductase ( RNR) inhibitor Bioactivity: CX-5461 is a potent and oral rRNA synthesis inhibitor. It with anticancer activity. COH29 inhibits α and β subunit of inhibits RNA polymerase I-driven transcription of rRNA with

RNR with IC50s of 16 μM. IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively.

Purity: 98.04% Purity: 98.47% Clinical Data: Phase 1 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

54 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

CX-5461 dihydrochloride Cycloheximide Cat. No.: HY-13323A (Naramycin A; Actidione; CHX) Cat. No.: HY-12320

Bioactivity: CX-5461 dihydrochloride is a potent and orally bioavailable Bioactivity: Cycloheximide (Naramycin A) is an protein synthesis inhibitor of Pol I-mediated rRNA synthesis, with IC s of 142 50 inhibitor, with IC50s of 532.5 nM and 2880 nM for protein nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, synthesis and RNA synthesis in vivo, respectively.

and shows little or no effect on Pol II ( IC50 ≥25 μM). Purity: 98.24% Purity: 99.45% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 200 mg, 500 mg

Cytarabine ( β-D-arabinofuranoside; Cytosine hydrochloride (Cytosine β-D-arabinofuranoside Arabinoside; Ara-C) Cat. No.: HY-13605 hydrochloride; Cytosine Arabinoside hydrochloride; …) Cat. No.: HY-13605A

Bioactivity: Cytarabine, a nucleoside analog, causes S phase cell cycle Bioactivity: Cytarabine hydrochloride, a nucleoside analog, causes S phase arrest and inhibits DNA polymerase. Cytarabine inhibits cell cycle arrest and inhibits DNA polymerase. Cytarabine

DNA synthesis with an IC50 of 16 nM. inhibits DNA synthesis with an IC50 of 16 nM.

Purity: 99.99% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 500 mg 100 mg, 500 mg, 1 g

Datelliptium chloride Cat. No.: HY-U00337 (RP 13057; Daunomycin; Rubidomycin) Cat. No.: HY-13062A

Bioactivity: Datelliptium chloride is a DNA-intercalating agent derived Bioactivity: Daunorubicin (RP 13057, Daunomycin, Rubidomycin) is a from ellipticine, with anti-tumor activities. topoisomerase II inhibitor with potent antineoplastic activities. Daunorubicin inhibites DNA and RNA synthesis in sensitive and resistant Ehrlich ascites tumor cells.

Purity: 99.63% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10 mg, 50 mg 1 mg, 5 mg, 10 mg, 20 mg

Daunorubicin Hydrochloride (RP 13057 (Hydrochloride); Deoxycytidine triphosphate Daunomycin (Hydrochloride); Rubidomycin (Hydrochloride)) Cat. No.: HY-13062 (dCTP) Cat. No.: HY-101400

Bioactivity: Daunorubicin Hydrochloride is a topoisomerase II inhibitor Bioactivity: Deoxycytidine triphosphate (dCTP), a nucleoside triphosphate, with potent antineoplastic activities. Daunorubicin is a raw material in DNA synthesis. Deoxycytidine triphosphate Hydrochloride inhibites DNA and RNA synthesis in sensitive and has many applications, such as real-time PCR, cDNA synthesis, resistant Ehrlich ascites tumor cells. and DNA sequencing.

Purity: 99.27% Purity: 98.15% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in Water, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg 10 mg, 50 mg

Didox (NSC-324360) Cat. No.: HY-19387 (F-ara-A; NSC 118218) Cat. No.: HY-B0069

Bioactivity: Didox (NSC-324360) is a synthetic ribonucleotide reductase ( Bioactivity: Fludarabine (NSC 118218) is a DNA synthesis inhibitor, which RR) inhibitor. also inhibits phosphorylation of STAT1.

Purity: 98.72% Purity: 99.28% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

www.MedChemExpress.com 55

Folic acid GC7 Sulfate (Vitamin B9; Vitamin M) Cat. No.: HY-16637 Cat. No.: HY-108314A

Bioactivity: Folic acid(Vitamin M; Vitamin B9) is a B vitamin; is necessary Bioactivity: GC7 Sulfate is a deoxyhypusine synthase ( DHPS) inhibitor. for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.

Purity: 99.56% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 g, 10 g 1 mg, 5 mg

Gemcitabine Gemcitabine Hydrochloride (NSC 613327; LY188011) Cat. No.: HY-17026 (LY 188011 hydrochloride) Cat. No.: HY-B0003

Bioactivity: Gemcitabine (NSC 613327;LY188011) is a DNA synthesis inhibitor Bioactivity: Gemcitabine hydrochloride is a DNA synthesis inhibitor with

which inhibits the growth of BxPC-3, Mia Paca-2, PANC-1, PL-45 IC50s of 37.6, 42.9, 92.7, 89.3 and 131.4 nM in BxPC-3, Mia and AsPC-1 cells with IC s of 37.6, 42.9, 92.7, 89.3 and 50 Paca-2, PANC-1, PL-45 and AsPC-1 cells, respectively. 131.4 nM, respectively.

Purity: 99.92% Purity: 99.93% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 100 mg, 200 mg, 500 mg, 1 g 100 mg, 200 mg, 500 mg, 1 g

GNE-371 Guanine Cat. No.: HY-112803 Cat. No.: HY-Y1055

Bioactivity: GNE-371 is a potent and selective chemical probe for the Bioactivity: Guanine is one of the fundamental components of nucleic acids second bromodomains of human transcription-initiation-factor ( DNA and RNA). Guanine is a purine derivative, consisting TFIID subunit 1 and transcription-initiation-factor TFIID of a fused - ring system with conjugated

subunit 1-like, with an IC50 of 10 nM for TAF1(2). double bonds.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg Size: 5 g

Halofuginone Halofuginone hydrobromide (RU-19110) Cat. No.: HY-N1584 (RU-19110 (hydrobromide)) Cat. No.: HY-N1584A

Bioactivity: Halofuginone (RU-19110) is a less-toxic form of Febrifugine, Bioactivity: Halofuginone hydrobromide (RU-19110 hydrobromide) is a which is isolated from the plant Dichroa febrifuga [1]. less-toxic form of Febrifugine, which is isolated from the Halofuginone inhibits prolyl-tRNA synthetase in an plant Dichroa febrifuga [1]. Halofuginone inhibits prolyl-tRNA [2] synthetase in an ATP-dependent manner with a K of 18.3… ATP-dependent manner with a Ki of 18.3 nM . Halofugin… i Purity: 98.32% Purity: 99.94% Clinical Data: Phase 2 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg

Hydroxyurea L189 () Cat. No.: HY-B0313 Cat. No.: HY-15588

Bioactivity: Hydroxyurea is a cell apoptosis inducer that inhibit DNA Bioactivity: L189 is a novel human DNA ligase inhibitor, inhibits synthesis through inhibition of ribonucleotide reductase. hLigI/III/IV with IC50 of 5/9/5 μM.

Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 10 mg, 50 mg

56 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

L67 Madrasin (DNA Ligase Inhibitor) Cat. No.: HY-15586 (DDD00107587) Cat. No.: HY-100236

Bioactivity: L67 is a novel, competitive human DNA ligase inhibitor, Bioactivity: Madrasin is a potent and cell penetrant splicing inhibitor inhibits DNA ligases I and III with IC50 of 10 μM and 10 μM. that interferes with the early stages of spliceosome assembly. Madrasin is cytotoxic at higher concentrations, although at lower concentrations it induces cell cycle arrest, promotes a specific reorganization of subnuclear protein localization,… Purity: 98.0% Purity: 99.88% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

MB-7133 Mitomycin C Cat. No.: HY-16311 (Ametycine) Cat. No.: HY-13316

Bioactivity: MB-7133 is a DNA synthesis inhibitor. Bioactivity: Mitomycin C is an antitumor drug and antibiotic that shows extraordinary ability to inhibit DNA synthesis. Mitomycin C is a DNA cross-linking agent, which induces DNA damaging.

Purity: >98% Purity: 99.45% Clinical Data: No Development Reported Clinical Data: Launched Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

ML216 (CID-49852229) Cat. No.: HY-12342 (NSC 375101D) Cat. No.: HY-13700

Bioactivity: ML216(CID-49852229) is a potent inhibitor of the DNA unwinding Bioactivity: Nedaplatin (NSC 375101D) is a derivative of cisplatin and DNA activity of BLM ; showing similar IC50s of 3.0 and damage agent. 0.97 μM for full length BLM and BLM636–1298 respectively. IC50 value: 3.0/0.97 uM(Full length/636–1298 BLM) Target: BLM helicase inhibitor ML216 shows cell-based activity, and can… Purity: 99.77% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 5 mg, 10 mg, 25 mg, 50 mg Size: 10mM x 1mL in Water, 10 mg, 50 mg

NITD008 Oxolinic acid (7-Deaza-2'-C-acetylene-adenosine) Cat. No.: HY-12957 Cat. No.: HY-B1002

Bioactivity: NITD008 is a potent and selective flaviviruse inhibitor which Bioactivity: Oxolinic acid is a potent inhibitor of DNA gyrase and DNA synthesis, lead to DNA cleavage when extracted chromosomes are can inhibit Dengue Virus Type 2 (DENV-2) with an EC50 of 0.64 μM. incubated with sodium dodecyl sulfate.

Purity: 98.0% Purity: 98.39% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 g 1 mg, 5 mg, 10 mg

Phen-DC3 Cat. No.: HY-15594 (Mithramycin A) Cat. No.: HY-A0122

Bioactivity: Phen-DC3 is a G-quadruplex (G4) specific ligand which can Bioactivity: Plicamycin is a selective specificity protein 1 ( Sp1)

inhibit FANCJ and DinG with IC50s of 65±6 and 50±10 inhibitor. Plicamycin inhibits the growth of various cancers nM, respectively. by decreasing Sp1 protein.

Purity: >98% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg Size: 1 mg, 5 mg

www.MedChemExpress.com 57

Quarfloxin RG7800 (CX 3543) Cat. No.: HY-14776 (RO6885247) Cat. No.: HY-101792

Bioactivity: Quarfloxin (CX 3543), a fluoroquinolone derivative with Bioactivity: RG7800 a small molecule SMN2 splicing modifier to enter antineoplastic activity, targets and inhibits RNA pol I human clinical trials to treat spinal muscular atrophy.

activity, with IC 50 values in the nanomolar range in neuroblastoma cells. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure… Purity: >98% Purity: 99.86% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

RG7800 hydrochloride Risdiplam (RO6885247 hydrochloride) Cat. No.: HY-101792A (RG7916; RO7034067) Cat. No.: HY-109101

Bioactivity: RG7800 hydrochloride is an orally active SMN2 splicing Bioactivity: Risdiplam (RG7916; RO7034067) is an orally administered,

modulator, with EC1.5xs of 23 nM and 87 nM for SMN2 centrally and peripherally distributed SMN2 pre-mRNA splicing and SMN protein; RG7800 hydrochloride has the splicing modifier that increases survival motor neuron (SMN) potential to treat spinal muscular atrophy. protein levels.

Purity: 99.70% Purity: 99.31% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 50 mg, 100 mg

Saccharin 1-methylimidazole SCR7 Cat. No.: HY-112060 Cat. No.: HY-12742

Bioactivity: Saccharin 1-methylimidazole is an activator for DNA/RNA Bioactivity: SCR7 is a DNA Ligase IV inhibitor with anticancer activity and Synthesis. is also a CRISPR HDR enhancer which increases the efficiency of Cas9-mediated HDR [1] [2].

Purity: 98.66% Purity: 99.75% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

SMN-C3 Streptozocin Cat. No.: HY-112633 (Streptozotocin; U 9889) Cat. No.: HY-13753

Bioactivity: SMN-C3 is an orally active SMN2 splicing modulator and has Bioactivity: Streptozocin is a potent DNA-methylating agent, with IC50s the potential to treat spinal muscular atrophy (SMA). of 11.7, 904 and 1024 μg/mL in HL60, K562 and C1498 cells respectively.

Purity: 99.66% Purity: 99.58% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

TH287 TH287 hydrochloride Cat. No.: HY-16965 Cat. No.: HY-16965A

Bioactivity: TH287 is a potent inhibitor of MTH1 (NUDT1) with an IC50 value Bioactivity: TH287 hydrochloride is a potent inhibitor of MTH1 (NUDT1) with of 0.8 nM, less potent for MTH2, NUDT5, NUDT12, NUDT14, and an IC50 value of 0.8 nM, less potent for MTH2, NUDT5, NUDT12, NUDT16. NUDT14, and NUDT16.

Purity: 97.62% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

58 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

TH588 TH588 hydrochloride Cat. No.: HY-12814 Cat. No.: HY-12814A

Bioactivity: TH588 is first-in-class nudix hydrolase family inhibitor that Bioactivity: TH588 hydrochloride is first-in-class nudix hydrolase family potently and selectively engage and inhibit the MTH1 ( inhibitor that potently and selectively engage and inhibit the

IC50= 5 nM). MTH1 ( IC50= 5 nM).

Purity: 99.06% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 25 mg, 50 mg, 100 mg 5 mg, 25 mg, 50 mg, 100 mg

Thiarabine Triapine (OSI-7836) Cat. No.: HY-16496 (3-AP; PAN-811; OCX191; NSC663249) Cat. No.: HY-10082

Bioactivity: Thiarabine (OSI-7836) shows potent anti-tumor activity and Bioactivity: Triapine is a novel inhibitor of the M2 subunit of inhibition of DNA synthesis. ribonucleotide reductase ( RR), and is a potent radiosensitizer.

Purity: >98% Purity: 98.32% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg

Triciribine YK-4-279 (API-2; NSC 154020; TCN) Cat. No.: HY-15457 Cat. No.: HY-14507

Bioactivity: Triciribine is a DNA synthesis inhibitor, also inhibits Akt Bioactivity: YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding to the oncogenic transciption factor EWS-FLI1. YK-4-279 inhibits and HIV-1/2 with IC50 of 130 nM, and 0.02-0.46 μM, respectively. Ewing's sarcoma family tumor (ESFT) cell growth; YK-4-279 induces apoptosis.

Purity: 99.20% Purity: 99.61% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

Zoliflodacin (ETX0914; AZD0914) Cat. No.: HY-17647

Bioactivity: Zoliflodacin (ETX0914;AZD0914) is a novel spiropyrimidinetrione bacterial DNA gyrase/. Zoliflodacin has potent in vitro antibacterial activity against Gram-positive and Gram-negative organisms,

including S. aureus with the MIC90 of 0.25 μg/mL. Purity: 98.0% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 59 Eukaryotic Initiation Factor (eIF)

Eukaryotic initiation factors (eIFs) are proteins involved in the initiation phase of eukaryotic translation. These proteins help stabilize the formation of the functional ribosome around the start codon and also provide regulatory mechanisms in translation initiation. Eukaryotic initiation factor 2B (eIF2B) is a guanine nucleotide-exchange factor which mediates the exchange of GDP (bound to initiation factor eIF2) for GTP, thus regenerating the active [eIF2.GTP] complex that is required for peptide-chain initiation. The activity of eIF2B is a key control point for eukaryotic protein synthesis and is altered in response to viral infection, hormones, nutrients, growth factors and certain stresses. Eukaryotic translation initiation factor 4E (eIF4E) is best known for its function in the initiation of protein synthesis on capped mRNAs in the cytoplasm. Eukaryotic initiation factor (elF) 4A functions as a subunit of the initiation factor complex elF4F, which mediates the binding of mRNA to the ribosome.

60 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Eukaryotic Initiation Factor (eIF) Inhibitors & Modulators

4E1RCat 4E2RCat Cat. No.: HY-14427 Cat. No.: HY-100733

Bioactivity: 4E1RCat is an inhibitor of cap-dependent translation, and Bioactivity: 4E2RCat is an inhibitor of eIF4E-eIF4G interaction with an IC50 inhibits eIF4E:eIF4GI interaction, with an IC an of 4 μM. 50 of 13.5 μM.

Purity: 98.0% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

4EGI-1 Briciclib Cat. No.: HY-19831 (ON 014185) Cat. No.: HY-16366

Bioactivity: 4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a Kd Bioactivity: Briciclib is a water soluble derivative of ON 013100, and has of 25 μM against eIF4E binding. the potential in targeting eIF4E for solid cancers.

Purity: 98.0% Purity: 99.58% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

CCT020312 eIF4A3-IN-2 Cat. No.: HY-119240 Cat. No.: HY-101785

Bioactivity: CCT020312 is capable of delivering potent, and eukaryotic Bioactivity: eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic initiation factor 2-alpha kinase 3 (EIF2AK3) selective, initiation factor 4A-3 (eIF4A3) inhibitor with an IC50 of 110 proliferation control and also is an activator of RNA-like nM. endoplasmic reticulum kinase (PERK).

Purity: 98.56% Purity: 99.52% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Episilvestrol GCN2iB Cat. No.: HY-15359 Cat. No.: HY-112654

Bioactivity: Episilvestrol is a derivative of silvestrol, isolated from the Bioactivity: GCN2iB is an ATP-competitive inhibitor of a fruits and twigs of Aglaia silvestris, and is a specific serine/threonine-protein kinase general control

eIF4A-targeting translation inhibitor, with antitumor activity. nonderepressible 2 (GCN2), with an IC50 of 2.4 nM.

Purity: 99.85% Purity: 99.81% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

SBI-0640756 Silvestrol (SBI-756) Cat. No.: HY-19560 ((-)-Silvestrol) Cat. No.: HY-13251

Bioactivity: SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1 Bioactivity: Silvestrol is a eukaryotic translation initiation factor 4A ( and disrupts the eIF4F complex. eIF4A) inhibitor isolated from the fruits and twigs of Aglaia foveolata.

Purity: 98.52% Purity: 98.00% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg 1 mg, 2 mg

www.MedChemExpress.com 61 G-quadruplex

G-quadruplexes (G-tetrads or G4-DNA) are sequences that are rich in guanine and are capable of forming a four-stranded structure. Four guanine bases can associate through Hoogsteen hydrogen bonding to form a square planar structure called a guanine tetrad, and two or more guanine tetrads can stack on top of each other to form a G-quadruplex. The quadruplex structure is further stabilized by the presence of a cation, especially potassium, which sits in a central channel between each pair of tetrads.They can be formed of DNA, RNA, LNA, and PNA, and may be intramolecular, bimolecular or tetramolecular. Depending on the direction of the strands or parts of a strand that form the tetrads, structures may be described as parallel or antiparallel.

62 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] G-quadruplex Inhibitors & Modulators

360A 360A iodide Cat. No.: HY-15595 (360 A iodide) Cat. No.: HY-15595A

Bioactivity: 360A is a selective stabilizer of G-quadruplex, and also Bioactivity: 360A iodide is a selective stabilizer of G-quadruplex, and also

inhibits telomerase activity with an IC50 of 300 nM for inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay. telomerase in TRAP-G4 assay.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

APTO-253 Phen-DC3 Trifluoromethanesulfonate (LOR-253; LT-253) Cat. No.: HY-16291 (Phen-DC3 Triflate) Cat. No.: HY-15594A

Bioactivity: APTO-253 is an inducer of Kruppel-like factor 4 (KLF4), and Bioactivity: Phen-DC3 Trifluoromethanesulfonate is a G-quadruplex (G4) also stabilizes Gquadruplex, with anti-proliferative activity. specific ligand which can inhibit FANCJ and DinG helicases

with IC50s of 65±6 and 50±10 nM, respectively.

Purity: 96.80% Purity: 98.66% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 50 mg

Pyridostatin Pyridostatin hydrochloride (RR82) Cat. No.: HY-15176 (RR-82 hydrochloride) Cat. No.: HY-15176A

Bioactivity: Pyridostatin is a G-quadruplexe stabilizer, with a Kd of 490 Bioactivity: Pyridostatin hydrochloride is a G-quadruplexe stabilizer, with a K of 490 nM. nM. d

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg, 100 mg

TMPyP4 tosylate (TMP 1363) Cat. No.: HY-108477

Bioactivity: TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand, which inhibits the interaction between G-quadruplexes and IGF-1 [1]. TMPyP4 tosylate (TMP 1363) is a telomerase inhibitor with antitumor effects in osteosarcoma cell li…

Purity: 98.0% Clinical Data: No Development Reported Size: 100 mg

www.MedChemExpress.com 63 Haspin Kinase

Haspin is a protein kinase that regulates and spindle function during mitosis and . Haspin expression is detected in fetal liver, skin, kidney, small intestine and in all proliferating cells. Haspin phosphorylates H3 thr3 (H3T3ph) in human cell lines and depletion of Haspin by RNA interference reveals that Haspin is required for H3 thr3 phosphorylation in mitotic cells. Phosphorylation of H3T3ph by Haspin is necessary for chromosomal passenger complex (CPC) accumulation at centromeres. H3T3ph then positions the CPC at centromeres to regulate selected targets of Aurora B during mitosis.

64 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Haspin Kinase Inhibitors & Modulators

CHR-6494 LDN-192960 Cat. No.: HY-15217 Cat. No.: HY-13455

Bioactivity: CHR-6494 is a potent inhibitor of haspin, inhibiting histone Bioactivity: LDN-192960 is a potent Haspin ( Haploid Germ Cell-Specific

H3T3 phosphorylation, with an IC50 of 2 nM. Nuclear Protein Kinase) inhibitor with an IC50 of 0.010 µM.

Purity: 98.12% Purity: 99.56% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 65 HDAC Histone deacetylases

HDAC (Histone deacetylases) are a class of enzymes that remove acetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid on ahistone, allowing the histones to wrap the DNA more tightly. This is important because DNA is wrapped around histones, and DNA expression is regulated by acetylation and de-acetylation. Its action is opposite to that of histone acetyltransferase. HDAC proteins are now also called lysine deacetylases (KDAC), to describe their function rather than their target, which also includes non-histone proteins. Together with the acetylpolyamine amidohydrolases and the acetoin utilization proteins, the histone deacetylases form an ancient protein superfamily known as the histone deacetylase superfamily.

66 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] HDAC Inhibitors & Modulators

Abexinostat ACY-1083 (CRA 024781; PCI-24781) Cat. No.: HY-10990 Cat. No.: HY-111791

Bioactivity: Abexinostat (CRA 024781) is a novel pan- HDAC inhibitor Bioactivity: ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor

mostly targeting HDAC1 with Ki of 7 nM. with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy [1]. Purity: 98.61% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

ACY-738 ACY-775 Cat. No.: HY-19327 Cat. No.: HY-19328

Bioactivity: ACY-738 is a potent, selective and orally-bioavailable HDAC6 Bioactivity: ACY-775 is a potent and selective inhibitor of the of histone deacetylase 6 ( HDAC6) with an IC of 7.5nM. inhibitor, with an IC50 of 1.7 nM; ACY-738 also inhibits 50

HDAC1, HDAC2, and HDAC3, with IC50s of 94, 128, and 218 nM.

Purity: 99.94% Purity: 99.54% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

ACY-957 AES-135 Cat. No.: HY-104008 Cat. No.: HY-114483

Bioactivity: ACY-957 is a selective inhibitor of HDAC1 and HDAC2, with Bioactivity: AES-135 is a potent HDAC inhibitor, inhibits HDAC3, HDAC6,

IC50s of 7 nM, 18 nM, and 1300 nM against HDAC1/2/3, HDAC11 with IC50s of 654, 190, and 636 nM, respectively. respectively, and shows no inhibition on HDAC4/5/6/7/8/9. Anti-tumor activity [1].

Purity: 98.96% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 100 mg, 500 mg, 250 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Belinostat Benzenebutyric acid (PXD101; PX105684) Cat. No.: HY-10225 (4-Phenylbutyric acid) Cat. No.: HY-A0281

Bioactivity: is a potent HDAC inhibitor with an IC50 of 27 nM Bioactivity: Benzenebutyric acid is an inhibitor of HDAC and endoplasmic in HeLa cell extracts. reticulum (ER) stress, used in cancer and infection research.

Purity: 99.97% Purity: 99.98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg, 200 mg 5 g

BG45 BML-210 Cat. No.: HY-18712 Cat. No.: HY-19350

Bioactivity: BG45 is an HDAC class I inhibitor with selectivity for HDAC3 Bioactivity: BML-210 is a novel HDAC inhibitor, and its mechanism of action (IC50 = 289 nM). It inhibits HDAC1, HDAC2, and HDAC6 with has not been characterized. IC50 value: 5 μM[1] Target: HDAC4 greatly reduced potency (IC50s = 2, 2.2, and >20 μM, In vitro: Cell cycle analysis indicated that HeLa cell respectively). IC50 value: 289 nM (HDAC3), 2 μM (HDAC1), 2.2 treatment with 20 and 30 μM concentration of BML-210 increased μM (HDAC2), >20 μM (HDAC6) Target: HDAC At concentrations… the proportion of cells in G0/G1 phase, and caused… Purity: 99.71 % Purity: 96.00% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

www.MedChemExpress.com 67

BRD 4354 BRD 4354 ditrifluoroacetate Cat. No.: HY-112719 Cat. No.: HY-112719B

Bioactivity: BRD 4354 is a moderately potent inhibitor of HDAC5 and Bioactivity: BRD 4354 (ditrifluoroacetate) is a moderately potent inhibitor of HDAC5 and HDAC9, with IC s of 0.85 and 1.88 μM, HDAC9, with IC50s of 0.85 and 1.88 μM, respectively. 50 respectively [1].

Purity: >98% Purity: 98.06% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

BRD73954 Bufexamac Cat. No.: HY-18700 (Bufexamic acid) Cat. No.: HY-B0494

Bioactivity: BRD73954 ia a potent and selective HDAC inhibitor with IC50 of Bioactivity: Bufexamac is a class IIB histone deacetylases (HDAC6 and 36 nM and 120 nM for HDAC6 and HDAC8, respectively. HDAC10) inhibitor used as an anti-inflammatory agent.

Purity: 98.0% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg 100 mg, 500 mg

CAY10603 CHDI-390576 (BML-281) Cat. No.: HY-18613 Cat. No.: HY-119939

Bioactivity: CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor, Bioactivity: CHDI-390576, a potent, cell permeable and CNS penetrant class

with an IC50 of 2 pM; CAY10603 (BML-281) also inhibits HDAC1, IIa histonedeacetylase (HDAC) inhibitor with IC50s of 54 nM,

HDAC2, HDAC3, HDAC8, HDAC10, with IC50s of 271, 252, 0.42, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, 6851, 90.7 nM. respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the… Purity: 98.08% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 500 mg, 100 mg, 250 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Citarinostat CM-675 (ACY241) Cat. No.: HY-15994 Cat. No.: HY-114303

Bioactivity: Citarinostat is a HDAC6 specific inhibitor, with IC50 of 4 nM Bioactivity: CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone and 76 nM for HDAC6 and HDAC3, respectively. IC50 value: 4 nM deacetylases-selective inhibitor, with IC50 values of 114 nM (HDAC6), 76 nM (HDAC3) Target: HDAC The detailed information and 673 nM for PDE5 and HDAC1, respectively. CM-675 has please refer to WO2015061684A1 and 2015054197A1. potential to treat Alzheimer’s disease [1]. Purity: 99.06% Purity: >98% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 100 mg, 250 mg, 500 mg 5 mg, 10 mg, 50 mg

Corin CRA-026440 Cat. No.: HY-111048 Cat. No.: HY-19754

Bioactivity: Corin is a dual inhibitor of histone lysine specific Bioactivity: CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The Ki demethylase (LSD1) and histone deacetylase (HDAC), with a values against recombinant HDAC isoenzymes HDAC1, HDAC2, K (inact) of 110 nM for LSD1 and an IC of 147 nM for i 50 HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and HDAC1. 20 nM respectively.

Purity: 98.75% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 50 mg, 100 mg

68 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

CUDC-101 Dacinostat Cat. No.: HY-10223 (NVP-LAQ824; LAQ824) Cat. No.: HY-13606

Bioactivity: CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with Bioactivity: Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; IC50s of 4.4, 2.4, and 15.7 nM, respectively. Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.

Purity: 99.59% Purity: 98.0% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg

Domatinostat Domatinostat tosylate (4SC-202 (free base)) Cat. No.: HY-16012A (4SC-202) Cat. No.: HY-16012

Bioactivity: Domatinostat (4SC-202 free base) is a selective class I HDAC Bioactivity: Domatinostat tosylate (4SC-202) is a selective class I HDAC

inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 inhibitory activity against Lysine specific demethylase 1 (LSD1). (LSD1). Purity: 98.99% Purity: 98.81% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Droxinostat EDO-S101 (NS 41080) Cat. No.: HY-13267 (Tinostamustine) Cat. No.: HY-101780

Bioactivity: Droxinostat(NS41080) is a selective inhibitor of HDAC3, HDAC6, Bioactivity: EDO-S101 is a pan HDAC inhibitor; inhibits HDAC1, HDAC2 and and HDAC8 with IC50 of 16.9, 2.47 and 1.46 μM, respectively; HDAC3 with IC50 values of 9, 9 and 25 nM, respectively. > 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10. IC50 Value: 16.9 μM(HDAC3); 2.47 μM(HDAC6); 1.46 μM(HDAC8) Target: HDAC3/6/8 in vitro:… Purity: 98.86% Purity: 98.09% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Entinostat Fimepinostat (MS-275; SNDX-275) Cat. No.: HY-12163 (CUDC-907) Cat. No.: HY-13522

Bioactivity: is an oral and selective class I HDAC inhibitor, Bioactivity: Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well

with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and HDAC3, respectively. and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.

Purity: 99.65% Purity: 99.95% Clinical Data: Phase 3 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in , 10 mg, 50 mg, 100 mg, 200 mg 2 mg, 5 mg, 10 mg, 50 mg

FT895 Givinostat Cat. No.: HY-112285 (ITF-2357) Cat. No.: HY-14842

Bioactivity: FT895 is a potent and selective HDAC11 inhibitor with an IC50 Bioactivity: Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 of 3 nM [1]. and 157 nM for HDAC1 and HDAC3, respectively.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 500 mg, 250 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 69

Givinostat hydrochloride Givinostat hydrochloride monohydrate (ITF-2357 hydrochloride) Cat. No.: HY-14842A (ITF-2357 hydrochloride monohydrate) Cat. No.: HY-14842B

Bioactivity: Givinostat hydrochloride (ITF-2357 hydrochloride) is a HDAC Bioactivity: Givinostat hydrochloride monohydrate (ITF-2357 hydrochloride monohydrate) is a HDAC inhibitor with an IC of 198 and 157 inhibitor with an IC50 of 198 and 157 nM for HDAC1 and 50 HDAC3, respectively. nM for HDAC1 and HDAC3, respectively.

Purity: >98% Purity: 98.0% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

HDAC-IN-3 HDAC-IN-4 Cat. No.: HY-19772 (CXD101) Cat. No.: HY-100748

Bioactivity: HDAC-IN-3 is a histone deacetylase (HDAC) inhibitor, extracted Bioactivity: HDAC-IN-4 is a histone deacetylase (HDAC) inhibitor, extracted from patent WO/2008040934 A1. from patent WO/2007045844 A1 20070426.

Purity: 98.86% Purity: 98.14% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

HDAC-IN-5 HDAC-IN-7 Cat. No.: HY-18362 (Chidamide impurity) Cat. No.: HY-13592

Bioactivity: HDAC-IN-5 is a histone deacetylase (HDAC) inhibitor. Bioactivity: HDAC-IN-7 (Chidamide impurity) is an impurity of Chidamide. Chidamide is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor.

Purity: >98% Purity: 96.09% Clinical Data: No Development Reported Clinical Data: Launched Size: 250 mg, 500 mg Size: 2 mg, 5 mg, 10 mg, 50 mg

HDAC6-IN-1 HDAC8-IN-1 Cat. No.: HY-18947 Cat. No.: HY-111342

Bioactivity: HDAC6-IN-1 is a potent and selective inhibitor for HDAC6 with Bioactivity: HDAC8-IN-1 is a HDAC8 inhibitor with an IC50 of 27.2 nM. an IC50 of 17 nM and shows 25-fold and 200-fold selectivity

relative to HDAC1 ( IC50=422 nM) and HDAC8 ( IC50=3398 nM), respectively. Purity: 98.49% Purity: 99.59% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

HDACs/mTOR Inhibitor 1 HPOB Cat. No.: HY-114414 Cat. No.: HY-19747

Bioactivity: HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) Bioactivity: HPOB is a highly potent and selective inhibitor of histone and mammalian target of Rapamycin (mTOR) target deacetylase 6 (HDAC6) with IC50 of 56 nM, >30 fold less potent against other HDACs. target: HDAC6 [1] IC 50: 56nM [1] inhibitor for treating hematologic malignancies, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM and >500 nM for HDAC1, HDAC6, mTOR In vitro: HPOB causes growth inhibition of normal and and PI3Kα, respectively. HDACs/mTOR Inhibitor 1 stimulates… transformed cells but does not induce cell death. HPOB… Purity: >98% Purity: 95.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

70 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

IDO1 and HDAC1 Inhibitor ITSA-1 Cat. No.: HY-112147 Cat. No.: HY-100508

Bioactivity: IDO1 and HDAC1 Inhibitor (Compound 10) is a dual IDO1 and Bioactivity: ITSA-1 is membrane permeable and specifically suppresses TSA inhibition of HDAC (histone deacetylase), but not other HDAC HDAC1 inhibitor with IC50s of 69.0 nM and 66.5 nM, inhibitors. respectively [1].

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg, 100 mg Size: 10mM x 1mL in DMSO, 10 mg, 25 mg, 50 mg, 100 mg

J22352 JAK/HDAC-IN-1 Cat. No.: HY-126147 Cat. No.: HY-126141

Bioactivity: J22352 is a PROTAC (proteolysis-targeting chimeras)-like and Bioactivity: JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits

highly selective HDAC6 inhibitor with an IC50 value of 4.7 antiproliferative and proapoptotic activities in several hematological cell lines. JAK/HDAC-IN-1 shows IC s of 4 and 2 nM. J22352 promotes HDAC6 degradation and induces anticancer 50 effects by inhibiting autophagy and eliciting the antitumor nM for JAK2 and HDAC, respectively [1]. immune response in glioblastoma cancers, and leading to the… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 100 mg, 250 mg, 500 mg Size: 100 mg, 250 mg, 500 mg

LMK-235 M344 Cat. No.: HY-18998 (D 237; MS 344) Cat. No.: HY-13506

Bioactivity: LMK-235 is a potent and selective HDAC4/5 inhibitor, inhibits Bioactivity: M344 (D 237) is an inhibitor of histone deacetylase ( IC50=100 HDAC5, HDAC4, HDAC6, HDAC1, HDAC2, HDAC11 and HDAC8, with nM) and an inducer of terminal cell fifferentiation. IC50s of 4.22 nM, 11.9 nM, 55.7 nM, 320 nM, 881 nM, 852 nM and 1278 nM, respectively, and is used in cancer research.

Purity: 99.46% Purity: 99.36% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg 5 mg, 10 mg, 50 mg

MC1568 Mocetinostat Cat. No.: HY-16914 (MGCD0103) Cat. No.: HY-12164

Bioactivity: MC1568 is a selective class II (IIa) histone deacetylas ( Bioactivity: Mocetinostat (MGCD0103) is a potent, orally active and

HDAC II) inhibitor, used for cancer research. isotype-selective HDAC (Class I/IV) inhibitor with IC50s of 0.15, 0.29, 1.66 and 0.59 μM for HDAC1, HDAC2, HDAC3 and HDAC11, respectively. Mocetinostat shows no inhibition on HDAC4, HDAC5, HDAC6, HDAC7, or HDAC8. Purity: 98.02% Purity: 99.81% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

Nanatinostat Nexturastat A (CHR-3996) Cat. No.: HY-13432 Cat. No.: HY-16699

Bioactivity: Nanatinostat (CHR-3996) is a potent, class I selective and Bioactivity: Nexturastat A is a potent and selective HDAC6 inhibitor with orally active histone deacetylase (HDAC) inhibitor with an IC50 of 5 nM; no inhibition on other HDAC forms. [1] IC50 of 8 nM .

Purity: >98% Purity: 97.92% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 71

NKL 22 Oxamflatin Cat. No.: HY-100384 (Metacept-3) Cat. No.: HY-102033

Bioactivity: NKL 22 is a HDAC inhibitor. The value of IC 50 is 78 uM NKL 22 Bioactivity: Oxamflatin (Metacept-3) is a potent HDAC inhibitor with an increase frataxin protein concentrations NKL 22 inhibitors IC50 of 15.7 nM. increase FXN mRNA in FRDA lymphocytes. HDAC inhibitors act directly on FXN. [1]

Purity: 97.97% Purity: 98.67% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 25 mg

Panobinostat PCI-34051 (LBH589; NVP-LBH589) Cat. No.: HY-10224 Cat. No.: HY-15224

Bioactivity: is a non-selective histone deacetylase ( HDAC) Bioactivity: PCI-34051 is a potent and selective HDAC8 inhibitor with IC50 inhibitor. of 10 nM, with >200-fold selectivity over the other HDAC isoforms.

Purity: 98.42% Purity: 99.46% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

PI3K/HDAC-IN-1 Pimelic Diphenylamide 106 Cat. No.: HY-128582 (RGFA-8; TC-H 106; Histone Deacetylase Inhibitor VII) Cat. No.: HY-19348

Bioactivity: PI3K/HDAC-IN-1 is a potent dual inhibitor of PI3K/HDAC, Bioactivity: Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I HDAC (HDAC 1, 2, and 3, with IC50 values of 150 nM potently inhibits PI3Kδ and HDAC1 with IC50s of 8.1 nM and 1.4 , 760nM, and 370 nM, respectively), demonstrating no activity nM, respectively [1]. against class II HDACs.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 100 mg, 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Pracinostat PTACH (SB939) Cat. No.: HY-13322 (NCH-51) Cat. No.: HY-12954

Bioactivity: Pracinostat is a potent histone deacetylase (HDAC) inhibitor, Bioactivity: PTACH (NCH-51) is a SAHA-based novel inhibitor of human HDAC. PTACH exerts potent growth inhibition against various human with IC50s of 40-140 nM, used for cancer research. cancer cells, with EC50 values ranging from 1 to 10 μM.

Purity: 99.07% Purity: 99.36% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

Quisinostat Remetinostat (JNJ-26481585) Cat. No.: HY-15433 (SHP-141) Cat. No.: HY-100365

Bioactivity: Quisinostat (JNJ-26481585) is an orally available, potent Bioactivity: Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of

HDAC inhibitor with an IC50 of 0.11 nM for HDAC1. histone deacetylase enzymes (HDAC) which is under development for the treatment of cutaneous T-cell lymphoma [1].

Purity: 98.0% Purity: 98.0% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

72 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Resminostat Resminostat hydrochloride (RAS2410; 4SC-201) Cat. No.: HY-14718 (RAS2410 hydrochloride; 4SC-201 hydrochloride) Cat. No.: HY-14718A

Bioactivity: Resminostat is a potent inhibitor of HDAC1, HDAC3 and Bioactivity: Resminostat hydrochloride is a potent inhibitor of HDAC1,

HDAC6, with mean IC50 values of 42.5, 50.1, 71.8 nM, HDAC3 and HDAC6, with mean IC50 values of 42.5, 50.1, 71.8 respectively, and shows less potent activities against HDAC8, nM, respectively, and shows less potent activities against

with an IC50 of 877 nM. HDAC8, with an IC50 of 877 nM. Purity: >98% Purity: 98.02% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

RG2833 RGFP966 (RGFP109) Cat. No.: HY-16425 Cat. No.: HY-13909

Bioactivity: RG2833 is a brain-penetrant HDAC inhibitor with IC50 of 60 nM Bioactivity: RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of and 50 nM for HDAC1 and HDAC3, respectively. 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM.

Purity: 99.14% Purity: 98.99% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Ricolinostat (ACY-1215; Rocilinostat) Cat. No.: HY-16026 (FK 228; FR 901228; NSC 630176) Cat. No.: HY-15149

Bioactivity: Ricolinostat (ACY-1215) is a potent and selective HDAC6 Bioactivity: Romidepsin is a potent HDAC1 and HDAC2 inhibitor with IC50s inhibitor, with an IC of 5 nM. ACY-1215 also inhibits 50 of 36 and 47 nM, respectively.

HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively. Purity: 99.70% Purity: 99.98% Clinical Data: Phase 2 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg

RTS-V5 Santacruzamate A Cat. No.: HY-112908 (CAY-10683) Cat. No.: HY-N0931

Bioactivity: RTS-V5 is a dual HDAC/ with IC50s of Bioactivity: Santacruzamate A (CAY-10683) is a potent and selective HDAC2 [1] 6.9, 18, 15, 0.27, 0.53 μM for HDAC1, HDAC2, HDAC3, HDAC6, inhibitor with an IC50 of 119 pM . HDAC8, respectively.

Purity: >98% Purity: 99.72% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg

Scriptaid Sinapinic acid (Scriptide; GCK1026) Cat. No.: HY-15489 (Sinapic acid) Cat. No.: HY-W009732

Bioactivity: Scriptaid is a potent histone deacetylase (HDAC) inhibitor, Bioactivity: Sinapinic acid (Sinapic acid) is a phenolic compound isolated used in cancer research. from Hydnophytum formicarum Jack. Rhizome, acts as an [1] inhibitor of HDAC, with an IC50 of 2.27 mM , and also inhibits ACE-I activity [2]. Sinapinic acid posssess pot… Purity: 99.12% Purity: 99.61% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 100 mg

www.MedChemExpress.com 73

Sodium Butyrate Sodium phenylbutyrate (Butanoic acid sodium salt) Cat. No.: HY-B0350A (Sodium 4-phenylbutyrate; TriButyrate) Cat. No.: HY-15654

Bioactivity: Butyric acid is a histone deacetylase (HDAC) inhibitor, with Bioactivity: Sodium phenylbutyrate is an inhibitor of HDAC and endoplasmic anti-tumor effects in several cancers. reticulum (ER) stress, used in cancer and infection research.

Purity: 98.00% Purity: 99.75% Clinical Data: Phase 3 Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in Water, 1 g, 5 g, 500 g 100 mg, 200 mg

SR-4370 ST8154AA1 Cat. No.: HY-111400 Cat. No.: HY-112805

Bioactivity: SR-4370 is an inhibitor of HDAC, with IC50s of 0.13 μM, 0.58 Bioactivity: ST8154AA1 is a part of antibody drug conjugates ( ADCs) μM, 0.006 μM, 2.3 μM, and 3.4 μM for HDAC1, HDAC2, HDAC3, charged with HDAC inhibitor by a linker, shows antitumor [1] HDAC8, and HDAC6, respectively. activity .

Purity: 98.33% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

ST8155AA1 Sulforaphane Cat. No.: HY-112806 Cat. No.: HY-13755

Bioactivity: ST8155AA1 is a part of antibody drug conjugates ( ADCs) Bioactivity: Sulforaphane is an isothiocyanate present naturally in widely charged with HDAC inhibitor by a linker, shows antitumor consumed vegetables; has shown anticancer and cardioprotective activity [1]. activities.

Purity: >98% Purity: 99.75% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 250 mg, 500 mg, 100 mg Size: 10mM x 1mL in DMSO, 10 mg, 25 mg, 50 mg, 100 mg

SW-100 Tacedinaline Cat. No.: HY-115475 (N-acetyldinaline; CI-994; Goe-5549) Cat. No.: HY-50934

Bioactivity: SW-100, a selective histone deacetylase 6 (HDAC6) inhibitor Bioactivity: Tacedinaline (N-acetyldinaline) is an inhibitor of the histone deacetylase ( HDAC) with IC s of 0.9, 0.9, 1.2 μM for with an IC50 of 2.3 nM, shows at least 1000-fold selectivity 50 for HDAC6 relative to all other HDAC isozymes. SW-100 displays recombinant HDAC 1, 2 and 3 respectively. a significantly improved ability to cross …

Purity: 99.92% Purity: 99.32% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

Tasquinimod TH34 (ABR-215050) Cat. No.: HY-10528 Cat. No.: HY-111818

Bioactivity: Tasquinimod is an oral antiangiogenic agent in clinical trials Bioactivity: TH34, an HDAC6/ 8/ 10 inhibitor with IC50s of 4.6 μM, 1.9 for the treatment of castration-resistant prostate cancer. μM, and 7.7 μM respectively, shows high selectivity over 2+ Tasquinimod binds to the regulatory Zn binding domain of HDAC1/2/3 [1]. HDAC4 with Kd of 10-30 nM. Purity: 99.85% Purity: >98% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

74 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

TMP195 TMP269 Cat. No.: HY-18361 Cat. No.: HY-18360

Bioactivity: TMP195 is a selective class IIa histone deacetylase ( HDAC) Bioactivity: TMP269 is a novel and selective class IIa histone deacetylase

inhibitor with Kis of 59, 60, 26, 15 nM for HDAC4, HDAC5, (HDAC) inhibitor with IC50s of 157 nM, 97 nM, 43 nM and 23 nM HDAC7 and HDAC9, respectively. for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.

Purity: 99.42% Purity: 98.42% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg

Trichostatin A Tubacin (TSA) Cat. No.: HY-15144 Cat. No.: HY-13428

Bioactivity: is a potent and specific inhibitor of HDAC Bioactivity: Tubacin is a potent and selective inhibitor of HDAC6, with an

class I/II, with an IC50 value of 1.8 nM for HDAC. IC50 value of 4 nM and approximately 350-fold selectivity over HDAC1.

Purity: 99.53% Purity: 98.87% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg 1 mg, 5 mg, 10 mg, 20 mg

Tubastatin A Hydrochloride Tubastatin-A (Tubastatin A HCl; TSA HCl) Cat. No.: HY-13271 Cat. No.: HY-13271A

Bioactivity: Tubastatin A (Hydrochloride) is a potent and selective Bioactivity: Tubastatin-A is a potent and selective

HDAC6 inhibitor with IC50 of 15 nM in a HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). other isozymes except HDAC8 (57-fold more).

Purity: 98.31% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg 10 mg, 50 mg, 100 mg, 200 mg

Tucidinostat UF010 (Chidamide; HBI-8000; CS 055) Cat. No.: HY-109015 Cat. No.: HY-18976

Bioactivity: Tucidinostat is a potent and orally bioavailable HDAC enzymes Bioactivity: UF010 is a potent and selective HDAC inhibitor with IC50 ~0.06 class I ( HDAC1/2/3) and class IIb ( HDAC10) inhibitor, with μM, 0.1 μM, 0.5 μM and 1.5 μM for HDACs 3, 2, 1 and 8, respectively. It has > 6-fold selectivity over other HDACs. IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 ( IC s, 733 nM, 432 nM, respectively), and shows… IC50 value: 0.06 μM (HDAC3), 0.1 μM (HDAC2), 0.5 μM (HDAC1), 50 1.5 μM(HDAC 8) Target: HDAC in vitro: UF010 is a competitive… Purity: 98.01% Purity: 99.36% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

Valproic acid Valproic acid sodium salt (VPA; 2-Propylpentanoic Acid) Cat. No.: HY-10585 (Sodium Valproate) Cat. No.: HY-10585A

Bioactivity: Valproic acid is an HDAC inhibitor, with IC50 in the range of Bioactivity: Valproic acid sodium salt is an anticonvulsants used to treat 0.5 and 2 mM, also inhibits HDAC1 ( IC , 400 μM), and epilepsy, bipolar disorder and migraines. Valproic acid 50 inhibits histone deacetylase 1 (HDAC1) with an IC of 0.4 mM. induces proteasomal degradation of HDAC2; Valproic acid 50 sodium salt is used in the treatment of epilepsy, bipo… Purity: 98.67% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 1 g, 5 g, 25 g 1 g, 5 g, 25 g

www.MedChemExpress.com 75

Vorinostat WT-161 (SAHA) Cat. No.: HY-10221 Cat. No.: HY-100871

Bioactivity: is a potent and orally available inhibitor of Bioactivity: WT-161 is a potent and selective HDAC6 inhibitor with an IC50 HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and of 0.40 nM. HDAC11 (Class IV ), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively.

Purity: 99.90% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 250 mg, 500 mg, 1 g, 5 g 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

76 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] HSP Heat shock proteins

HSP (Heat shock proteins) are a group of proteins induced by heat shock, the most prominent members of this group are a class of functionally related proteins involved in the folding and unfolding of other proteins. HSP expression is increased when cells are exposed to elevated temperatures or other stress. This increase in expression is transcriptionally regulated. The dramatic upregulation of the heat shock proteins is a key part of the heat shock response and is induced primarily by heat shock factor (HSF). HSPs are found in virtually all living organisms, from bacteria to humans. Heat shock proteins appear to serve a significant cardiovascular role. Hsp90, Hsp84, Hsp70, Hsp27, Hsp20 and alpha B crystallin all have been reported as having roles in the cardiovasculature.

www.MedChemExpress.com 77 HSP Inhibitors & Modulators

Alvespimycin Alvespimycin hydrochloride (17-DMAG; NSC 707545) Cat. No.: HY-10389 (17-DMAG hydrochloride; KOS-1022; BMS 826476) Cat. No.: HY-12024

Bioactivity: Alvespimycin is a potent inhibitor of Hsp90, binding to Hsp90 Bioactivity: Alvespimycin hydrochloride is a potent inhibitor of Hsp90,

with an EC50 of 62 ± 29 nM. binding to Hsp90 with EC50 of 62±29 nM.

Purity: >98% Purity: 99.32% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 1 mg Size: 10mM x 1mL in DMSO, 10 mg, 25 mg, 100 mg, 200 mg

Apoptozole Arimoclomol maleate (Apoptosis Activator VII) Cat. No.: HY-15098 (BRX-220) Cat. No.: HY-106443A

Bioactivity: Apoptozole is an inhibitor of the ATPase domain of Hsc70 and Bioactivity: Arimoclomol maleate (BRX-220) is a co-inducer of heat shock proteins ( HSP). Hsp70, with Kds of 0.21 and 0.14 μM, respectively, and can induce apoptosis.

Purity: 99.57% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg 5 mg, 10 mg, 50 mg

BIIB021 Bimoclomol (CNF2024) Cat. No.: HY-10212 Cat. No.: HY-U00398

Bioactivity: BIIB021 is an orally available, fully synthetic inhibitor of Bioactivity: Bimoclomol is a heat shock protein (HSP) coinducer, used for

HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively. treatment of cardiovascular diseases.

Purity: 99.93% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

CCT251236 Col003 Cat. No.: HY-101026 Cat. No.: HY-124817

Bioactivity: CCT251236 is an orally available pirin ligand from a heat Bioactivity: Col003 is a potent inhibitor of Hsp47, competitively binds to shock transcription factor 1 (hsf1) phenotypic screen with an the collagen binding site on Hsp47 ( IC50, 1.8 μM), and IC of 19 nM for inhibition of HSF1-mediated HSP72 50 inhibits collagen secretion by destabilizing the collagen induction. triple helix [1]. Purity: 99.03% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 5 mg

Debio 0932 Ethoxyquin (CUDC-305) Cat. No.: HY-13469 Cat. No.: HY-B1425

Bioactivity: Debio 0932 is an orally active HSP90 inhibitor, with IC50s of Bioactivity: Ethoxyquin is an antioxidant which has been used in animal 100 and 103 nM for HSP90α and HSP90β, respectively. feed for many years and also an inhibitor of heat shock protein 90 ( Hsp90).

Purity: 99.97% Purity: 98.05% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg 1 g

78 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Feretoside Ganetespib Cat. No.: HY-N6249 (STA-9090) Cat. No.: HY-15205

Bioactivity: Feretoside, a phenolic compound extracted from the barks of E. Bioactivity: Ganetespib is a heat shock protein 90 ( HSP90) inhibitor ulmoides, is a HSP inducer which act as cytoprotective which exhibits potent cytotoxicity in a wide variety of agent. hematological and solid tumor cell lines.

Purity: >98% Purity: 99.94% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 5 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

Geldanamycin Grp94 Inhibitor-1 Cat. No.: HY-15230 Cat. No.: HY-112910

Bioactivity: Geldanamycin is a Hsp90 inhibitor with antimicrobial activity Bioactivity: Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with

against many Gram-positive and some Gram-negative bacteria. an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α [1].

Purity: 99.78% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 100 mg, 250 mg, 500 mg 5 mg, 10 mg

HA15 HSF1A Cat. No.: HY-100437 Cat. No.: HY-103000

Bioactivity: HA15, a molecule that targets specifically BiP/ GRP78/ HSPA5, Bioactivity: HSF1A is a cell-permeable activator of heat shock inhibits the ATPase activity of BiP. HA15 strongly increases transcription factor 1 ( HSF1). BiP protein expression in A375 cells [1].

Purity: 99.82% Purity: 99.33% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg

HSP70-IN-1 JG-98 Cat. No.: HY-12622 Cat. No.: HY-117282

Bioactivity: HSP70-IN-1 is a heat shock protein ( HSP) inhibitor; inhibits Bioactivity: JG-98 is an allosteric heat shock protein 70 (Hsp70)

the growth of Kasumi-1 cells with an IC50 of 2.3 μM. inhibitor with anti-cancer activities, which disrupts Hsp70 interaction with a co-chaperone Bag3 and affects signaling pathways important for cancer development [1] [2] [3].

Purity: 98.05% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

KNK437 KRIBB11 (Heat Shock Protein Inhibitor I) Cat. No.: HY-100110 Cat. No.: HY-100872

Bioactivity: KNK437 is a HSP inhibitor, and inhibits the induction of Bioactivity: KRIBB11 is an inhibitor of Heat shock factor 1 (HSF1), with

HSP105, HSP70, and HSP40. IC50 of 1.2 μM.

Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg

www.MedChemExpress.com 79

KU-32 KW-2478 Cat. No.: HY-108248 Cat. No.: HY-13468

Bioactivity: KU-32 is a novel, novobiocin-based Hsp90 inhibitor that can Bioactivity: KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, protect against neuronal cell death. and has antitumor activity against various human hematological tumor cells.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Luminespib MKT-077 (NVP-AUY922; AUY922; VER-52296) Cat. No.: HY-10215 (FJ-776) Cat. No.: HY-15096

Bioactivity: Luminespib (NVP-AUY922) is a potent HSP90 inhibitor with Bioactivity: MKT-077 is a rhodacyanine dye and also a heat shock protein 70 ( Hsp70) inhibitor which exhibits significant antitumor IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively. activity.

Purity: 99.14% Purity: 98.0% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg, 100 mg, 200 mg, 500 mg Size: 1 mg, 5 mg, 10 mg

NVP-HSP990 Onalespib (HSP-990) Cat. No.: HY-15190 (AT13387) Cat. No.: HY-14463

Bioactivity: NVP-HSP990 is a potent and selective Hsp90 inhibitor, with Bioactivity: Onalespib (AT13387) is a potent inhibitor of Hsp90, with a

IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Kd of 0.71 nM. Grp94, respectively.

Purity: 98.98% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

p5 Ligand for Dnak and DnaJ Pifithrin-μ Cat. No.: HY-P1887 (PFTμ; 2-Phenylethynesulfonamide) Cat. No.: HY-10940

Bioactivity: p5 Ligand for Dnak and DnaJ is a nonapeptide, which Bioactivity: Pifithrin-μ is an inhibitor of p53 and HSP70, with antitumor corresponds to the main binding site for the 23-residue part and neuroprotective activity. of the presequence of mitochondrial aspartate aminotransferase. p5 Ligand for Dnak and DnaJ is a high-affinity ligand for DnaK and DnaJ [1]. Purity: >98% Purity: 98.31% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 10mM x 1mL in DMSO, 10 mg

PU-WS13 Retaspimycin Cat. No.: HY-18680 Cat. No.: HY-15263

Bioactivity: PU-WS13 is a selective Grp94 inhibitor, with an EC50 of Bioactivity: Retaspimycin is a potent and water-soluble inhibitor of Hsp90, with EC s of 119 nM for both Hsp90 and Grp9. 0.22 μM. 50

Purity: 95.69% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 100 mg 5 mg, 10 mg, 50 mg

80 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Retaspimycin Hydrochloride Shepherdin 79-87 (IPI-504) Cat. No.: HY-10210 Cat. No.: HY-P1750

Bioactivity: Retaspimycin Hydrochloride is a potent and water-soluble Bioactivity: Shepherdin (79-87) is amino acids 79 to 87 fragment of

inhibitor of Hsp90 with EC50s of 119 nM for both Hsp90 and Shepherdin. Shepherdin is a peptidomimetic antagonist of the [1] Grp9. complex between Hsp90 and Survivin. Anticancer activity .

Purity: 95.0% Purity: >98% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

SNX-5422 Mesylate Tanespimycin (PF-04929113 (Mesylate)) Cat. No.: HY-10213A (17-AAG; NSC 330507; CP 127374) Cat. No.: HY-10211

Bioactivity: SNX-5422 Mesylate (PF-04929113 Mesylate), a prodrug of Bioactivity: Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an SNX-2112, is an orally active Hsp90 inhibitor, with a K of d IC50 of 5 nM, having a 100-fold higher binding affinity for

41 nM, and also induces Her-2 degradation, with an IC50 of tumour cell derived HSP90 than normal cell derived HSP90. 37nM. Purity: >98% Purity: 99.03% Clinical Data: Phase 2 Clinical Data: Phase 3 Size: 5 mg, 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 10 mg, 25 mg, 100 mg, 200 mg

TAS-116 Teprenone Cat. No.: HY-15785 (Geranylgeranylacetone) Cat. No.: HY-B0779

Bioactivity: TAS-116 is an oral bioavailable, ATP-competitive, highly Bioactivity: Teprenone is a anti-ulcer drug, and works as an inducer of

specific HSP90α/HSP90β inhibitor ( Kis of 34.7 nM and 21.3 heat shock proteins ( HSPs). nM, respectively) without inhibiting other HSP90 family proteins such as GRP94 [1]. TAS-116 demonstrates less ocu… Purity: >98% Purity: 99.82% Clinical Data: No Development Reported Clinical Data: Launched Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 100 mg, 500 mg

TRC051384 VER-155008 Cat. No.: HY-101712 Cat. No.: HY-10941

Bioactivity: TRC051384 is a heat shock protein 70 ( HSP70) inducer. Bioactivity: VER-155008 is an inhibitor of Hsp70, with IC50s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively,

and with a Kd of 0.3 μM for Hsp70.

Purity: 97.40% Purity: 99.64% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg 5 mg, 10 mg, 50 mg, 100 mg

VER-49009 VER-50589 (CCT 129397) Cat. No.: HY-15986 Cat. No.: HY-15984

Bioactivity: VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM and a Bioactivity: VER-50589 is a Hsp90 inhibitor, with an IC50 of 21 nM and a

Kd of 78 nM. Kd of 4.5 nM.

Purity: 99.26% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg

www.MedChemExpress.com 81

VER-82576 XL888 (NVP-BEP800) Cat. No.: HY-10942 Cat. No.: HY-13313

Bioactivity: VER-82576 (NVP-BEP800) is a potent, orally available and Bioactivity: XL888 is a heat shock protein-90 ( HSP90) inhibitor, with an selective Hsp90 inhibitor, with an IC of 58 nM for Hsp90β; 50 IC50 of 24 nM.

VER-82576 also slightly blocks Grp94 and Trap-1, with IC50s of 4.1 and 5.5 μM, respectively. Purity: 99.48% Purity: 99.24% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

YZ129 Cat. No.: HY-114413

Bioactivity: YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathway against glioblastoma, directly binding to heat shock protein

90 (HSP90) with an IC50 of 820 nM on NFAT nuclear translocation. YZ129-induced GBM cell-cycle arrest at the G2/M phase promotes apoptosis and inhibited tumor cell… Purity: >98% Clinical Data: No Development Reported Size: 100 mg, 250 mg, 500 mg

82 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] IRE1 requiring enzyme 1

The serine/threonine-protein kinase/endoribonuclease inositol-requiring enzyme 1 (IRE1) is an enzyme that in humans is encoded by the ERN1 gene. IRE1 is an endoplasmic reticulum (ER) transmembrane sensor that activates UPR to maintain ER and cellular function. While mammalian IRE1 promotes cell survive, it can initiate apoptosis via decay of anti-apoptotic . IRE1 activation is initiated by homotypic interactions of the stress-sensing lumenal domain favoring transautophosphorylation of the kinase-extension nuclease (KEN) domain on the cytoplasmic side of the ER membrane. IRE1/XBP-1 has been shown to regulate a variety of genes in various cell types in response to ER stress, mostly related to ER function and the secretory pathway, although the target genes vary depending on the cell type and nature of the stress stimuli.

www.MedChemExpress.com 83 IRE1 Inhibitors & Modulators

3,6-DMAD hydrochloride 4μ8C Cat. No.: HY-U00460 (IRE1 Inhibitor III) Cat. No.: HY-19707

Bioactivity: 3,6-DMAD hydrochloride is a inhibitor of the IRE1α-XBP1 pathway Bioactivity: 4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of of the unfolded protein response. IRE1α.

Purity: 98.0% Purity: 98.52% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

6-Bromo-2-hydroxy-3-methoxybenzaldehyde APY29 (NSC95682) Cat. No.: HY-107371 Cat. No.: HY-17537

Bioactivity: 6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) is an Bioactivity: APY29 is an allosteric modulator of IRE1α which inhibits IRE1α IRE-1α autophosphorylation with IC50 of 280 nM and activates IRE1α inhibitor with an IC of 0.08 μM, extracted from patent WO 50 RNase activity. 2008154484 A1, IRE-lα inhibitor compound 3-5.

Purity: 99.87% Purity: 99.54% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg 10 mg, 50 mg

B I09 GSK2850163 Cat. No.: HY-107400 Cat. No.: HY-U00459

Bioactivity: B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM. Bioactivity: GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha ( IRE1α) which can inhibit IRE1α kinase activity and RNase

activity with IC50s of 20 and 200 nM, respectively.

Purity: >98% Purity: 98.50% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg

GSK2850163 hydrochloride KIRA6 Cat. No.: HY-U00459B Cat. No.: HY-19708

Bioactivity: GSK2850163 hydrochloride is a novel inhibitor of Bioactivity: KIRA6 allosterically inhibits IRE1α RNase kinase activity with inositol-requiring enzyme-1 alpha ( IRE1α) which can inhibit an IC50 of 0.6 µM. IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.

Purity: >98% Purity: 98.75% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg Size: 1 mg, 5 mg, 10 mg

Kira8 MKC3946 Cat. No.: HY-114368 Cat. No.: HY-19710

Bioactivity: Kira8 is a mono-selective IRE1α inhibitor that allosterically Bioactivity: MKC3946 is a potent and soluble IRE1α inhibitor, used for [1] cancer research. attenuates IRE1α RNase activity with an IC50 of 5.9 nM .

Purity: >98% Purity: 99.77% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

84 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

MKC8866 MKC9989 Cat. No.: HY-104040 Cat. No.: HY-12399

Bioactivity: MKC8866 is an IRE1 RNase inhibitor with an IC50 of less than Bioactivity: MKC9989 is a Hydroxy aryl aldehydes ( HAA) inhibitor and also inhibits IRE1α with an IC of 0.23 to 44 μM. 0.1 μM for IRE1α RNase. 50

Purity: 98.38% Purity: 98.61% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

STF-083010 Cat. No.: HY-15845

Bioactivity: STF-083010 is an Ire1 inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.

Purity: 98.0% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

www.MedChemExpress.com 85 Kinesin

Kinesin is a protein belonging to a class of motor proteins found in eukaryotic cells. Kinesins move along microtubule filaments, and are powered by the hydrolysis of ATP (thus kinesins are ATPases). The active movement of kinesins supports several cellular functions including mitosis, meiosis and transport of cellular cargo. Most kinesins walk towards the plus end of a microtubule, entails transporting cargo from the centre of the cell towards the periphery. Kinesins were discovered as microtubule (MT)-based anterograde intracellular transport motors. The founding member of this superfamily, the genomes of mammals encode more than 40 kinesin proteins, organized into at least 14 families named kinesin-1 through kinesin-14.

86 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Kinesin Inhibitors & Modulators

(R)-Filanesib AZ82 ((R)-ARRY-520) Cat. No.: HY-15187A Cat. No.: HY-12241

Bioactivity: (R)-Filanesib ((R)-ARRY-520) is the R-enantiomer of ARRY-520. Bioactivity: AZ82 is a selective kinesin-like protein KIFC1 (HSET/KIFC1) (R)-Filanesib ((R)-ARRY-520) is a synthetic kinesin spindle inhibitor, with a Ki of 43 nM and an IC50 of 300 nM for KIFC1. protein (KSP) inhibitor with IC50 of 6 nM.

Purity: 98.86% Purity: 99.08% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg

CW-069 Dimethylenastron Cat. No.: HY-15857 Cat. No.: HY-19944

Bioactivity: CW-069 is an allosteric inhibitor of microtubule motor Bioactivity: Dimethylenastron is a potent kinesin Eg5 inhibitor, with an

protein HSET with an IC50 of 75 μM. IC50 of 200 nM.

Purity: 99.75% Purity: 98.24% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg

Eg5 Inhibitor V, trans-24 EMD534085 Cat. No.: HY-112915 Cat. No.: HY-15000

Bioactivity: Eg5 Inhibitor V, trans-24 is a potent and specific kinesin Eg5 Bioactivity: EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC of 8 nM. inhibitor with an IC50 of 0.65 μM, and can be used in the 50 research of cancer.

Purity: >98% Purity: 98.61% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg

Filanesib Ispinesib (ARRY-520) Cat. No.: HY-15187 (SB-715992) Cat. No.: HY-50759

Bioactivity: Filanesib (ARRY-520) is a synthetic kinesin spindle protein Bioactivity: Ispinesib is a specific inhibitor of kinesin spindle protein

(KSP) inhibitor with IC50 of 6 nM. (KSP), with a Ki app of 1.7 nM.

Purity: 99.73% Purity: 98.71% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg

K858 Racemic Kif15-IN-1 Cat. No.: HY-19966 Cat. No.: HY-15948

Bioactivity: K858 Racemic is an ATP-uncompetitive inhibitor of kinesin Eg5 Bioactivity: Kif15-IN-1 is an inhibitor of the mitotic Kinesin family member

with an IC50 of 1.3 μM. 15 (Kif15), and is used for the research of cellular proliferative diseases.

Purity: 99.93% Purity: 99.04% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 87

Kif15-IN-2 Litronesib Cat. No.: HY-15949 (LY-2523355; KF-89617) Cat. No.: HY-14846

Bioactivity: Kif15-IN-2 is an inhibitor of the mitotic kinesin Kif15, and is Bioactivity: Litronesib is a selective mitosis-specific kinesin Eg5 used for the research of cellular proliferative diseases. inhibitor, with antitumor activity.

Purity: 96.51% Purity: 99.59% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Litronesib Racemate Monastrol (LY-2523355 Racemate; KF-89617 Racemate) Cat. No.: HY-14846A ((±)-Monastrol) Cat. No.: HY-101071A

Bioactivity: Litronesib (Racemate) is the racemate of litronesib. Bioactivity: Monastrol is a potent and cell-permeable inhibitor of the

Litronesib is a selective, allosteric inhibitor of kinesin mitotic kinesin Eg5 with an IC50 value of 14 μM. Eg5.

Purity: 99.00% Purity: 99.89% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

Paprotrain PF-2771 Cat. No.: HY-101298 Cat. No.: HY-19530

Bioactivity: Paprotrain is a cell-permeable inhibitor of the kinesin Bioactivity: PF-2771 is a potent and selective centromere protein E

MKLP-2, inhibits the ATPase activity of MKLP-2 with an IC50 (CENP-E) inhibitor, inhibiting CENP-E motor activity with an IC50 of 16.1 nM; PF-2771 is used as an anticancer agent. of 1.35 μM and a Ki of 3.36 μM and shows a moderate inhibition

activity on DYRK1A with an IC50 of 5.5 μM. Purity: 97.05% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

SB-743921 Cat. No.: HY-12069

Bioactivity: SB-743921 is a potent inhibitor of the mitotic kinesin KSP

(Eg5), with a Ki of 0.1 nM.

Purity: 97.31% Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

88 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] LIM Kinase (LIMK) LIMKs

LIM kinases (LIMKs) are important cell cytoskeleton regulators that play a prominent role in cancer manifestation and neuronal diseases. The LIMK family consists of two homologues, LIMK1 and LIMK2, which differ from one another in expression profile, intercellular localization, and function. The main substrate of LIMK is cofilin, a member of the actin-depolymerizing factor (ADF) protein family. When phosphorylated by LIMK, cofilin is inactive. LIMKs play a contributory role in several neurodevelopmental disorders and in cancer growth and . LIM domain kinases (LIMK1 and 2) are substrate for Cdc42/Rac-PAK, and modulate actin dynamics by phosphorylating cofilin at serine-3. This modification inactivates cofilin’s actin severing and depolymerizing activity. LIMKs also translocate into the nucleus and regulate cell cycle progression. LIMKs are potential therapeutic targets for NF2 and other merlin-deficient tumors.

www.MedChemExpress.com 89 LIM Kinase (LIMK) Inhibitors & Modulators

BMS-3 BMS-5 Cat. No.: HY-18304 (LIMKi 3) Cat. No.: HY-18305

Bioactivity: BMS-3 is a potent LIMK inhibitor with IC50s of 5 nM and 6 Bioactivity: BMS-5 (LIMKi 3) is a potent LIMK inhibitor with IC50s of 7 nM for LIMK1 and LIMK2, respectively. nM and 8 nM for LIMK1 and LIMK2, respectively.

Purity: 99.98% Purity: 99.35% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

R-10015 T56-LIMKi Cat. No.: HY-120097 (T5601640) Cat. No.: HY-19352

Bioactivity: R-10015, a broad-spectrum antiviral compound for HIV Bioactivity: T56-LIMKi is a selective inhibitor of LIMK2; inhibits the infection, acts as a potent and selective inhibitor of LIM growth of Panc-1 cells with an IC50 of 35.2 μM. domain kinase (LIMK) and binds to the ATP-binding pocket, [1] with an IC50 of 38 nM for human LIMK1 . Purity: >98% Purity: 98.02% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

90 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Microtubule/Tubulin

Microtubules are a component of the cytoskeleton, found throughout the cytoplasm. These tubular of tubulin can grow as long as 50 micrometres, with an average length of 25 µm, and are highly dynamic. The outer diameter of a microtubule is about 24 nm while the inner diameter is about 12 nm. are found in eukaryotic cells and are formed by the polymerization of a dimer of two globular proteins, alpha and beta tubulin. Tubulin is one of several members of a small family of globular proteins. The tubulin superfamily includes five distinct families, the alpha-, beta-, gamma-, delta-, and epsilon- and a sixth family which is present only in kinetoplastid protozoa. The most common members of the tubulin family are α-tubulin and β-tubulin, the proteins that make up microtubules. Microtubules are very important in a number of cellular processes. They are involved in maintaining the structure of the cell.

www.MedChemExpress.com 91 Microtubule/Tubulin Inhibitors & Modulators

10-Deacetyl-7-xylosyl (10-Deacetyl-7-xylosyltaxol; 10-Oxo 10-Deacetylpaclitaxel 7-Xyloside; …) Cat. No.: HY-20584 (Docetaxel Impurity 1) Cat. No.: HY-16674

Bioactivity: 10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivative Bioactivity: 10-Oxo Docetaxel (Docetaxel Impurity) is a novel taxoid having with improved pharmacological features and higher water remarkable anti-tumor properties and a Docetaxel intermediate. solubility. IC50 value: Target: Microtubule inhibitor 10-Deacetyl-7-xylosyl paclitaxel induced mitotic cell cycle arrest and apoptosis as measured by flow cytometry, DNA… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 50 mg Size: 1 mg, 5 mg, 10 mg

2-Methoxyestradiol 4'-Demethylepipodophyllotoxin (2-ME2; NSC-659853) Cat. No.: HY-12033 (4'-O-demethylepipodophyllotoxin; 4'-DMEP) Cat. No.: HY-17435

Bioactivity: 2-Methoxyestradiol is an angiogenesis inhibitor and apoptosis Bioactivity: 4'-Demethylepipodophyllotoxin(4'-DMEP) is a key intermediate inducer with potent antineoplastic activity. compound for the preparation of -type 2-Methoxyestradiol also destablize microtubules. anti-cancer drugs; a potent inhibitor of microtubule assembly.

Purity: 99.82% Purity: 99.20% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 50 mg, 100 mg

7-Epi-10-oxo-docetaxel 7-Epi-docetaxel (Docetaxel Impurity 2) Cat. No.: HY-16675 (4-epi-Docetaxel; 7-Epidocetaxel; 7-Epitaxotere) Cat. No.: HY-16676

Bioactivity: 7-Epi-10-oxo-docetaxel (Docetaxel Impurity D) is a impurity of Bioactivity: 7-Epi-10-oxo-docetaxel (Docetaxel Impurity C; 7-Epitaxotere) docetaxel detected by high performance liquid chromatography is a impurity of docetaxel. (HPLC).

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10mM x 1mL in DMSO, 1 mg, 10 mg

7-epi-Taxol 7-xylosyltaxol (7-epi-Paclitaxel) Cat. No.: HY-N0227 (7-Xylosylpaclitaxel; Taxol-7-xyloside) Cat. No.: HY-77574

Bioactivity: 7-epi-Taxol is an active metabolite of taxol, with activity Bioactivity: 7-xylosyltaxol(Taxol-7-xyloside) is a taxol (Paclitaxel) comparable to that of taxol against cell replication, derivative; Paclitaxel binds to tubulin and inhibits the promoting microtubule bundle formation and against disassembly of microtubules. microtubule depolymerization.

Purity: 99.75% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

ABT-751 Amphethinile (E7010) Cat. No.: HY-13270 (Amphetinile; CRC 82-07) Cat. No.: HY-100190

Bioactivity: ABT-751(E 7010) is a novel bioavailable tubulin-binding and Bioactivity: Amphethinile is an anti-tubulin agent. The affinity constant

antimitotic sulfonamide agent with IC50 of about 1.5 and 3.4 for the association ( Ka) of Amphethinile with tubulin is μM in neuroblastoma and non-neuroblastoma cell lines, 1.3 μM. respectively. IC50 Value: 1.5 μM(neuroblastoma); 3.4 μM(non-neuroblastoma) Target: Microtubule/Tubulin in vitro:… Purity: 99.87% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 10 mg, 50 mg, 100 mg

92 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Ansamitocin P-3 Auristatin E (Antibiotic C 15003P3; Maytansinol isobutyrate) Cat. No.: HY-15739 Cat. No.: HY-15582

Bioactivity: Ansamitocin P-3 is a microtubule inhibitor. Ansamitocin P-3 Bioactivity: Auristatin E is a cytotoxic tubulin modifier with potent and is a macrocyclic antitumor antibiotic. selective antitumor activity; MMAE analog and cytotoxin in Antibody-drug conjugates.

Purity: 98.0% Purity: 99.36% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg

Auristatin F BNC105 Cat. No.: HY-15583 Cat. No.: HY-16114

Bioactivity: Auristatin F is a cytotoxic tubulin modifier with potent and Bioactivity: BNC105 is a tubulin polymerization inhibitor with potent selective antitumor activity; MMAF analog and cytotoxin in antiproliferative and tumor vascular disrupting properties. Antibody-drug conjugates.

Purity: 97.51% Purity: 99.49% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg

BTB-1 Cat. No.: HY-101770 (XRP6258; RPR-116258A; taxoid XRP6258) Cat. No.: HY-15459

Bioactivity: BTB-1 is a potent, selective and reversible mitotic motor Bioactivity: Cabazitaxel is a semi-synthetic derivative of the natural

protein Kif18A inhibitor with an IC50 of 1.69 μM. taxoid 10-deacetylbaccatin III with potential antineoplastic activity.

Purity: 99.62% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

CCB02 Cephalomannine Cat. No.: HY-114302 Cat. No.: HY-77554

Bioactivity: CCB02 is a selective CPAP-tubulin interaction inhibitor, binding Bioactivity: Cephalomannine is a taxol derivative with antitumor, to tubulin and competing for the CPAP binding site of antiproliferative properties.

β-tubulin, with an IC50 of 689 nM, and shows potent anti-tumor activity. CCB02 shows no inhibition on the cell cycle- and centrosome-related kinases, or the phosphorylation status of… Purity: >98% Purity: 99.29% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg

Cevipabulin Cevipabulin fumarate (TTI-237) Cat. No.: HY-14949 (TTI-237 fumarate) Cat. No.: HY-14949C

Bioactivity: Cevipabulin (TTI-237) is an oral, microtubule-active antitumor Bioactivity: Cevipabulin fumarate (TTI-237 fumarate) is an oral, compound and inhibits the binding of [ 3H] vinblastine to microtubule-active, antitumor compound and inhibits the 3 tubulin, with an IC50 of 18-40 nM for cytotoxicity in human binding of [ H] vinblastine to tubulin, with an IC50 of tumor cell line [1] [2]. 18-40 nM for cytotoxicity in human tumor cell line [1] [2]. Purity: 99.03% Purity: 99.08% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 93

Colchicine Combretastatin A4 Cat. No.: HY-16569 (CRC 87-09) Cat. No.: HY-N2146

Bioactivity: is a tubulin inhibitor and a microtubule Bioactivity: Combretastatin A4 is a microtubule-targeting agent that

disrupting agent. Colchicine inhibits microtubule binds β-tubulin with Kd of 0.4 μM. polymerization with an IC50 of 3 nM.

Purity: 99.98% Purity: 99.41% Clinical Data: Launched Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 200 mg, 500 mg 5 mg, 10 mg, 25 mg

Crolibulin Cys-mcMMAD (EPC2407) Cat. No.: HY-13603 Cat. No.: HY-15750

Bioactivity: Crolibulin is a small molecule tubulin polymerization Bioactivity: Monomethyl auristatin D (MMAD), a potent tubulin inhibitor, is inhibitor. a toxin payload in antibody drug conjugate. IC50 Value: N/A Target: tubulin; ADCs For comparison purposes, the ADC A1 -mc-MMAD and/or A1 -vc-MMAD were used. The linker payload, mc-MMAD (6-maleimidocaproyl-monomethylauristatin-D) was… Purity: 98.04% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

D-64131 D8-MMAD (Demethyldolastatin 10 D8; Monomethylauristatin D D8; Cat. No.: HY-15482 Monomethyl Dolastatin 10 D8) Cat. No.: HY-15581S

Bioactivity: D-64131 is a novel inhibitor of Tubulin polymerization that Bioactivity: D8-MMAD is a deuterated form of MMAD, which is a competitively binds with [(3)H]colchicine to αβ-Tubulin. microtubule disrupting agent.

Purity: 99.42% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 1 mg, 5 mg, 10 mg

D8-MMAE D8-MMAF (D8-) Cat. No.: HY-15162A (Monomethylauristatin F D8) Cat. No.: HY-15579S

Bioactivity: D8-MMAE is a deuterated labeled MMAE, a potent mitotic Bioactivity: D8-MMAF is a deuterated form of MMAF, which is a inhibitor. microtubule disrupting agent.

Purity: 98.31% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg

D8-MMAF hydrochloride DM4 Cat. No.: HY-15579AS Cat. No.: HY-12454

Bioactivity: D8-MMAF hydrochloride is a deuterated form of MMAF Bioactivity: DM4 is is an antitubulin agent that inhibit cell division. DM4 hydrochloride, which is a microtubule disrupting agent. can be used in the preparation of antibody drug conjugate.

Purity: 99.56% Purity: 98.28% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

94 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Docetaxel Docetaxel Trihydrate (RP-56976) Cat. No.: HY-B0011 (RP-56976 (Trihydrate)) Cat. No.: HY-B0011A

Bioactivity: Docetaxel is an antineoplastic drug by inhibiting Bioactivity: Docetaxel Trihydrate is a semi-synthetic analogue, acts microtubule depolymerization, and attenuating of the as a microtubule stabilizer. effects of bcl-2 and bcl-xL gene expression.

Purity: 99.93% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 200 mg 100 mg, 200 mg

Dolastatin 10 ELR510444 (DLS 10; NSC 376128) Cat. No.: HY-15580 Cat. No.: HY-16191

Bioactivity: Angiotensin II human is a vasoconstrictor that acts on the Bioactivity: ELR510444 is a novel microtubule disruptor; inhibits AT1 and the AT2 receptor. MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.

Purity: 99.83% Purity: 95.55% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Entasobulin A Cat. No.: HY-16777 (Epo A) Cat. No.: HY-13503

Bioactivity: Entasobulin is a β-tubulin polymerization inhibitor with Bioactivity: Epothilone A is a competitive inhibitor of the binding of [ potential anticancer activity. 3 H] paclitaxel to tubulin polymers, with a Ki of 0.6-1.4 μM.

Purity: 98.04% Purity: 99.05% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 20 mg 1 mg, 5 mg, 10 mg, 25 mg

Epothilone B Epothilone D (EPO 906; Patupilone) Cat. No.: HY-17029 (KOS 862) Cat. No.: HY-15278

Bioactivity: Epothilone B is a microtubule stabilizer with a Ki of Bioactivity: Epothilone D (KOS 862) is a potent microtubule stabilizer. 0.71μM. It acts by binding to the αβ-tubulin heterodimer subunit which causes decreasing of αβ-tubulin dissociation.

Purity: 99.88% Purity: 99.93% Clinical Data: Phase 3 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg 2 mg, 5 mg, 10 mg, 25 mg

Eribulin mesylate (B1939; E7389; ER-086526) Cat. No.: HY-13442 (B1939 mesylate; E7389 mesylate; ER-086526 mesylate) Cat. No.: HY-13442A

Bioactivity: Eribulin (E7389) is a microtubule targeting agent that is Bioactivity: Eribulin mesylate (E7389 mesylate) is a microtubule used in the treatment of metastatic breast cancer. Eribulin targeting agent that is used in the treatment of metastatic (E7389) inhibits the proliferation of cancer cells by binding breast cancer. Eribulin mesylate (E7389 mesylate) inhibits the microtubule proteins and microtubules. proliferation of cancer cells by binding microtubule proteins and microtubules. Purity: >98% Purity: 98.97% Clinical Data: Launched Clinical Data: Launched Size: 1 mg Size: 500u g, 1 mg

www.MedChemExpress.com 95

Estramustine phosphate sodium Fosbretabulin disodium Cat. No.: HY-13627 (CA 4DP; CA 4P; Combretastatin A4 disodium phosphate) Cat. No.: HY-17449

Bioactivity: sodium is an antimicrotubule Bioactivity: Fosbretabulin disodium(CA 4DP; CA 4P) is a microtubule chemotherapy agent; arrests prostate cancer cells in the G2/M destabilizing drug, a type of vascular-targeting agent, a drug phase of the cell cycle. designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis. IC50 Value: 4 nM [1] Target: microtubule in vitro: Cytotoxic IC(50) values of CA-4 in human… Purity: 98.01% Purity: 99.47% Clinical Data: Launched Clinical Data: Phase 3 Size: 10mM x 1mL in Water, Size: 10mM x 1mL in Water, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

Ixabepilone Lexibulin (Azaepothilone B; BMS 247550; BMS 247550-1) Cat. No.: HY-10222 (CYT-997) Cat. No.: HY-10498

Bioactivity: is an orally bioavailable Bioactivity: Lexibulin(CYT-997) is a potent tubulin polymerisation microtubule inhibitor, which binds to tubulin and inhibitor with IC50 of 10-100 nM in cancer cell lines; with promotes tubulin polymerization and microtubule stabilization, potent cytotoxic and vascular disrupting activity in vitro and thereby arrests cells in the G2-M phase of the cell cycle and in vivo. induces tumor cell apoptosis. Purity: 99.93% Purity: 99.46% Clinical Data: Launched Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg

Lexibulin dihydrochloride Maytansinol (CYT-997 dihydrochloride) Cat. No.: HY-10498A (Ansamitocin P-0) Cat. No.: HY-19474

Bioactivity: Lexibulin 2Hcl (CYT-997 2Hcl) is a potent tubulin Bioactivity: Maytansinol inhibits microtubule assembly and induces polymerisation inhibitor with IC50 of 10-100 nM in cancer cell microtubule disassembly in vitro. Target: Microtubule/Tubulin lines; with potent cytotoxic and vascular disrupting activity in vitro: Maytansinol disrupts the mitotic spindle and in vitro and in vivo. prevents mitotic exit in Drosophila. Maytansinol reduces the growth and/or survival of HCT116 cells in a dose-dependent… Purity: >98% Purity: 99.03% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

Mc-MMAD Mc-MMAE Cat. No.: HY-15740 (Maleimidocaproyl-monomethylauristatin E) Cat. No.: HY-15741

Bioactivity: Monomethyl auristatin D (MMAD), a potent tubulin inhibitor, is Bioactivity: Mc-MMAE is a protective group (maleimidocaproyl)-conjugated a toxin payload in antibody drug conjugate; Mc-MMAD is a monomethyl auristatin E (MMAE), which is a potent tubulin protective group (maleimidocaproyl) -conjugated MMAD. IC50 inhibitor, is a toxin payload in antibody drug conjugate ( Value: Target: tubulin; ADCs For comparison purposes, the ADC ADC). A1 -mc-MMAD and/or A1 -vc-MMAD were used. The linker Purity: payload,…>98% Purity: 97.23% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg 1 mg, 5 mg, 10 mg

McMMAF Mertansine (Maleimidocaproyl monomethylauristatin F) Cat. No.: HY-15578 (DM1; Maytansinoid DM1) Cat. No.: HY-19792

Bioactivity: Mc-MMAF is a protective group-conjugated MMAF. MMAF is a more Bioactivity: Mertansine (DM1) is a microtubulin inhibitor and is an potent drug than Monomethyl auristatin E (MMAE), but is antibody-conjugatable maytansinoid that is developed to charged and relatively membrane-impermeable, is a potent overcome systemic toxicity associated with maytansine and to tubulin inhibitor, is a toxin payload in antibody drug enhance tumor-specific delivery. Mertansine can be attached to conjugate. Target: MMAF is a new auristatin derivative with a… a monoclonal antibody with a linker to create an antibody-drug… Purity: 99.58% Purity: 98.74% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg

96 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Microtubule inhibitor 1 MMAD (Demethyldolastatin 10; Monomethylauristatin D; Cat. No.: HY-114313 Monomethyl Dolastatin 10) Cat. No.: HY-15581

Bioactivity: Microtubule inhibitor 1 is an antitumor agent with Bioactivity: MMAD is a potent tubulin inhibitor, is a toxin payload in microtubule polymerization inhibitory activity, with an antibody drug conjugates ( ADCs). [1] IC50 value of 9-16 nM in cancer cells .

Purity: >98% Purity: 99.92% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 100 mg, 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

MMAF MMAF Hydrochloride (Monomethylauristatin F) Cat. No.: HY-15579 (Monomethylauristatin F Hydrochloride) Cat. No.: HY-15579A

Bioactivity: MMAF (Monomethylauristatin F) is an antitubulin agent that Bioactivity: MMAF hydrochloride is an antitubulin agent that inhibit cell

inhibit cell division; inhibits H3397 cell growth with an IC50 division; inhibits H3397 cell growth with an IC50 of 105 nM. of 105 nM.

Purity: >98% Purity: 99.89% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 2 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg

Monomethyl auristatin E Nocodazole (MMAE; SGD-1010) Cat. No.: HY-15162 (Oncodazole; R17934) Cat. No.: HY-13520

Bioactivity: Monomethyl auristatin E (MMAE; SGD-1010) is a synthetic Bioactivity: Nocodazole is a rapidly-reversible inhibitor of derivative of dolastatin 10 and functions as a potent microtubule. Nocodazole binds to β-tubulin and disrupts mitotic inhibitor by inhibiting tubulin polymerization. microtubule assembly/disassembly dynamics, which prevents MMAE is widely used as a cytotoxic component of antibody-drug mitosis and induces apoptosis in tumor cells. Nocodazole conjugates (ADCs) to treat several different cancer types. inhibits Bcr-Abl, activates CRISPR/Cas9. Purity: 99.94% Purity: 98.68% Clinical Data: Phase 4 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg, 500 mg, 1 g 10 mg, 50 mg, 100 mg

Ombrabulin Ombrabulin hydrochloride (AVE8062; AC7700) Cat. No.: HY-14797 (AVE8062 (hydrochloride); AC7700 (hydrochloride)) Cat. No.: HY-18256

Bioactivity: Ombrabulin (AVE8062) is a derivative of CA-4 phosphate, which Bioactivity: Ombrabulin hydrochloride is a derivative of CA-4 phosphate, is known to exhibit antivascular effects through selective which is known to exhibit antivascular effects through disruption of the tubulin cytoskeleton of endothelial cells. selective disruption of the tubulin cytoskeleton of endothelial cells.

Purity: >98% Purity: 99.57% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in Water, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

OSIP-486823 Paclitaxel (OSIP 486823; OSIP486823; CP248) Cat. No.: HY-U00004 (Taxol) Cat. No.: HY-B0015

Bioactivity: OSIP-486823 is a novel microtubule-interfering agent with Bioactivity: Paclitaxel (Taxol), a naturally occurring antineoplastic distinct biological effects on both protein kinase G (PKG) and agent, stabilizes tubulin polymerization, resulting in microtubules. arrest at the G2/M phase of the cell cycle and apoptotic cell death [1] [2].

Purity: >98% Purity: 99.97% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 500 mg

www.MedChemExpress.com 97

Parbendazole PBOX 6 (SKF 29044) Cat. No.: HY-115364 Cat. No.: HY-U00446

Bioactivity: Parbendazole is a potent inhibitor of microtubule assembly, Bioactivity: PBOX 6 is a pyrrolo-1,5-benzoxazepine (PBOX) compound, acts as a microtubule-depolymerizing agent and an apoptotic agent. destabilizes tubulin, with an EC50 of 8.79nM, and exhibits a broad-spectrum anthelmintic activity.

Purity: 98.0% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg 10 mg, 25 mg, 50 mg, 100 mg

PE859 PF-06380101 Cat. No.: HY-12662 Cat. No.: HY-12522

Bioactivity: PE859 is a potent inhibitor of both tau and Aβ aggregation Bioactivity: PF-06380101 is a novel cytotoxic Dolastatin 10 analogue; with excellent potencies in tumor cell proliferation assays and with IC50 values of 0.66 and 1.2 μM, respectively. differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs. IC50 value: ~0.2 nM(GI50 in BT474, MDA-MB-361-DYT2 and N87… Purity: 98.01% Purity: 99.68% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg

Plinabulin Podofilox (NPI-2358) Cat. No.: HY-14444 (Podophyllotoxin) Cat. No.: HY-15552

Bioactivity: Plinabulin (NPI-2358) is a vascular disrupting agents (VDA) Bioactivity: Podofilox (Podophyllotoxin) is a potent inhibitor of against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor microtubule assembly and DNA topoisomerase II. cells. IC50 Value: 9.8~18 nM Target: Microtubule/Tubulin in vitro: NPI-2358 binds to the colchicine-binding site of tubulin and has potent inhibitory to human tumor cell lines… Purity: 93.44% Purity: 99.79% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 100 mg, 500 mg

Rosabulin Soblidotin (STA 5312) Cat. No.: HY-14934 (Auristatin PE; TZT-1027) Cat. No.: HY-14672

Bioactivity: Rosabulin is a potent microtubule inhibitor, with Bioactivity: Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10 anti-cancer activities. derivative and inhibitor of tubulin polymerization.

Purity: >98% Purity: 99.76% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

SSE15206 Taltobulin Cat. No.: HY-111425 (HTI-286; SPA-110) Cat. No.: HY-15584

Bioactivity: SSE15206 is a microtubule polymerization inhibitor (GI 50 Bioactivity: Taltobulin (HTI-286; SPA-110) is an analogue of Hemiasterlin; = 197 nM in HCT116 cells) that overcomes multidrug resistance. potent tubulin inhibitor; ADCs cytotoxin. IC50 value: Target: Causes aberrant mitosis resulting in G2/M arrest due to tubulin in vitro: HTI-286 significantly inhibited proliferation of all three hepatic tumor cell lines (mean IC50 incomplete spindle formation in cancer cells [1]. = 2 nmol/L +/- 1 nmol/L) in vitro. Interestingly, no decrease… Purity: 99.74% Purity: 99.90% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

98 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Taltobulin hydrochloride Taltobulin trifluoroacetate (HTI-286 hydrochloride; SPA-110 hydrochloride) Cat. No.: HY-15584B (HTI-286 trifluoroacetate; SPA-110 trifluoroacetate) Cat. No.: HY-15584A

Bioactivity: Taltobulin hydrochloride is an analogue of Hemiasterlin; Bioactivity: Taltobulin trifluoroacetate (HTI-286; SPA-110) is an analogue potent tubulin inhibitor; ADCs cytotoxin. IC50 value: Target: of Hemiasterlin; potent tubulin inhibitor; ADCs cytotoxin. tubulin in vitro: HTI-286 significantly inhibits proliferation IC50 value: Target: tubulin in vitro: HTI-286 significantly of all three hepatic tumor cell lines (mean IC50 = 2 nmol/L inhibited proliferation of all three hepatic tumor cell lines +/- 1 nmol/L). Interestingly, no decrease in viable primary… (mean IC50 = 2 nmol/L +/- 1 nmol/L) in vitro. Interestingly,… Purity: 99.05% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg

Tasidotin hydrochloride Tirbanibulin (ILX651) Cat. No.: HY-13760 (KX2-391; KX-01) Cat. No.: HY-10340

Bioactivity: Tasidotin hydrochloride is a peptide analog of the antimitotic Bioactivity: Tirbanibulin (KX2-391) is an inhibitor of Src that targets depsipeptide dolastatin 15, as an inhibitor of microtubule the peptide substrate site of Src, with GI50 of 9-60 nM in assembly and microtubule dynamics. cancer cell lines.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

Tirbanibulin dihydrochloride Tirbanibulin Mesylate (KX2-391 (dihydrochloride); KX-01 (dihydrochloride)) Cat. No.: HY-10340A (KX2-391 (Mesylate); KX01 (Mesylate)) Cat. No.: HY-10340B

Bioactivity: Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) is Bioactivity: Tirbanibulin (Mesylate) (KX2-391 (Mesylate)) is an inhibitor an inhibitor of Src that targets the peptide substrate site of Src that targets the peptide substrate site of Src, with

of Src, with GI50 of 9-60 nM in cancer cell lines. GI50 of 9-60 nM in cancer cell lines.

Purity: 96.24% Purity: 99.97% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Triclabendazole Tubulin inhibitor 1 (CGA89317) Cat. No.: HY-B0621 Cat. No.: HY-112607

Bioactivity: Triclabendazole(CGA89317) is a , it binds to Bioactivity: Tubulin inhibitor 1 is a tubulin inhibitor, occupying the tubulin impairing intracellular transport mechanisms and colchicine binding site, inhibits tubulin polymerization. interferes with protein synthesis. Target: Microtubule/Tubulin Tubulin inhibitor 1 shows potent anti-tumor activity, casues Triclabendazole treatment produces percentage decreases of the cellular mitotic arrest in the G2/M phase, and induces fluke egg output by 15.3%, 4.3% and 36.6%, respectively, in… cellular apoptosis [1]. Purity: 98.38% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

Tubulysin A Valecobulin (TubA) Cat. No.: HY-15995 (CKD-516) Cat. No.: HY-13598

Bioactivity: Tubulysin A(TubA) is a myxobacterial product that can function Bioactivity: Valecobulin (CKD516), a valine prodrug of (S516) and a as an antiangiogenic agent in many in vitro assays; vascular disrupting agent (VDA), is a potent beta-tubulin anti-microtubule, anti-mitotic, an apoptosis inducer, polymerization inhibitor with marked antitumor activity anticancer, anti-angiogenic, and antiproliferative. IC50 against murine and human solid tumors [1] [2]. value: Target: microtubule Tubulysin A is a novel antibiotic,… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg Size: 250 mg, 500 mg

www.MedChemExpress.com 99

Vc-MMAD VcMMAE Cat. No.: HY-15742 (mc-vc-PAB-MMAE) Cat. No.: HY-15575

Bioactivity: Vc-MMAD consists the ADCs linker(Val-Cit) and potent tubulin Bioactivity: VcMMAE is a drug-linker conjugate for ADC with potent inhibitor (MMAD), Vc-MMAD is an antibody drug conjugate. IC50 antitumor activity by using the anti-mitotic agent, monomethyl Valu: N/A Target: tubulin; ADCs Monomethyl auristatin D auristatin E (MMAE), linked via the lysosomally cleavable (MMAD), a potent tubulin inhibitor, is a toxin payload and dipeptide, valine-citrulline (vc). antibody drug conjugate. For comparison purposes, the ADC A1… Purity: >98% Purity: 99.89% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Vinblastine sulfate sulfate (Vincaleukoblastine sulfate salt) Cat. No.: HY-13780 (Leurocristine sulfate; 22-Oxovincaleukoblastine sulfate) Cat. No.: HY-N0488

Bioactivity: Vinblastine sulfate is a cytotoxic used against Bioactivity: Vincristine sulfate is an antitumor which various cancer types. Vinblastine sulfate inhibits the inhibits microtubule formation in mitotic spindle,

formation of microtubule and suppresses nAChR with an IC50 of resulting in an arrest of dividing cells at the metaphase 8.9 μM. stage. It binds to microtubule with a Ki of 85 nM.

Purity: 99.87% Purity: 99.66% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg, 100 mg, 200 mg 5 mg, 10 mg, 50 mg, 100 mg

Vinflunine Tartrate Cat. No.: HY-B0628 Cat. No.: HY-B0628A

Bioactivity: Vinflunine is a new vinca alkaloid uniquely fluorinated with Bioactivity: Vinflunine Tartrat is a new vinca alkaloid uniquely the properties of mitotic-arresting and tubulin-interacting fluorinated with the properties of mitotic-arresting and activity. tubulin-interacting activity. Target: Microtubule/Tubulin The major effects of Vinflunine on dynamic instability are a slowing of the microtubule growth rate, an increase in growth… Purity: >98% Purity: 99.14% Clinical Data: Launched Clinical Data: Launched Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

Vinorelbine ditartrate (KW-2307 base) Cat. No.: HY-12053 (KW-2307; Nor-5'-anhydrovinblastine ditartrate) Cat. No.: HY-12053A

Bioactivity: Vinorelbine is an anti-mitotic agent which inhibits the Bioactivity: Vinorelbine (ditartrate) is an anti-mitotic agent which

proliferation of Hela cells with IC 50 of 1.25 nM. inhibits the proliferation of Hela cells with IC 50 of 1.25 nM.

Purity: >98% Purity: 99.58% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

100 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Mps1 Monopolar spindle 1

Monopolar spindle 1 (Mps1), also known as TTK, is a serine threonine kinase, which ensures proper biorientation of sister chromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC). Mps1 has been shown to function as the key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughter cells. Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and for maintaining the spindle assembly checkpoint until all chromosomes are properly attached. Mps1 is expressed at high levels during mitosis and is abundantly expressed in cancer cells. Disruption of Mps1 function induces aneuploidy and cell death.

www.MedChemExpress.com 101 Mps1 Inhibitors & Modulators

AZ3146 BAY1217389 Cat. No.: HY-14710 Cat. No.: HY-12859

Bioactivity: AZ3146 is a reasonably potent and selective Mps1 inhibitor Bioactivity: BAY 1217389 is a potent, and selective inhibitor of the Cat monopolar spindle 1 ( MPS1) kinase with an IC value less with IC50 of 35 nM for Mps1 . 50 than 10 nM.

Purity: 99.92% Purity: 99.94% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg

BOS-172722 CCT251455 Cat. No.: HY-112162 Cat. No.: HY-12603

Bioactivity: BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1) Bioactivity: CCT251455 is a potent and selective mitotic kinase monopolar spindle 1 ( MPS1) inhibitor with an IC of 3 nM. checkpoint with an IC50 of 2 nM. 50

Purity: 99.41% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

CFI-402257 CFI-402257 hydrochloride Cat. No.: HY-101340 Cat. No.: HY-101340A

Bioactivity: CFI-402257 is a highly selective and orally bioavailable Bioactivity: CFI-402257 hydrochloride is a highly selective and orally

TTK/Mps1 inhibitor with an IC50 of 1.7 nM for TTK in vitro. bioavailable TTK/Mps1 inhibitor with an IC50 of 1.7 nM for CFI-402257 has anti-cancer activity [1]. TTK in vitro. CFI-402257 hydrochloride has anti-cancer activity [1]. Purity: 99.52% Purity: 99.48% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Empesertib MPI-0479605 (BAY 1161909) Cat. No.: HY-12858 Cat. No.: HY-12660

Bioactivity: Empesertib (BAY 1161909) is a potent Mps1 inhibitor, with Bioactivity: MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC of 1.8 nM. an IC50 of < 1 nM. 50

Purity: 98.0% Purity: 99.85% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 2 mg, 5 mg, 10 mg, 50 mg

Mps1-IN-1 Mps1-IN-2 Cat. No.: HY-13298 Cat. No.: HY-13994

Bioactivity: Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 Bioactivity: Mps1-IN-2 is a potent, selective and ATP-competitive dual

kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM. Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and

12 nM for Mps1 and a Kd of 61 nM for Plk1.

Purity: 99.66% Purity: 98.06% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

102 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Mps1-IN-3 NMS-P715 Cat. No.: HY-12401 Cat. No.: HY-12382

Bioactivity: Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, Bioactivity: NMS-P715 is a selective, ATP-competitive inhibitor of MPS1,

with an IC50 of 50 nM. with an IC50 of 182 nM.

Purity: 98.0% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

NMS-P715 analog Cat. No.: HY-14712

Bioactivity: NMS-P715 analog is an inhibitor of MPS1, with an IC50 of 84 nM.

Purity: >98% Clinical Data: No Development Reported Size: 5 mg

www.MedChemExpress.com 103 Nucleoside Antimetabolite/Analog

Nucleoside analogues are molecules that act like in DNA synthesis. They include a range of antiviral products used to prevent viral replication in infected cells. Nucleoside analogues can be used against hepatitis B virus, hepatitis C virus, herpes simplex, and HIV. Once they are phosphorylated, they work as by being similar enough to nucleotidesto be incorporated into growing DNA strands. Less selective nucleoside analogues are used as chemotherapy agents to treat cancer, eg gemcitabine and 5-FU. Antimetabolite is a chemical that inhibits the use of a metabolite, which is another chemical that is part of normal metabolism. Such substances are often similar in structure to the metabolite that they interfere with, such as the antifolates that interfere with the use of folic acid. The presence of antimetabolites can have toxic effects on cells, such as halting cell growth and cell division, so these compounds are used as chemotherapy for cancer.

104 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Nucleoside Antimetabolite/Analog Inhibitors & Modulators

1-(2'-O-4-C-Methylene-beta-D-ribofuranosyl) 1-Methylcytosine Cat. No.: HY-111638 Cat. No.: HY-W006395

Bioactivity: 1-(2'-O-4-C-Methylene-beta-D-ribofuranosyl)thymine is a Bioactivity: 1-Methylcytosine is a methylated form of the DNA base cytosine bicyclic nucleoside. and used as a nucleobase of hachimoji DNA, in which it pairs with Isoguanine [1] [2].

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 50 mg Size: 50 mg

1-Methylinosine 2'-Deoxypseudoisocytidine (N1-Methylinosine) Cat. No.: HY-113139 Cat. No.: HY-101968

Bioactivity: 1-Methylinosine is a modified nucleotide found at position 37 Bioactivity: 2'-Deoxypseudoisocytidine is a nucleoside analogue. in tRNA 3' to the anticodon of eukaryotic tRNA [1].

Purity: 99.96% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

2’-O,4’-C-Methyleneuridine 3'-Azido-3'-deoxy-5-fluorocytidine Cat. No.: HY-111639 Cat. No.: HY-111641

Bioactivity: 2’-O,4’-C-Methyleneuridine (Compound 15a) is a bicyclic Bioactivity: 3'-Azido-3'-deoxy-5-fluorocytidine (Compound 12) is a nucleoside. derivative.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 10 mg, 50 mg

3'-Azido-3'-deoxy-beta-L- 3-Methylcytidine Cat. No.: HY-111642 Cat. No.: HY-111645

Bioactivity: 3'-Azido-3'-deoxy-beta-L-uridine (Compound 25) is a nucleoside Bioactivity: 3-Methylcytidine, a urinary nucleoside, can be used as a derivative. biomarker of four different types of cancer: , gastric cancer, colon cancer, and breast cancer [1].

Purity: 99.70% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg 10 mg, 50 mg

5'-O-(4,4'-Dimethoxytrityl)-2'-O,4'-C-methylene-5-methylurid 5-Aza-7-deazaguanine ine Cat. No.: HY-111807 Cat. No.: HY-111627 Bioactivity: 5'-O-(4,4'-Dimethoxytrityl)-2'-O,4'-C-methylene-5-methyluridin Bioactivity: 5-Aza-7-deazaguanine is a substrate for wild-type (WT) E. coli e is a derivative of LNA-type nucleoside. purine nucleoside phosphorylase and its Ser90Ala mutant in the synthesis of base-modified nucleosides [1].

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 500 mg, 100 mg, 250 mg

www.MedChemExpress.com 105

5-Azacytidine 5-BrdU (Ladakamycin; 5-AzaC; ) Cat. No.: HY-10586 (BUdR; BRDU) Cat. No.: HY-15910

Bioactivity: 5-Azacytidine is a nucleoside analogue of cytidine that Bioactivity: 5-BrdU is a nucleoside analog that competes with thymidine for specifically inhibits DNA methylation by trapping DNA incorporation into DNA. 5-BrdU is commonly used in the methyltransferases. detection of proliferating cells.

Purity: 99.97% Purity: 99.99% Clinical Data: Launched Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 200 mg, 500 mg 100 mg, 500 mg, 1 g, 5 g

5- 6-Amino-5-nitropyridin-2-one (5-FU) Cat. No.: HY-90006 Cat. No.: HY-50071

Bioactivity: 5-Fluorouracil is a potent antitumor agent that affects Bioactivity: 6-Amino-5-nitropyridin-2-one is a pyridine base and used as a pyrimidine synthesis by inhibiting thymidylate synthetase nucleobase of hachimoji DNA, in which it pairs with thus depleting intracellular dTTP pools. 5-aza-7-deazaguanine [1].

Purity: 99.86% Purity: 95.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 1 g, 5 g 50 mg

6- 6-Mercaptopurine hydrate (Mercaptopurine; 6-MP) Cat. No.: HY-13677 (Mercaptopurine hydrate; 6-MP hydrate) Cat. No.: HY-13677A

Bioactivity: 6-Mercaptopurine is a which acts as an Bioactivity: 6-Mercaptopurine hydrate (Mercaptopurine hydrate; 6-MP antagonist of the endogenous and has been widely used hydrate) is a purine analogue which acts as an antagonist of as antileukemic agent and immunosuppressive drug. the endogenous purines and has been widely used as antileukemic agent and immunosuppressive drug.

Purity: 96.0% Purity: 98.74% Clinical Data: Launched Clinical Data: Phase 4 Size: 50 mg, 100 mg, 500 mg Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 500 mg

6-O-Methyl 7-Methylguanosine Cat. No.: HY-111648 Cat. No.: HY-122524

Bioactivity: 6-O-Methyl Guanosine is a modified nucleoside [1]. 6-O-Methyl Bioactivity: 7-Methylguanosine is a novel cNIIIB nucleotidase inhibitor Guanosine (6-methylguanosine) inhibit colony-forming ability with IC 50 value of 87.8 ± 7.5 µM. in a malignant xeroderma pigmentosum cell line [2].

Purity: 99.86% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 50 mg 50 mg

8-Azaguanine Adenosine Cat. No.: HY-B1468 (Adenine riboside; D-Adenosine) Cat. No.: HY-B0228

Bioactivity: 8-Azaguanine is a purine analogue which shows antineoplastic Bioactivity: Adenosine is a nucleoside composed of a molecule of adenine activity. attached to a ribose sugar molecule (ribofuranose) moiety via a β-N9-glycosidic bond. Target: Nucleoside antimetabolite/analog Adenosine plays an important role in biochemical processes, such as energy transfer — as adenosine… Purity: 98.0% Purity: 99.84% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 1 g, 5 g

106 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Capecitabine Cat. No.: HY-B0016 (HCFU) Cat. No.: HY-B0182

Bioactivity: Capecitabine is an oral prodrug that is converted to its Bioactivity: Carmofur is a derivative of fluorouracil, an antimetabolite active metabolite, 5-FU, by thymidine phosphorylase. used as an antineoplastic agent.

Purity: 99.97% Purity: 99.95% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 100 mg, 500 mg

Clofarabine CNDAC Cat. No.: HY-A0005 Cat. No.: HY-16445A

Bioactivity: (Clolar; Clofarex) inhibits the enzymatic Bioactivity: CNDAC is a major metabolite of oral drug , and a activities of ribonucleotide reductase (IC50 = 65 nM) and DNA nucleoside analog. polymerase. IC50 Value: 65 nM Target: in vitro: Clofarabine is a second generation purine nucleoside analog with antineoplastic activity. It is phosphorylated intracellularly,… Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg 10 mg, 50 mg

Cytarabine (Cytosine β-D-arabinofuranoside; Cytosine Cytarabine hydrochloride (Cytosine β-D-arabinofuranoside Arabinoside; Ara-C) Cat. No.: HY-13605 hydrochloride; Cytosine Arabinoside hydrochloride; …) Cat. No.: HY-13605A

Bioactivity: Cytarabine, a nucleoside analog, causes S phase cell cycle Bioactivity: Cytarabine hydrochloride, a nucleoside analog, causes S phase arrest and inhibits DNA polymerase. Cytarabine inhibits cell cycle arrest and inhibits DNA polymerase. Cytarabine

DNA synthesis with an IC50 of 16 nM. inhibits DNA synthesis with an IC50 of 16 nM.

Purity: 99.99% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 500 mg 100 mg, 500 mg, 1 g

Cytidine (Cytosine β-D-riboside; Cytosine-1-β-D-ribofuranoside) Cat. No.: HY-B0158 (Imidazole Carboxamide) Cat. No.: HY-B0078

Bioactivity: Cytidine is a nucleoside molecule that is formed when cytosine Bioactivity: Dacarbazine(DTIC-Dome; DTIC) is an antineoplastic agent. It is attached to a ribose ring, cytidine is a component of RNA. has significant activity against . Target: Nucleoside Target: Nucleoside antimetabolite/analog Cytidine is a antimetabolite/analog Approved: May 1975 Dacarbazine (DTIC) is nucleoside molecule that is formed when cytosine is attached the only single-agent approved by the Food and Drug to a ribose ring (also known as a ribofuranose) via a… Administration for treating metastatic melanoma. With DTIC as… Purity: 98.97% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 200 mg, 1 g

Deoxycytidine triphosphate Deoxypseudouridine (dCTP) Cat. No.: HY-101400 Cat. No.: HY-101970

Bioactivity: Deoxycytidine triphosphate (dCTP), a nucleoside triphosphate, Bioactivity: Deoxypseudouridine is a nucleotide analog. is a raw material in DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.

Purity: 98.15% Purity: 98.18% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

www.MedChemExpress.com 107

DMTr-LNA-5MeU-3-CED-phosphoramidite Doxifluridine Cat. No.: HY-111531 (Ro 21-9738; 5-Fluoro-5'-deoxyuridine; 5'-DFUR) Cat. No.: HY-B0021

Bioactivity: DMTr-LNA-5MeU-3-CED-phosphoramidite is a nucleoside derivative Bioactivity: Doxifluridine is a thymidine phosphorylase activator for [1]. PC9-DPE2 cells with IC50 of 0.62 μM.

Purity: >98% Purity: 99.91% Clinical Data: No Development Reported Clinical Data: Launched Size: 50 mg Size: 10mM x 1mL in Water, 1 g, 5 g

Ethynylcytidine (ECyD; TAS-106; 3'-C-Ethynylcytidine) Cat. No.: HY-16200 (5-Fluorouracil 2'-deoxyriboside) Cat. No.: HY-B0097

Bioactivity: Ethynylcytidine is a new nucleoside antimetabolite. Bioactivity: Floxuridine (5-fluorodeoxyuridine) is an oncology drug that belongs to the class known as antimetabolites with an GI50 of 5.1 μM for the inhibition of PEPT1. IC50 value: Target: Nucleoside antimetabolite/analog Floxuridine (Fludara) is a prodrug of floxuridine and an oncology agent with an GI50 of… Purity: 99.52% Purity: 99.93% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg 100 mg, 200 mg, 500 mg

Fludarabine Fludarabine phosphate (F-ara-A; NSC 118218) Cat. No.: HY-B0069 (NSC 118218 (phosphate)) Cat. No.: HY-B0028

Bioactivity: Fludarabine (NSC 118218) is a DNA synthesis inhibitor, which Bioactivity: Fludarabine (phosphate) is an analogue of adenosine and also inhibits phosphorylation of STAT1. deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.

Purity: 99.28% Purity: 99.69% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 10 mg, 50 mg, 100 mg

Forodesine hydrochloride (BCX-1777 freebase; Immucillin-H) Cat. No.: HY-16210 (BCX-1777; Immucillin-H hydrochloride) Cat. No.: HY-16209

Bioactivity: Forodesine(BCX-1777 freebase; Immucillin-H) is an orally Bioactivity: Forodesine hydrochloride is a potent and oral purine nucleoside bioavailable PNP inhibitor with picomolar potency; induces phosphorylase (PNP) inhibitor with IC50s ranging from 0.48 to apoptosis, mainly in T cells. 1.57 nM.

Purity: >98% Purity: 99.86% Clinical Data: Launched Clinical Data: Launched Size: 2500u g, 5 mg, 10 mg Size: 10mM x 1mL in Water, 1000u g, 2500u g, 5 mg, 10 mg

Fosteabine Gemcitabine (Cytarabine ocfosfate; YNK 01) Cat. No.: HY-106349 (NSC 613327; LY188011) Cat. No.: HY-17026

Bioactivity: Fosteabine is an oral and prodrug analogue of cytarabine which Bioactivity: Gemcitabine (NSC 613327;LY188011) is a DNA synthesis inhibitor is resistant to deoxycytidine deaminase. which inhibits the growth of BxPC-3, Mia Paca-2, PANC-1, PL-45

and AsPC-1 cells with IC50s of 37.6, 42.9, 92.7, 89.3 and 131.4 nM, respectively.

Purity: >98% Purity: 99.92% Clinical Data: No Development Reported Clinical Data: Launched Size: 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 100 mg, 200 mg, 500 mg, 1 g

108 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Gemcitabine elaidate Gemcitabine Hydrochloride (CP-4126; CO-101; Gemcitabine 5'-elaidate) Cat. No.: HY-13538 (LY 188011 hydrochloride) Cat. No.: HY-B0003

Bioactivity: Gemcitabine elaidate(CP-4126; CO-101) is a lipophilic, Bioactivity: Gemcitabine hydrochloride is a DNA synthesis inhibitor with unsaturated fatty acid ester derivative of gemcitabine (dFdC), IC50s of 37.6, 42.9, 92.7, 89.3 and 131.4 nM in BxPC-3, Mia an antimetabolite deoxynucleoside analogue, with potential Paca-2, PANC-1, PL-45 and AsPC-1 cells, respectively. antineoplastic activity. IC50 value: Target: Gemcitabine analog Upon hydrolysis intracellularly by esterases, the… Purity: 99.24% Purity: 99.93% Clinical Data: Phase 2 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg 100 mg, 200 mg, 500 mg, 1 g

Isocytosine Isoguanine Cat. No.: HY-W002272 Cat. No.: HY-124143

Bioactivity: Isocytosine is a non-natural nucleobase and an isomer of Bioactivity: Isoguanine is a purine base that is an isomer of guanine. A cytosine. It is used in combination with Isoguanine in studies building block in organic synthesis. of unnatural nucleic acid analogues of the normal base pairs in DNA and used as a nucleobase of hachimoji RNA [1] [2].

Purity: 99.62% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 100 mg, 250 mg, 500 mg 100 mg

LY2334737 N2-Methylguanosine Cat. No.: HY-13672 Cat. No.: HY-111647

Bioactivity: LY2334737 is an orally available prodrug of gemcitabine which Bioactivity: N2-methylguanosine is a modified nucleoside that occurs at is a nucleoside analog used as chemotherapy. several specific locations in many tRNA's.

Purity: 98.29% Purity: >98% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg 5 mg, 10 mg, 50 mg, 100 mg

N6,N6-Dimethyladenosine N6-Etheno 2'-deoxyadenosine Cat. No.: HY-101984 Cat. No.: HY-111646

Bioactivity: N6,N6-Dimethyladenosine is a modified ribonucleoside Bioactivity: N6-Etheno 2'-deoxyadenosine is a reactive oxygen species previously found in rRNA, and also exhibits in mycobacterium (ROS)/reactive nitrogen species (RNS)-induced DNA oxidation bovis Bacille Calmette-Guérin tRNA [1]. product, used as a biomarker to evaluate chronic inflammation and lipid peroxidation in animal or human tissues [1].

Purity: 99.71% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg 50 mg

Nelarabine Orotic acid (506U78; GW 506U78; Nelzarabine) Cat. No.: HY-13701 (6-Carboxyuracil; Vitamin B13) Cat. No.: HY-N0157

Bioactivity: (Arranon, 506U78) is a purine nucleoside analog and Bioactivity: Orotic acid (OA) is an intermediate in pyrimidine metabolism. DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor IC50 Value: Target: Nucleoside antimetabolite/analog in vitro: cells. Nelarabine is a chemotherapy drug used in T-cell acute OA increases cell proliferation and decreases apoptosis in lymphoblastic leukemia. serum-starved SK-Hep1 hepatocellular carcinoma cells, which may ascribe to the inhibition of AMP-activated protein kinase… Purity: 99.76% Purity: 95.75% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 100 mg, 500 mg

www.MedChemExpress.com 109

Pseudothymidine Raltitrexed (5-Methyl-2'-Deoxypseudouridin) Cat. No.: HY-101969 (ZD1694; D1694; ICI-D1694) Cat. No.: HY-10821

Bioactivity: Pseudothymidine is a C-nucleoside analog of thymidine. Bioactivity: Raltitrexed is an antimetabolite drug used in chemotherapy, acting by inhibiting thymidylate synthase.

Purity: 99.85% Purity: 99.21% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

RX-3117 Sapacitabine (TV-1360; fluorocyclopentenylcytosine) Cat. No.: HY-15228 (CS682; CYC682) Cat. No.: HY-16445

Bioactivity: RX-3117(TV-1360; Fluorocyclopentenylcytosine) is novel a Bioactivity: Sapacitabine is an orally available nucleoside analog prodrug cytidine analog; shows anticancer activity in several cancer that is structurally related to cytarabine. cell lines, including gemcitabine-resistant variants.

Purity: 97.45% Purity: 98.87% Clinical Data: Phase 2 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Tegafur Tipiracil (FT 207NSC 148958) Cat. No.: HY-17400 Cat. No.: HY-A0063A

Bioactivity: (FT 207; NSC 148958) is a chemotherapeutic 5-FU Bioactivity: Tipiracil is a thymidine phosphorylase ( TPase) inhibitor. prodrug used in the treatment of cancers; is a component of tegafur-.

Purity: 99.95% Purity: 97.83% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 100 mg, 500 mg

Tipiracil hydrochloride Trifluridine Cat. No.: HY-A0063 (Trifluorothymidine; 5-Trifluorothymidine; TFT) Cat. No.: HY-A0061

Bioactivity: Tipiracil (hydrochloride) is a thymidine phosphorylase Bioactivity: Trifluridine (Trifluorothymidine; 5-Trifluorothymidine; TFT) inhibitor (TPI), used for cancer research. is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral drug for herpes simplex virus (HSV) infection.

Purity: 99.99% Purity: 99.69% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg 50 mg, 100 mg, 200 mg

Trifluridine/tipiracil hydrochloride mixture Vidarabine (Ara-A; Adenine Arabinoside; (TAS-102) Cat. No.: HY-16478 9-β-D-Arabinofuranosyladenine) Cat. No.: HY-B0277

Bioactivity: Trifluridine-tipiracil hydrochloride mixture (TAS-102) is a Bioactivity: Vidarabine (Ara-A) an antiviral drug which is active against novel oral combination drug that consists of an antineoplastic herpes simplex and varicella zoster viruses. thymidine-based nucleoside analog, trifluorothymidine, and a potent thymidine phosphorylase inhibitor, tipiracil, in a 1:0.5 molar ratio. Purity: 99.72% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 100 mg, 200 mg, 500 mg

110 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] p97 VCP;Cdc48

p97, an abundant hexameric ATPase of the AAA family, is involved in homotypic membrane fusion. It is thought to disassemble SNARE complexes formed during the process of membrane fusion. Two structures have been reported: a crystal structure of the N-terminal and D1 ATPase domains of murine p97 at 2.9 A resolution, and a cryoelectron microscopy structure of full-length rat p97 at 18 A resolution. Together, these structures show that the D1 and D2 hexamers pack in a tail-to-tail arrangement, and that the N domain is flexible. A comparison with NSF D2 (ATP complex) reveals possible conformational changes induced by ATP hydrolysis.

www.MedChemExpress.com 111 p97 Inhibitors & Modulators

CB-5083 DBeQ Cat. No.: HY-12861 (JRF 12) Cat. No.: HY-15945

Bioactivity: CB-5083 is a potent, selective and orally bioavailable p97 Bioactivity: DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC value of 1.5 μM and 1.6 μM for inhibitor with an IC50 value of 11 nM. 50 p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4

with an IC50 of 11.5 μM. Purity: 99.95% Purity: 98.84% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

ML240 ML241 hydrochloride Cat. No.: HY-19795 Cat. No.: HY-19797A

Bioactivity: ML240 is a potent p97 inhibitor, inhibiting p97 ATPase with Bioactivity: ML241 hydrochloride is a potent p97 inhibitor, inhibiting p97

IC50 value of 100 nM. ATPase with IC50 value of 100 nM.

Purity: 99.76% Purity: 99.86% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

NMS-859 NMS-873 Cat. No.: HY-15714 Cat. No.: HY-15713

Bioactivity: NMS-859 is a potent, covalent VCP (p97) inhibitor, with Bioactivity: NMS-873 is a potent, selective allosteric VCP/p97 inhibitor

IC50s of 0.37 and 0.36 μM for wild-type VCP in the presence of with IC50 value of 30 nM. 60 μM and 1 mM ATP in cells, respectively.

Purity: 97.65% Purity: 99.93% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

112 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] PAK p21 activated kinases

PAKs (p21-activated kinases) are key regulators of actin dynamics, cell proliferation and cell survival. PAKs are Ser/Thr kinases that are classified into two groups on the basis of their structural and functional features: group I (PAK1–3) and group II (PAK4–6). Group I PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain, CD) and are activated by the binding of the active (that is, GTP-bound) forms of Rho GTPases, such as Cdc42 and Rac1. Group II PAKs have no auto-inhibitory domains and are not activated by active Rho GTPases. Because the deregulation of PAKs is closely associated with various human diseases,small-molecule inhibitors of these kinases have great potential as therapeutic agents. In addition, these compounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway. PAKs are considered prime regulators of the actin cytoskeleton and motility. Due to their central role in actin remodelling and their ability to activate Matrix metalloproteinases (MMPs), Rho GTPases play an important role in tumor cell invasion and metastasis. The current evidence suggests the involvement of PAKs in motility, cell survival, anchorage-independent growth, angiogenesis, invasion, migration and regulation of cell cycle and mitosis. Consequently, PAKs have also been implicated in a number of pathological conditions including cancer.

www.MedChemExpress.com 113 PAK Inhibitors & Modulators

5-Aminosalicylic Acid Fingolimod (Mesalamine; 5-ASA; Mesalazine) Cat. No.: HY-15027 (FTY720 free base) Cat. No.: HY-11063

Bioactivity: 5-Aminosalicylic acid acts as a specific PPARγ agonist and Bioactivity: Fingolimod is a sphingosine 1-phosphate ( S1P) antagonist

also inhibits p21-activated kinase 1 ( PAK1) and NF-κB. with IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator.

Purity: 98.0% Purity: 99.95% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 g 5 mg, 10 mg

Fingolimod hydrochloride FRAX1036 (FTY720) Cat. No.: HY-12005 Cat. No.: HY-19538

Bioactivity: Fingolimod hydrochloride is a sphingosine 1-phosphate ( S1P) Bioactivity: FRAX1036 is a PAK inhibitor with Kis of 23.3 nM, 72.4 nM, and antagonist with an IC of 0.033 nM in K562 and NK cells. 50 2.4 μM for PAK1, PAK2 and PAK4, respectively. Fingolimod hydrochloride also is a pak1 activator.

Purity: 99.76% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 200 mg, 1 g, 5 g 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

FRAX486 FRAX597 Cat. No.: HY-15542B Cat. No.: HY-15542A

Bioactivity: FRAX486 is a p21-activated kinase ( PAK) inhibitor with IC50s Bioactivity: FRAX597 is a potent group I p21-activated Kinases ( PAKs) inhibitor with IC of 8, 13 and 19 nM for PAK1, 2 and 3. of 14, 33 and 39 nM for PAK1, PAK2 and PAK3, respectively. 50

Purity: 98.0% Purity: 99.02% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

G-5555 G-5555 hydrochloride Cat. No.: HY-19635 Cat. No.: HY-19635A

Bioactivity: G-5555 is a potent p21-activated kinase 1 ( PAK1) inhibitor Bioactivity: G-5555 hydrochloride is a potent and selective p21-activated kinase 1 ( PAK1) inhibitor with a K of 3.7 nM. with Kis of 3.7 nM and 11 nM for PAK1 and PAK2, respectively. i

Purity: 99.18% Purity: 98.19% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 25 mg

IPA-3 NVS-PAK1-1 Cat. No.: HY-15663 Cat. No.: HY-100519

Bioactivity: IPA-3 is a selective non-ATP competitive PAK1 inhibitor with Bioactivity: NVS-PAK1-1 is a potent and selective allosteric PAK1

IC50 of 2.5 μM, and shows no inhibition to group II PAKs (PAKs inhibitor with an IC50 of 5 nM. 4-6).

Purity: 98.0% Purity: 99.82% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

114 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

PAK-IN-1 PF-3758309 Cat. No.: HY-12632 Cat. No.: HY-13007

Bioactivity: PAK-IN-1 is a PAK inhibitor that displays group II Bioactivity: PF-3758309 is an inhbitor of PAK with IC50 of 1.3 nM for selectivity. PAK-IN-1 inhibits PAK4, PAK5 and PAK6 with IC s 50 PAK4. of 7.5, 36, 126 nM, respectively.

Purity: >98% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 115 PARP poly ADP ribose polymerase

PARP is a family of proteins involved in a number of cellular processes involving mainly DNA repair and . The PARP family comprises 17 members. They have all very different structures and functions in the cell. PARP1, PARP2, VPARP (PARP4), Tankyrase-1 and -2 (PARP-5a or TNKS, and PARP-5b or TNKS2) have a confirmed PARP activity. Others include PARP3, PARP6, TIPARP (or PARP7), PARP8, PARP9, PARP10, PARP11, PARP12, PARP14, PARP15, and PARP16. PARP is found in the cell’s nucleus. The main role is to detect and signal single-strand DNA breaks (SSB) to the enzymatic machinery involved in the SSB repair.

116 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] PARP Inhibitors & Modulators

3-Aminobenzamide A-966492 (PARP-IN-1) Cat. No.: HY-12022 Cat. No.: HY-10614

Bioactivity: 3-Aminobenzamide is a potent inhibitor of Bioactivity: A-966492 is a novel and potent inhibitor of

PARP with IC50 of appr 50 nM in CHO cells, PARP1 and PARP2 with Ki of 1 nM and and acts as a mediator of oxidant-induced myocyte dysfunction 1.5 nM, respectively. during reperfusion.

Purity: 99.92% Purity: 98.59% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 200 mg, 500 mg 5 mg, 10 mg, 50 mg

AG14361 AZ6102 Cat. No.: HY-12032 Cat. No.: HY-12975

Bioactivity: AG14361 is a potent PARP-1 inhibitor, with a Ki of < 5 nM, Bioactivity: AZ6102 is a potent dual TNKS1 and TNKS2 inhibitor, with IC50s of 3 nM and 1 nM, respectively, and alao has 100-fold and in permeabilized SW620 and intact SW620 cells, the IC50s selectivity against other PARP family enzymes, with IC s of are 29 nM and 14 nM, respectively. 50 2.0 μM, 0.5 μM, and >3 μM, for PARP1, PARP2, and PAR… Purity: 99.41% Purity: 99.65% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

AZD-2461 BGP-15 Cat. No.: HY-13536 Cat. No.: HY-100828

Bioactivity: AZD-2461 is a potent PARP inhibitor, with IC50s of 5 nM, 2 nM Bioactivity: BGP-15 is a PARP inhibitor, with an IC50 and a Ki of 120 and and 200 nM for PARP1, PARP2 and PARP3, respectively. 57 μM, respectively.

Purity: 98.39% Purity: 98.0% Clinical Data: Phase 1 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg

BRCA1-IN-1 Dehydrocorydaline Cat. No.: HY-100863 (13-Methylpalmatine) Cat. No.: HY-N0674

Bioactivity: BRCA1-IN-1 is a novel small-molecule-like BRCA1 inhibitor Bioactivity: Dehydrocorydaline (13-Methylpalmatine) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. with IC50 and Ki of 0.53 μM and 0.71 μM, respecrively. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 5 mg, 10 mg, 50 mg

E7449 G007-LK Cat. No.: HY-12418 Cat. No.: HY-12438

Bioactivity: E7449 is a potent PARP1 and PARP2 inhibitor and also Bioactivity: G007-LK is a potent and selective inhibitor of TNKS1 and

inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, 50 and TNKS2, with IC50s of 46 nM and 25 nM, respectively. 50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD + as substrate. Purity: 99.0% Purity: 99.24% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 117

GeA-69 Iniparib Cat. No.: HY-108708 (BSI-201; NSC-746045; IND-71677) Cat. No.: HY-12015

Bioactivity: GeA-69 is a selective, highly cell permeable allosteric Bioactivity: Iniparib (BSI-201) is an irreversible inhibitor of PARP1, inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 used in the research of triple negative breast cancer. [1] (PARP14) targeting macrodomain 2, with a Kd of 2.1 µM .

Purity: >98% Purity: 99.65% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 5 mg, 10 mg, 25 mg, 50 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

JW 55 K-756 Cat. No.: HY-13968 Cat. No.: HY-U00422

Bioactivity: JW 55 is a potent and selective β-catenin signaling pathway Bioactivity: K-756 is a direct and selective tankyrase ( TNKS) inhibitor, inhibitor, which functions via inhibition of the PARP domain which inhibits the ADP-ribosylation activity of TNKS1 and of tankyrase 1 and tankyrase 2 (TNKS1/2). JW 55 decreases TNKS2 with IC50s of 31 and 36 nM, respectively. auto-PARsylation of TNKS1/2 in vitro with IC50s of 1.9 μM and 830 nM respectively. Purity: 99.10% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg

ME0328 MN-64 Cat. No.: HY-100225 Cat. No.: HY-19351

Bioactivity: ME0328 is a potent and selective ARTD3/ PARP3 inhibitor with Bioactivity: MN-64 is a potent tankyrase 1 inhibitor, with IC50s of 6 nM, an IC of 0.89±0.28 μM. 50 72 nM, 19.1 μM, and 39.4 μM for TNKS1, TNKS2, ARTD1 and ARTD2, respectively.

Purity: 99.34% Purity: 98.22% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Niraparib hydrochloride (MK-4827) Cat. No.: HY-10619 (MK-4827 (hydrochloride)) Cat. No.: HY-10619A

Bioactivity: Niraparib (MK-4827) is a highly potent PARP1 and PARP2 Bioactivity: Niraparib hydrochloride (MK-4827 hydrochloride) is an excellent PARP1 and PARP2 inhibitor with IC of 3.8 and 2.1 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. 50 nM, respectively.

Purity: 99.93% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Niraparib R-enantiomer Niraparib tosylate (MK 4827 (R-enantiomer)) Cat. No.: HY-10619D (MK-4827 (tosylate)) Cat. No.: HY-10619B

Bioactivity: Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent Bioactivity: Niraparib tosylate (MK-4827 tosylate) is an excellent PARP1

PARP1 inhibitor with IC50 of 2.4 nM. and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively.

Purity: 98.58% Purity: 99.52% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

118 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

NMS-P118 NMS-P515 Cat. No.: HY-18954 Cat. No.: HY-128599

Bioactivity: NMS-P118 is a potent, orally available, and highly selective Bioactivity: NMS-P515 is a potent and stereospecific PARP-1 inhibitor, PARP-1 Inhibitor for cancer therapy. [1] with an IC50 of 27 nM in hela cells. Anti-tumor activity .

Purity: 99.08% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg, 100 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

NVP-TNKS656 (TNKS656) Cat. No.: HY-13990 (AZD2281; KU0059436) Cat. No.: HY-10162

Bioactivity: NVP-TNKS656 is a highly potent, selective, and orally active Bioactivity: Olaparib (AZD2281;KU0059436) is a potent and oral PARP TNKS2 inhibitor with IC of 6 nM, and is > 300 fold 50 inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, selectivity against PARP1 and PARP2. respectively.

Purity: 99.31% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g, 2 g

Pamiparib PARP-2-IN-1 (BGB-290) Cat. No.: HY-104044 Cat. No.: HY-102035

Bioactivity: Pamiparib is a PARP inhibitor which can be used for the Bioactivity: PARP-2-IN-1 is a potent and selective PARP-2 inhibitor with

treatment of various cancers including the solid tumor, an IC50 of 11.5 nM. extracted from patent WO 2013097225 A1.

Purity: 99.97% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

PJ34 PJ34 hydrochloride Cat. No.: HY-13688A Cat. No.: HY-13688

Bioactivity: PJ34 is a potent specific inhibitor of PARPl/ 2 with IC50 of Bioactivity: PJ34 hydrochloride is an inhibitor of PARPl1/2 with IC50 of 110 110 nM and 86 nM, respectively. nM and 86 nM, respectively.

Purity: 98.0% Purity: 97.68% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in Water, 10 mg, 50 mg, 100 mg

PROTAC PARP1 degrader RK-287107 Cat. No.: HY-114324 Cat. No.: HY-123892

Bioactivity: PROTAC PARP1 degrader is a PARP1 degrader based on the Bioactivity: RK-287107 is a potent and specific tankyrase inhibitor with

PROTAC technology. It induces significant PARP1 cleavage and IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h respectively. RK-287107 blocks cell growth inhibits MDA-MB-231 cell line with an IC of 6.12 μM. 50 [1]. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 100 mg, 250 mg Size: 500 mg, 250 mg

www.MedChemExpress.com 119

Rucaparib Camsylate (AG014699; PF-01367338) Cat. No.: HY-10617A Cat. No.: HY-102003

Bioactivity: Rucaparib (AG014699) is an inhibitor of Bioactivity: Rucaparib Camsylate is an inhibitor of PARP with a Ki of 1.4 PARP with K of 1.4 nM for PARP1 in a i nM for PARP1, and also shows binding affinity to eight other cell-free assay, and also shows binding affinity to eight PARP domains. other PARP domains.

Purity: >98% Purity: 99.81% Clinical Data: Launched Clinical Data: Phase 3 Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Rucaparib phosphate (AG-014699 phosphate; PF-01367338 phosphate) Cat. No.: HY-10617 (BMN-673; LT-673) Cat. No.: HY-16106

Bioactivity: Rucaparib phosphate (AG-014699 phosphate) is a potent and oral Bioactivity: Talazoparib (BMN-673) is a highly potent PARP1/2 inhibitor PARP inhibitor, with a K of 1.4 nM for PARP1 in cell-free i with Kis of 1.2 nM and 0.87 nM, respectively. assay, also showing binding affinity to eight other PARP domains.

Purity: 99.89% Purity: 99.83% Clinical Data: Launched Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

Talazoparib 8R,9S Talazoparib tosylate (BMN-673 (8R,9S); (8R,9S)-LT-673) Cat. No.: HY-16106A (BMN 673ts) Cat. No.: HY-108413

Bioactivity: Talazoparib 8R,9S (BMN-673 8R,9S) is an enantiomer of Bioactivity: Talazoparib tosylate (BMN 673ts) is a novel, potent and orally

Talazoparib, less active than Talazoparib on the inhibition of available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1, with an IC of 144 nM. 50 PARP1.

Purity: 95.08% Purity: 99.74% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg 5 mg, 10 mg, 50 mg

UPF 1069 Cat. No.: HY-14478 (ABT-888) Cat. No.: HY-10129

Bioactivity: UPF 1069 is a PARP inhibitor, with IC50s of 8 and 0.3 μM for Bioactivity: Veliparib is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with K s of 5.2 and 2.9 nM, respectively. PARP-1 and PARP-2, respectively. i

Purity: 98.88% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

Veliparib dihydrochloride WD2000-012547 (ABT-888 dihydrochloride) Cat. No.: HY-10130 Cat. No.: HY-U00223

Bioactivity: Veliparib (dihydrochloride) is a potent inhibitor of Bioactivity: WD2000-012547 is a selective poly(ADP-ribose)-polymerase

PARP1 and PARP2 with Kis of 5.2 (PARP-1) inhibitor with a pK i of 8.221. nM and 2.9 nM in cell-free assays, respectively.

Purity: 99.62% Purity: >98% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

120 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

XAV-939 Cat. No.: HY-15147

Bioactivity: XAV-939 is a tankyrase (TNKS) inhibitor and an indirect

inhibitor of Wnt/β-catenin signaling, with IC50s of 5 and 2 nM for TNKS1 and TNKS2, respectively.

Purity: 98.04% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

www.MedChemExpress.com 121 PERK Protein kinase R-like endoplasmic reticulum kinase;PKR-like endoplasmic reticulum kinase

Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states. PERK is implicated in tumorigenesis and cancer cell survival. GSK2606414 is an orally available, potent, and selective PERK inhibitor. GSK2606414 inhibits PERK activation in cells and inhibits the growth of a human tumor xenograft in mice. PERK activation is independent of the large increase in unfolded nascent proteins within the ER following transient global brain ischemia.

122 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] PERK Inhibitors & Modulators

CCT020312 GSK2606414 Cat. No.: HY-119240 Cat. No.: HY-18072

Bioactivity: CCT020312 is capable of delivering potent, and eukaryotic Bioactivity: GSK2606414 is a cell-permeable and orally available protein initiation factor 2-alpha kinase 3 (EIF2AK3) selective, kinase R-like endoplasmic reticulum (ER) kinase (PERK) proliferation control and also is an activator of RNA-like inhibitor with an IC50 of 0.4 nM. endoplasmic reticulum kinase (PERK).

Purity: 98.56% Purity: 99.38% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

GSK2656157 ISRIB trans-isomer Cat. No.: HY-13820 Cat. No.: HY-12495

Bioactivity: GSK2656157 is a selective and ATP-competitive inhibitor of Bioactivity: ISRIB (trans-isomer) is a potent inhibitor of PERK with an protein kinase R (PKR)-like endoplasmic reticulum kinase ( IC50 of 5 nM. PERK) with an IC50 of 0.9 nM.

Purity: 99.66% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 123 Polo-like Kinase (PLK)

Polo-like Kinases (PLKs) are important regulators of the cell cycle. Plks are involved in the formation of and the changes in the mitotic spindle and in the activation of CDK/cyclin complexes during M-phase of the cell cycle.Polo-like kinases (Plks) are a family of conserved serine/threonine kinases involved in the regulation of cell cycle progression through G2 and mitosis. Mammalian polo-like kinases include Plk1 (Xenopus Plx1), Plk2/Snk (Xenopus Plx2), Plk3/Prk/FnK (Xenopus Plx3), Plk4/Sak and Plk5. Plk1 is involved in the regulation of key steps during cell division, DNA damage repair pathways, apoptosis, and the progression of the cell cycle. Plk3 is a multifunctional stress response protein that responses to signals induced by DNA damage and/or mitotic spindle disruption.

124 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Polo-like Kinase (PLK) Inhibitors & Modulators

BI 2536 Centrinone Cat. No.: HY-50698 (LCR-263) Cat. No.: HY-18682

Bioactivity: BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 Bioactivity: Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 ( PlK4) with a K of 0.16 nM. and 25 nM, respectively [1]. BI-2536 suppresses IFNB i (encoding IFN-β) gene transcription [4].

Purity: 99.95% Purity: 98.57% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Centrinone-B CFI-400945 free base (LCR-323) Cat. No.: HY-18683 Cat. No.: HY-12300

Bioactivity: Centrinone-B (LCR-323) is a potent and highly selective PLK4 Bioactivity: CFI-400945 free base is a potent, selective and orally bioavailable PLK4 inhibitor with a K and an IC of 0.26 nM inhibitor, with a Ki of 0.59 nM. i 50 and 2.8 nM, respectively.

Purity: 98.97% Purity: 98.45% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

CFI-400945 fumarate GSK461364 Cat. No.: HY-12300B (GSK461364A) Cat. No.: HY-50877

Bioactivity: CFI-400945 fumarate is a potent, selective and orally Bioactivity: GSK461364 is a selective, reversible and ATP-competitive

bioavailable PLK4 inhibitor with a Ki and an IC50 of 0.26 nM Polo-like kinase 1 (PLK1) inhibitor with a Ki value of 2.2 nM. and 2.8 nM, respectively.

Purity: 99.27% Purity: 99.82% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

GW843682X HMN-214 (GW843682) Cat. No.: HY-11003 (IVX-214) Cat. No.: HY-12045

Bioactivity: GW843682X is a selective, ATP-competitive inhibitor of PLK1 Bioactivity: HMN-214, an orally bioavailable prodrug of HMN-176, is an inhibitor of polo-like kinase-1 ( plk1), with antitumor and PLK3, with IC50s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against 30 other kinases. activity.

Purity: 99.75% Purity: 99.25% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

LFM-A13 MLN0905 Cat. No.: HY-18009 (PLK1 Inhibitor) Cat. No.: HY-15155

Bioactivity: LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits Bioactivity: MLN0905 is a potent PLK1 inhibitor, with an IC50 of 2 nM. recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.

Purity: 99.70% Purity: 99.94% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg

www.MedChemExpress.com 125

Mps1-IN-2 NMS-1286937 Cat. No.: HY-13994 (NMS-P937) Cat. No.: HY-15828

Bioactivity: Mps1-IN-2 is a potent, selective and ATP-competitive dual Bioactivity: NMS-1286937 is a potent, selective and orally available PLK1 Mps1/Plk1 inhibitor, with an IC and a K of 145 nM and 50 d inhibitor, with an IC50 of 2 nM.

12 nM for Mps1 and a Kd of 61 nM for Plk1.

Purity: 98.06% Purity: 99.70% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Poloxime Poloxin Cat. No.: HY-77195 Cat. No.: HY-12134

Bioactivity: Poloxime, a hydrolysis product of poloxin, is a Bioactivity: Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) non-ATP-competitive Plk1 inhibitor, with moderate Plk1 inhibitor that targets the polo-box domain, with an IC50 of inhibitory activity. appr 4.8 μM.

Purity: 95.0% Purity: 96.26% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 500 mg, 1 g 10 mg, 50 mg

Rigosertib Rigosertib sodium (ON-01910) Cat. No.: HY-12037A (ON-01910 sodium) Cat. No.: HY-12037

Bioactivity: Rigosertib (ON-01910) is a multi-kinase inhibitor and a Bioactivity: Rigosertib sodium (ON-01910 sodium) is a multi-kinase selective anti-cancer agent, which induces apoptosis by inhibitor and a selective anti-cancer agent, which induces inhibition the PI3 kinase/Akt pathway, promots the apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in phosphorylation of histone H2AX and induces G2/M arrest in cell cycle [1] [2]. Rigosertib is a selective and… cell cycle [1] [2]. Rigosertib sodium is a selective and… Purity: 98.09% Purity: 99.49% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Ro3280 SBE13 Cat. No.: HY-15161 Cat. No.: HY-15158A

Bioactivity: Ro3280 is a potent, highly selective inhibitor of PLK1 with Bioactivity: SBE13 is a potent and selective Plk1 inhibitor, with an IC50 of an IC and a K of 3 nM and 0.09 nM, respectively, and 50 d 200 pM; SBE13 poorly inhibits Plk2 (IC 50>66 μM) or Plk3 nearly has no effect on PLK2 and PLK3. (IC 50=875 nM).

Purity: 99.85% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 2 mg, 5 mg, 10 mg, 50 mg

SBE13 Hydrochloride TAK-960 Cat. No.: HY-15158 Cat. No.: HY-15160

Bioactivity: SBE13 Hydrochloride is a potent and selective Plk1 inhibitor, Bioactivity: TAK-960 is an orally available, selective inhibitor of

with an IC50 of 200 pM; SBE13 Hydrochloride poorly inhibits polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM at 10 μM

Plk2 (IC 50>66 μM) or Plk3 (IC 50=875 nM). ATP; TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. Purity: 98.61% Purity: 97.59% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

126 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

TAK-960 dihydrochloride TAK-960 hydrochloride Cat. No.: HY-15160B Cat. No.: HY-15160A

Bioactivity: TAK-960 dihydrochloride is an orally available, selective Bioactivity: TAK-960 hydrochloride is an orally available, selective

inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM at 10 μM ATP; TAK-960 dihydrochloride also shows inhibitory at 10 μM ATP; TAK-960 hydrochloride also shows inhibitory

activities against PLK2 and PLK3, with IC50s of 16.9 … activities against PLK2 and PLK3, with IC50s of 16.9 … Purity: 99.80% Purity: >98% Clinical Data: Phase 1 Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

TC-S 7005 Volasertib Cat. No.: HY-108597 (BI 6727) Cat. No.: HY-12137

Bioactivity: TC-S 7005 is a Polo-like kinases (Plks) inhibitor with IC50s of Bioactivity: Volasertib is a highly potent Polo-like kinase 1 (PLK1) inhibitor with an IC of 0.87 nM, as well as the two closely 4 nM, 24 nM and 214 nM for Plk2, Plk3, and Plk1, respectively 50 [1] . related kinases PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Purity: >98% Purity: 99.55% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg 5 mg, 10 mg, 50 mg, 100 mg

Wortmannin (SL-2052; KY-12420) Cat. No.: HY-10197

Bioactivity: Wortmannin is a multi-target inhibitor. Wortmannin inhibits PI3K [1], MLCK [1], DNA-PK [2], ATM [2], ATR [2], [3] and Polo-like kinase 3 ( Plk3 ) with IC50s of 3 nM, 200 nM, 16 nM, 150 nM, 1.8 μM and 48 nM, respectively. Purity: 99.85% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg

www.MedChemExpress.com 127 PPAR Peroxisome proliferator-activated receptors

PPARs (Peroxisome proliferator-activated receptors) are ligand-activated transcription factors of nuclear hormone receptor superfamily comprising of the following three subtypes: PPARα, PPARγ, and PPARβ/δ. PPARs play essential roles in the regulation of cellular differentiation, development, and metabolism (carbohydrate, lipid, protein), and tumorigenesis of higher organisms. All PPARs heterodimerize with the X receptor (RXR) and bind to specific regions on the DNA of target genes. Activation of PPAR-α reduces triglyceride level and is involved in regulation of energy homeostasis. Activation of PPAR-γ enhances glucose metabolism, whereas activation of PPAR-β/δ enhances fatty acids metabolism.

128 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] PPAR Inhibitors & Modulators

4-O-Methyl honokiol 5-Aminosalicylic Acid Cat. No.: HY-U00450 (Mesalamine; 5-ASA; Mesalazine) Cat. No.: HY-15027

Bioactivity: 4-O-Methyl honokiol is a natural neolignan isolated from Bioactivity: 5-Aminosalicylic acid acts as a specific PPARγ agonist and Magnolia officinalis, acts as a PPARγ agonist, and inhibtis also inhibits p21-activated kinase 1 ( PAK1) and NF-κB. NF-κB activity, used for cancer and inflammation research.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 5 mg, 10 mg, 25 mg Size: 10mM x 1mL in DMSO, 10 g

Adelmidrol Aleglitazar Cat. No.: HY-B1026 (R1439; RO0728804) Cat. No.: HY-14728

Bioactivity: Adelmidrol exerts important anti-inflammatory effects that are Bioactivity: Aleglitazar(R1439; RO-0728804) is a new dual PPAR-α/γ agonist partly dependent on PPARγ. Adelmidrol reduces NF-κB with IC50 of 2.8 nM/4.6 nM. translocation, and COX-2 expression.

Purity: 98.0% Purity: 99.00% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 100 mg

Arhalofenate Astaxanthin (MBX 102; JNJ 39659100) Cat. No.: HY-14831 Cat. No.: HY-B2163

Bioactivity: Arhalofenate (MBX 102) is a selective partial agonist of Bioactivity: Astaxanthin, a red dietary carotenoid isolated from peroxisome proliferator-activated receptor (PPAR)-γ, used for Haematococcus pluvialis, is an inhibitor of PPARγ and a the treatment of type 2 diabetes. potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity [1]. Astaxanthin has potential in the treatment of various diseases, such as cancers and… Purity: >98% Purity: 98.0% Clinical Data: Phase 2 Clinical Data: Launched Size: 1 mg Size: 5 mg, 10 mg

Astragalus polysaccharide AVE-8134 (Astragalus Polysacharin) Cat. No.: HY-N0937 Cat. No.: HY-U00014

Bioactivity: Astragalus polysaccharide are active components of the Bioactivity: AVE-8134 is a potent PPARα agonist, with EC50 values of 100 polysaccharides extract of Astragulus, attenuates and 3000 nM for human and rodent PPARα receptor, respectively. TNF-α-induced insulin resistance by suppressing miR-721 and activating PPAR-γ and PI3K/Akt in 3T3-L1 adipocytes.

Purity: 98.0% Purity: >98% Clinical Data: Phase 4 Clinical Data: No Development Reported Size: 50 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Balaglitazone Bezafibrate (DRF 2593; NN 2344) Cat. No.: HY-16086 (BM15075) Cat. No.: HY-B0637

Bioactivity: Balaglitazone is a selective partial PPARγ agonist with an Bioactivity: Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 EC of 1.351 μM for human PPARγ. 50 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.

Purity: 99.21% Purity: 99.05% Clinical Data: Phase 3 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 100 mg

www.MedChemExpress.com 129

BMS-687453 CDDO-Im Cat. No.: HY-10678 (RTA-403; TP-235; CDDO-Imidazolide) Cat. No.: HY-15725

Bioactivity: BMS-687453 is a potent and selective PPARα agonist, with an Bioactivity: CDDO-Im (CDDO-imidazolide) is an activator of Nrf2 and PPAR,

EC50 and IC50 of 10 nM and 260 nM for human PPARα and 4100 with Kis of 232 and 344 nM for PPARα and PPARγ. nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.

Purity: 99.04% Purity: 98.20% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg

Chiglitazar Choline Cat. No.: HY-106266 (ABT-335) Cat. No.: HY-14739

Bioactivity: Chiglitazar is a PPARα/γ dual agonist, with EC50s of 1.2, Bioactivity: Choline Fenofibrate (ABT-335) is the choline salt of 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively. fenofibric acid under clinical development as a combination therapy with rosuvastatin for the management of dyslipidemia.

Purity: >98% Purity: 99.81% Clinical Data: No Development Reported Clinical Data: Launched Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 10 mg, 100 mg

Ciprofibrate Ciprofibrate D6 (Win35833) Cat. No.: HY-B0664 Cat. No.: HY-B0664S

Bioactivity: Ciprofibrate is a peroxisome proliferator-activated receptor Bioactivity: Ciprofibrate D6 is deuterium labeled Ciprofibrate, which is a agonist. peroxisome proliferator-activated receptor agonist.

Purity: 99.62% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 100 mg, 500 mg

Clofibrate Daidzein Cat. No.: HY-B0287 Cat. No.: HY-N0019

Bioactivity: Clofibrate is an agonist of PPAR, with EC50s of 50 μM, 500 Bioactivity: Daidzein is a soy isoflavone, which acts as a PPAR activator. μM for murine PPARα and PPARγ, and 55 μM, 500 μM for human PPARα and PPARγ, respectively.

Purity: 99.59% Purity: 99.66% Clinical Data: Launched Clinical Data: Phase 4 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 500 mg, 1 g, 5 g, 10 g

DG172 dihydrochloride Elafibranor Cat. No.: HY-19737A (GFT505) Cat. No.: HY-16737

Bioactivity: DG172 dihydrochloride is a selective PPARβ/δ antagonist, with Bioactivity: Elafibranor is a PPARα/δ agonist with EC50s of 45 and 175 an IC of 27 nM. 50 nM, respectively.

Purity: 99.70% Purity: 98.77% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

130 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Ertiprotafib Eupatilin (PTP 112) Cat. No.: HY-19383 Cat. No.: HY-N0783

Bioactivity: Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), Bioactivity: Eupatilin, a lipophilic flavonoid isolated from Artemisia species, is a PPARα agonist, and possesses anti-apoptotic, and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM anti-oxidative and anti-inflammatory activities. for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ. Purity: >98% Purity: 99.01% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg

Fenofibrate Fenofibric acid Cat. No.: HY-17356 (FNF acid) Cat. No.: HY-B0760

Bioactivity: Fenofibrate is a PPARα agonist with an EC50 of 30 μM. Bioactivity: Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 µM, 1.47 µM, and 1.06 µM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also

inhibits COX-2 enzyme activity, with an IC50 of 48 nM. Purity: 99.92% Purity: 99.38% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 g, 10 g 1 g, 5 g

FH535 Fisetin Cat. No.: HY-15721 Cat. No.: HY-N0182

Bioactivity: FH535 is an inhibitor of Wnt/β-catenin and PPAR, with Bioactivity: Fisetin is a natural flavonol found in many fruits and anti-tumor activities. vegetables with various benefits, such as antioxidant, anticancer, neuroprotection effects.

Purity: 99.93% Purity: 98.02% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 100 mg, 500 mg, 1 g

Fonadelpar Gemfibrozil (NPS-005; SJP-0035) Cat. No.: HY-17633 (CI-719) Cat. No.: HY-B0258

Bioactivity: Fonadelpar is a PPARδ agonist, used in the research of Bioactivity: Gemfibrozil is an activator of PPAR-α, used as a neuroparalytic keratopathy. lipid-lowering drug; Gemfibrozil is also a nonselective

inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively. Purity: >98% Purity: 99.91% Clinical Data: No Development Reported Clinical Data: Launched Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 100 mg, 500 mg

Ginsenoside Rh1 Glabridin (Prosapogenin A2; Sanchinoside B2; Sanchinoside Rh1) Cat. No.: HY-N0604 Cat. No.: HY-N0393

Bioactivity: Ginsenoside Rh1 (Prosapogenin A2; Sanchinoside B2; Bioactivity: Glabridin is a natural isoflavan from Glycyrrhiza glabra, binds

Sanchinoside Rh1) is isolated from the root of Panax Ginseng. to and activates PPARγ, with an EC50 of 6115 nM. Glabridin Ginsenoside Rh1 inhibits the expression of PPAR-γ, TNF-α, exhibits antioxidant, anti-bacterial, anti-nephritic, IL-6, and IL-1β. anti-diabetic, anti-fungal, antitumor, anti-inflammatory, antiosteoporotic, cardiovascular protective, neuroprotective… Purity: 98.17% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 10 mg

www.MedChemExpress.com 131

GSK0660 GSK376501A Cat. No.: HY-12377 Cat. No.: HY-101746

Bioactivity: GSK0660 is a potent antagonist of PPARβ and PPARδ, with Bioactivity: GSK376501A is a selective peroxisome proliferator-activated receptor gamma ( PPARγ) modulator for the treatment of type 2 IC50s of 155 nM for both isoforms. diabetes mellitus.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

GSK3787 GW 501516 Cat. No.: HY-15577 (GW 1516; GSK-516) Cat. No.: HY-10838

Bioactivity: GSK3787 is a selective and irreversible peroxisome Bioactivity: GW 501516 is a PPARδ agonist with an EC50 of 1.1 nM. proliferator-activated receptor δ ( PPARδ) antagonist with

pIC50 of 6.6.

Purity: 96.67% Purity: 99.27% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

GW 6471 GW0742 Cat. No.: HY-15372 (GW610742) Cat. No.: HY-13928

Bioactivity: GW 6471 is a potent PPARα antagonist. Bioactivity: GW0742 is a potent PPARβ and PPARδ agonist, with an IC50 of

1 nM for human PPARδ in binding assay, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively. Purity: 98.98% Purity: 97.27% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

GW1929 GW7647 Cat. No.: HY-15655 Cat. No.: HY-13861

Bioactivity: GW1929 is a potent PPAR-γ agonist, with a pKi of 8.84 for Bioactivity: GW7647 is a potent PPARα agonist, with EC50s of 6 nM, 1.1

human PPAR-γ, and pEC50s of 8.56 and 8.27 for human PPAR-γ μM, and 6.2 μM for human PPARα, PPARγ and PPARδ, respectively. and murine PPAR-γ, respectively.

Purity: 99.13% Purity: 98.04% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

GW9662 Icariin Cat. No.: HY-16578 (Ieariline) Cat. No.: HY-N0014

Bioactivity: GW9662 is a potent and selective PPARγ antagonist with an Bioactivity: Icariin is a flavonol glycoside. Icariin inhibits PDE5 and

IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PDE4 activities with IC50s of 432 nM and 73.50 μM, PPARα and PPARδ, respectively. respectively. Icariin also is a PPARα activator.

Purity: 99.53% Purity: 98.75% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 100 mg, 200 mg, 500 mg

132 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Imiglitazar Indeglitazar (TAK-559) Cat. No.: HY-101649 (PPM 204) Cat. No.: HY-14817

Bioactivity: Imiglitazar (TAK559) is a potent and dual human PPARα and Bioactivity: Indeglitazar is an orally available peroxisome proliferator-activated receptor ( PPAR) pan-agonist for all PPARγ1 agonist with EC50 values of 67 and 31 nM. three PPAR subtypes alpha (α), delta (δ) and gamma (γ).

Purity: >98% Purity: 99.42% Clinical Data: Phase 3 Clinical Data: Phase 2 Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 20 mg

Inolitazone Inolitazone dihydrochloride (Efatutazone (dihydrochloride); (Efatutazone; CS-7017; RS5444) Cat. No.: HY-14792 CS-7017 (dihydrochloride); RS5444 (dihydrochloride)) Cat. No.: HY-14792B

Bioactivity: Inolitazone a novel high-affinity PPARγ agonist that is Bioactivity: Inolitazone dihydrochloride is a novel high-affinity PPARγ

dependent upon PPARγ for its biological activity with IC50 of agonist that is dependent upon PPARγ for its biological activity with IC of 0.8 nM for growth inhibition. 0.8 nM for growth inhibition. 50

Purity: >98% Purity: 99.21% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 5 mg Size: 10mM x 1mL in DMSO, 5 mg

KD-3010 L-165041 Cat. No.: HY-111068 Cat. No.: HY-20019

Bioactivity: KD3010 is a potent, orally active, and selective PPARδ Bioactivity: L-165041 is a cell permeable PPARδ agonist, with Kis of 6 nM agonist. and appr 730 nM for PPARδ and PPARγ, respectively, and induces adipocyte differentiation in NIH-PPARδ cells.

Purity: >98% Purity: 99.14% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Lanifibranor LJ570 (IVA337) Cat. No.: HY-104049 Cat. No.: HY-111775

Bioactivity: Lanifibranor is a pan peroxisome proliferator-activated Bioactivity: LJ570 is a PPARα/ PPARγ dual agonist with EC50s of 1.05 receptor ( PPAR) agonist with EC s of 1.5, 0.87 and 0.21 50 and 0.12 μM, respectively [1]. μM for human PPARα, PPARσ and PPARγ, respectively.

Purity: 98.89% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

MA-0204 Magnolol Cat. No.: HY-114739 Cat. No.: HY-N0163

Bioactivity: MA-0204 is a potent, highly selective and orally available Bioactivity: Magnolol, a natural lignan isolated from the stem bark of peroxisome proliferator activated receptor δ ( PPARδ) Magnolia officinalis, is a dual agonist of both RXRα and

modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, PPARγ, with EC50 values of 10.4 µM and 17.7 µM, mouse and rat PPARδ, respectively. Potential treatment … respectively.

Purity: >98% Purity: 99.72% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 133

Naringenin Naveglitazar racemate Cat. No.: HY-N0100 Cat. No.: HY-U00036

Bioactivity: Naringenin is the predominant flavanone in grapefruit; Bioactivity: Naveglitazar racemate is the racemate of Naveglitazar. displays strong anti-inflammatory and antioxidant activities. Naveglitazar is a nonthiozolidinedione peroxisome proliferator-activated receptor ( PPAR) α-γ dual, γ-dominant agonist that has shown glucose-lowering potential in animal models and in the clinic. Purity: 98.72% Purity: >98% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 100 mg, 500 mg, 1 g, 5 g

NXT629 Oleoylethanolamide (N-(2-Hydroxyethyl)oleamide; Cat. No.: HY-114263 N-Oleoyl-2-aminoethanol; N-Oleoylethanolamide; …) Cat. No.: HY-107542

Bioactivity: NXT629 is a potent, selective, and competitive PPAR-α Bioactivity: Oleoylethanolamide is a high affinity endogenous PPAR-α

antagonist, with an IC50 of 77 nM for human PPARα, shows high agonist, which plays an important role in the treatment of selectivity over other nuclear hormone receptor, such as obesity and arteriosclerosis.

PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 3… Purity: 99.05% Purity: >98% Clinical Data: No Development Reported Clinical Data: Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 10 mg, 50 mg

Palmitelaidic Acid Peliglitazar racemate (9-trans-Hexadecenoic acid; trans-Palmitoleic acid) Cat. No.: HY-N2341 (BMS 426707-01 racemate) Cat. No.: HY-101738A

Bioactivity: Palmitelaidic acid is the trans isomer of palmitoleic acid. Bioactivity: Peliglitazar racemate is the racemate of Peliglitazar. Palmitoleic acid is one of the most abundant fatty acids in Peliglitazar is a novel dual α/γ PPAR activator. serum and tissue.

Purity: 99.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Ethanol, Size: 1 mg, 5 mg, 10 mg 10 mg

Pemafibrate Pemafibrate racemate ((R)-K-13675) Cat. No.: HY-17618 (K13675 (racemate)) Cat. No.: HY-17618A

Bioactivity: Pemafibrate is a highly selective PPARα agonist, with an Bioactivity: Pemafibrate racemate is the racemate of pemafibrate, and activates PPARα activity, with EC s of 1 nM, >10 μM and EC50 of 1 nM. 50 1.7 μM for h-PPARα, h-PPARγ and h-PPARδ, respectively.

Purity: 99.78% Purity: >98% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Pioglitazone Pioglitazone hydrochloride (U 72107) Cat. No.: HY-13956 (U 72107A; AD 4833) Cat. No.: HY-14601

Bioactivity: Pioglitazone is a potent and selective PPARγ agonist with Bioactivity: Pioglitazone hydrochloride is a potent and selective PPARγ

high affinity binding to the PPARγ ligand-binding domain with agonist with EC50s of 0.93 and 0.99 μM for human and mouse EC of 0.93 and 0.99 μM for human and mouse PPARγ, 50 PPARγ, respectively. respectively.

Purity: 99.18% Purity: 96.39% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 100 mg, 500 mg

134 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Pirinixic acid PPAR agonist 1 (Wy-14643) Cat. No.: HY-16995 Cat. No.: HY-U00340

Bioactivity: Pirinixic acid (Wy-14643) is a potent agonist of PPARα, with Bioactivity: PPAR agonist 1 is an agonist of PPAR α and PPAR γ, used

EC50s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 for reducing blood glucose, lipid levels, lowering cholesterol μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, and reducing body weight. respectively.

Purity: 99.48% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 10 mg, 50 mg, 100 mg, 250 mg

PPARα-MO-1 Pparδ agonist Cat. No.: HY-U00068 Cat. No.: HY-112597

Bioactivity: PPARα-MO-1 is a potent PPARα modulator extracted from patent Bioactivity: PPARδ agonist is a PPARδ agonist extracted from patent WO/2004/110982A1, formula I. US20180071304, compound example 10.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 500 mg, 250 mg

Pparδ agonist 1 Pparδ agonist 2 Cat. No.: HY-107901 Cat. No.: HY-100120

Bioactivity: Pparδ agonist 1 is a PPAR-δ agonist, with an EC50 of 5.06 Bioactivity: Pparδ agonist 2 is a PPARδ agonist extracted from patent WO nM, used in the research of PPAR-delta related diseases, such 2016057656 A1. as mitochondrial diseases, muscular diseases, vascular diseases, demyelinating diseases and metabolic diseases.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 1 mg, 5 mg, 10 mg

Raspberry ketone Retinoic acid (Frambione; 4-(4-Hydroxyphenyl)-2-butanone) Cat. No.: HY-N1426 (ATRA; ; acid; all-trans-Retinoic acid) Cat. No.: HY-14649

Bioactivity: Raspberry ketone is a major aromatic compound of red Bioactivity: Retinoic acid is a metabolite of vitamin A that plays raspberry, widely used as a fragrance in cosmetics and as a important roles in cell growth, differentiation, and flavoring agent in foodstuff; also shows PPAR-α agonistic organogenesis. Retinoic acid is a natural agonist of RAR

activity. nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retin…

Purity: 99.91% Purity: 98.36% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 100 mg, 500 mg, 1 g, 5 g

RG-12525 Rosiglitazone (NID 525) Cat. No.: HY-101676 (BRL49653) Cat. No.: HY-17386

Bioactivity: RG-12525 is a a specific, competitive and orally effective Bioactivity: Rosiglitazone (BRL49653) is a selective PPARγ agonist with

antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal PPARγ, respectively. strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome… Purity: >98% Purity: 99.21% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 50 mg, 200 mg

www.MedChemExpress.com 135

Rosiglitazone maleate Saroglitazar (BRL 49653C) Cat. No.: HY-14600 Cat. No.: HY-19937

Bioactivity: Rosiglitazone maleate is a potent and selective activator of Bioactivity: Saroglitazar is a novel peroxisome proliferator-activated

PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, receptor ( PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of … cells, respectively. Purity: 99.25% Purity: 98.03% Clinical Data: Launched Clinical Data: Phase 3 Size: 100 mg, 500 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Saroglitazar Seladelpar Cat. No.: HY-19937A (MBX-8025) Cat. No.: HY-19522

Bioactivity: Saroglitazar magnesium is a novel peroxisome Bioactivity: Seladelpar is an orally active, potent (50% effect

proliferator-activated receptor ( PPAR) agonist with concentration EC50 2 nM), and specific PPAR-δ agonist. predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.

Purity: 98.85% Purity: >98% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

Seladelpar sodium salt T0070907 (MBX-8025 sodium salt; RWJ-800025 sodium salt) Cat. No.: HY-19522A Cat. No.: HY-13202

Bioactivity: Seladelpar sodium salt (MBX-8025) is an orally active, potent Bioactivity: T0070907 is a potent PPARγ antagonist with a Ki of 1 nM. and specific PPARδ agonist with an EC50 of 2 nM, showing more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively.

Purity: 98.52% Purity: 99.34% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

Troglitazone (CS-045) Cat. No.: HY-50935

Bioactivity: Troglitazone is a PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murinePPARγ receptor, respectively.

Purity: 99.53% Clinical Data: Launched Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

136 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] RAD51

RAD51 protein family assist in repair of DNA double strand breaks. RAD51 family members are homologous to the bacterial RecA and yeast Rad51. In humans, RAD51 is a 339-amino acid protein that plays a major role in of DNA during double strand break repair. RAD51 is involved in the search for homology and strand pairing stages of the process. RAD51 can interact with the ssDNA-binding protein RPA, BRCA2, PALB2 and RAD52. Recent studies using fluorescent labeled Rad5 has indicated that Rad51 fragments elongate via multiple nucleation events followed by growth, with the total fragment terminating when it reaches about 2 μm in length.

www.MedChemExpress.com 137 RAD51 Inhibitors & Modulators

Harmine IBR2 (Telepathine) Cat. No.: HY-N0737A Cat. No.: HY-103710

Bioactivity: Harmine is a natural dual-specificity tyrosine Bioactivity: IBR2 is a specific RAD51 inhibitor. phosphorylation-regulated kinase ( (DYRK)) inhibitor with anticancer and anti-inflammatory activities.

Purity: 99.78% Purity: 98.14% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

RAD51 Inhibitor B02 RAD51-IN-2 (B02) Cat. No.: HY-101462 Cat. No.: HY-111887

Bioactivity: RAD51 Inhibitor B02 (B02) is an inhibitor of human RAD51 with Bioactivity: RAD51-IN-2 (compound example 67A) is a RAD51 inhibitor [1] an IC50 of 27.4 μM. extracted from patent WO2019/051465A1 .

Purity: 99.18% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 500 mg, 250 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

RI-1 RI-2 Cat. No.: HY-15317 Cat. No.: HY-16904

Bioactivity: RI-1 is a RAD51 inhibitor with IC50 ranging from 5 to 30 μM. Bioactivity: RI-2 is a reversible RAD51 inhibitor, with an IC50 of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.

Purity: 99.30% Purity: 99.22% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

RS-1 T0070907 Cat. No.: HY-19793 Cat. No.: HY-13202

Bioactivity: RS-1 is a RAD51 activator, and also increases Bioactivity: T0070907 is a potent PPARγ antagonist with a Ki of 1 nM. CRISPR/Cas9-mediated knock-in efficiencies.

Purity: 99.55% Purity: 99.34% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

138 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] ROCK Rho-associated protein kinase;Rho-associated kinase;Rho-kinase;ROK

ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA/ PKG/PKC) family of serine-threonine kinases. ROCKs (ROCK1 and ROCK2) occur in mammals, zebrafish, Xenopus, invertebrates and chicken. Human ROCK1 has a molecular mass of 158 kDa and is a major downstream effector of the small GTPase RhoA. Mammalian ROCK consists of a kinase domain, acoiled-coil region and a Pleckstrin homology (PH) domain, which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular fold if RhoA-GTP is not present. ROCK plays a role in a wide range of different cellular phenomena, as ROCK is a downstream effector protein of the small GTPase Rho, which is one of the major regulators of the cytoskeleton.

www.MedChemExpress.com 139 ROCK Inhibitors & Modulators

AT13148 Azaindole 1 Cat. No.: HY-16071 (TC-S 7001) Cat. No.: HY-10319

Bioactivity: AT13148 is an orally active and ATP-competitive, multi- AGC Bioactivity: Azaindole 1 is an orally active and ATP-competitive ROCK

kinase inhibitor with IC50s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, inhibitor with IC50s of 0.6 and 1.1nM for human ROCK-1 and and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, ROCK-2, respectively. respectively.

Purity: 99.54% Purity: 99.46% Clinical Data: Phase 1 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

BDP5290 Chroman 1 Cat. No.: HY-12437 Cat. No.: HY-15392

Bioactivity: BDP5290 is a potent inhibitor of both ROCK and MRCK with Bioactivity: Chroman 1 is a highly potent ROCK2 inhibitor, with an IC50 of IC s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, 50 1 nM. MRCKα and MRCKβ, respectively.

Purity: 98.0% Purity: 99.76% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg

Fasudil Fasudil Hydrochloride (HA-1077; AT877) Cat. No.: HY-10341A (HA-1077 (Hydrochloride); AT-877 (Hydrochloride)) Cat. No.: HY-10341

Bioactivity: Fasudil (HA-1077; AT877), a potent inhibitor of ROCK with a Bioactivity: Fasudil Hydrochloride (HA-1077 Hydrochloride; AT-877 2+ Hydrochloride), a potent inhibitor of ROCK with a K of 0.33 Ki of 0.33 μM for ROCK1, which is also a potent Ca channel i antagonist and vasodilator. μM for ROCK1, which is also a potent Ca2+ channel antagonist and vasodilator. Purity: >98% Purity: 99.91% Clinical Data: Launched Clinical Data: Launched Size: 100 mg, 200 mg, 500 mg Size: 10mM x 1mL in DMSO, 200 mg, 500 mg

GSK180736A GSK269962A Cat. No.: HY-18990 (GSK 269962) Cat. No.: HY-15556

Bioactivity: GSK180736A is a G protein-coupled receptor kinase 2 ( GRK2) Bioactivity: GSK269962A is a potent ROCK inhibitor with IC50s of 1.6 and 4 inhibitor with an IC of 0.77 μM. 50 nM for recombinant human ROCK1 and ROCK2 respectively.

Purity: 98.05% Purity: 98.01% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

GSK429286A H-1152 Cat. No.: HY-11000 Cat. No.: HY-15720

Bioactivity: GSK429286A is a selective inhibitor of ROCK1 with an IC50 Bioactivity: H-1152 is a membrane-permeable and selective ROCK inhibitor, with a K value of 1.6 nM, and an IC value of 12 nM for value of 14 nM. i 50 ROCK2.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 5 mg, 10 mg

140 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

H-1152 dihydrochloride Hydroxyfasudil Cat. No.: HY-15720A (HA-1100) Cat. No.: HY-13911

Bioactivity: H-1152 dihydrochloride is a membrane-permeable and selective Bioactivity: Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and ROCK inhibitor, with a K value of 1.6 nM, and an IC value i 50 0.72 μM for ROCK1 and ROCK2, respectively. of 12 nM for ROCK2.

Purity: 98.0% Purity: 98.13% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 5 mg, 10 mg, 50 mg

Hydroxyfasudil hydrochloride (HA-1100 hydrochloride; HA 1100 LX7101 hydrochloride; HA1100 hydrochloride) Cat. No.: HY-13911A Cat. No.: HY-12659

Bioactivity: Hydroxyfasudil hydrochloride is a ROCK inhibitor, with IC50s Bioactivity: LX7101 is a potent inhibitor of LIMK and ROCK2 with IC50 of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively. values of 24, 1.6 and 10 nM for LIMK1, LIMK2 and ROCK2,

respectively; also inhibits PKA with an IC50 less than 1 nM.

Purity: 99.40% Purity: 99.29% Clinical Data: Launched Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

Narciclasine Pentanoic acid (Lycoricidinol) Cat. No.: HY-16563 Cat. No.: HY-N6056

Bioactivity: Narciclasine is a plant growth modulator. Narciclasine Bioactivity: Pentanoic acid, a short-chain fatty acid, is a product of modulates the Rho/Rho kinase/LIM kinase/cofilin signaling bacterial metabolism and are associated with allergic skin pathway, greatly increasing GTPase RhoA activity as well as disorders. Pentanoic acid activates ROCK signaling pathway. inducing actin stress fiber formation in a RhoA-dependent manner. Purity: 99.94% Purity: >98% Clinical Data: No Development Reported Clinical Data: Size: 10mM x 1mL in DMSO, Size: 10 mg 1 mg, 5 mg, 10 mg

Ripasudil Ripasudil free base (K-115) Cat. No.: HY-15685 (K-115 (free base)) Cat. No.: HY-15685A

Bioactivity: Ripasudil (K-115) is a specific inhibitor of ROCK, with IC50s Bioactivity: Ripasudil free base (K-115 free base) is a specific inhibitor of ROCK, with IC s of 19 and 51 nM for ROCK2 and ROCK1, of 19 and 51 nM for ROCK2 and ROCK1, respectively. 50 respectively.

Purity: 99.75% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

RKI-1447 ROCK inhibitor-2 Cat. No.: HY-15755 Cat. No.: HY-119937

Bioactivity: RKI-1447 is a potent small molecule inhibitor of ROCK1 and Bioactivity: ROCK inhibitor-2 is a selective dual ROCK1 and ROCK2 ROCK2 with IC values of 14.5 nM and 6.2 nM, respectively. [1] 50 inhibitor with IC50s of 17 nM and 2 nM, respectively .

Purity: 97.26% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 100 mg, 500 mg, 250 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 141

ROCK-IN-1 ROCK2-IN-2 Cat. No.: HY-U00351 Cat. No.: HY-103620

Bioactivity: ROCK-IN-1 is a potent inhibitor of ROCK, with an IC50 of 1.2 Bioactivity: ROCK2-IN-2 is a selective ROCK2 inhibitor extracted from patent US20180093978A1, Compound A-30, has an IC of <1 nM for ROCK2. 50 μM.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 250 mg, 500 mg

SAR407899 SAR407899 hydrochloride Cat. No.: HY-15687A Cat. No.: HY-15687

Bioactivity: SAR407899 is a selective, potent and ATP-competitive ROCK Bioactivity: SAR407899 hydrochloride is a selective, potent and ATP-competitive ROCK inhibitor, with an IC of 135 nM for inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 50

nM and 41 nM for human and rat ROCK-2, respectively. ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively. Purity: 98.43% Purity: 99.81% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

SB-772077B dihydrochloride SLx-2119 Cat. No.: HY-108518 (KD-025) Cat. No.: HY-15307

Bioactivity: SB-772077B dihydrochloride is an aminofurazan-based Rho Bioactivity: SLx-2119 (KD-025) is a selective inhibitor of ROCK2 with an

kinase( ROCK) inhibitor with IC50s of 5.6 nM and 6 nM toward IC50 of 105 nM. ROCK1 and ROCK2, respevtively [1].

Purity: 99.0% Purity: 99.59% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg 5 mg, 10 mg, 50 mg, 100 mg

SR-3677 Thiazovivin Cat. No.: HY-13300 Cat. No.: HY-13257

Bioactivity: SR-3677 is a potent and selective ROCK-II inhibitor with an Bioactivity: Thiazovivin is a potent ROCK inhibitor, which can protect

IC50 of ~3 nM. human embryonic stem cells.

Purity: 99.46% Purity: 99.32% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Y-27632 Y-27632 dihydrochloride Cat. No.: HY-10071 Cat. No.: HY-10583

Bioactivity: Y-27632 is an ATP-competitive inhibitor of ROCK-I and ROCK-II, Bioactivity: Y-27632 dihydrochloride is a cell-permeable, ATP-competitive

with Ki of 220 nM and 300 nM for ROCK-I and ROCK-II, inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively, which primes human induced pluripotent stem respectively, which primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal… mesendodermal lineage via epithelial-mesenchymal… Purity: 99.65% Purity: 99.83% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g, 2 g

142 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Y-33075 Y-33075 dihydrochloride (Y 39983) Cat. No.: HY-10067 Cat. No.: HY-10069

Bioactivity: Y-33075 is a selective ROCK inhibitor derived from Y-27632, Bioactivity: Y-33075 dihydrochloride is a selective ROCK inhibitor with an

and is more potent than Y-27632, with an IC50 of 3.6 nM. IC50 of 3.6 nM.

Purity: 98.98% Purity: 97.92% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

ZINC00881524 Cat. No.: HY-101244

Bioactivity: ZINC00881524 is a ROCK inhibitor.

Purity: 99.23% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 143 Sirtuin

Sirtuin (Sir2 proteins) are a class of proteins that possess either mono-ADP-ribosyltransferase, or deacylase activity, including deacetylase, desuccinylase, demalonylase, demyristoylase and depalmitoylase activity. Sirtuins regulate important biological pathways in bacteria, archaeaand . Sirtuins have been implicated in influencing a wide range of cellular processes like aging, transcription, apoptosis, inflammation and stress resistance, as well as energy efficiency and alertness during low-calorie situations. Sirtuins can also control circadian clocks and mitochondrial biogenesis.

144 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Sirtuin Inhibitors & Modulators

3-TYP AGK2 Cat. No.: HY-108331 Cat. No.: HY-100578

Bioactivity: 3-TYP is a selective SIRT3 inhibitor, with an IC50 of 16 nM, Bioactivity: AGK2 is a selective SIRT2 inhibitor with IC50 of 3.5 μM. AGK2

more potent over SIRT1 ( IC50=88 nM), SIRT2 ( IC50=92 nM). can also inhibit SIRT1 and SIRT3 with IC50 of 30 and 91 μM, respectively.

Purity: 99.87% Purity: 98.66% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg

AK-1 AK-7 Cat. No.: HY-101465 Cat. No.: HY-16691

Bioactivity: AK-1 is a potent, specific and cell-permeable SIRT2 inhibitor, Bioactivity: AK-7 is a selective cell- and brain-permeable SIRT2 inhibitor,

with an IC50 of 12.5 μM. with an IC50 of 15.5 μM.

Purity: 98.0% Purity: 99.59% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg 10 mg, 50 mg, 100 mg

Cambinol CAY10602 Cat. No.: HY-100732 Cat. No.: HY-104073

Bioactivity: Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 Bioactivity: CAY10602 is a SIRT1 activator. and 59 μM, respectively.

Purity: 99.70% Purity: 98.56% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Dihydrocoumarin Fisetin (Hydrocoumarin; Chroman-2-one) Cat. No.: HY-N1926 Cat. No.: HY-N0182

Bioactivity: Dihydrocoumarin is a compound found in Melilotus Bioactivity: Fisetin is a natural flavonol found in many fruits and officinalis. Dihydrocoumarin is a yeast Sir2p inhibitor. vegetables with various benefits, such as antioxidant, Dihydrocoumarin also inhibits human SIRT1 and SIRT2 with anticancer, neuroprotection effects. [1] IC50s of 208 μM and 295 μM, respectively . Purity: 99.09% Purity: 98.02% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 100 mg, 500 mg, 1 g

Ginkgolide C Inauhzin (BN-52022; Ginkgolide-C) Cat. No.: HY-N0785 (INZ) Cat. No.: HY-15869

Bioactivity: Ginkgolide C is a flavone isolated from Ginkgo biloba leaves, Bioactivity: Inauhzin is a dual SirT1/IMPDH2 inhibitor, and acts as an possessing multiple biological functions, such as decreasing activator p53, used in the research of cancer. platelet aggregation and ameliorating Alzheimer disease.

Purity: 98.0% Purity: 98.91% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 145

MC3482 Cat. No.: HY-112587 (Niacinamide; Nicotinic acid amide; Vitamin B3) Cat. No.: HY-B0150

Bioactivity: MC3482 is a specific sirtuin5 ( SIRT5) inhibitor. Bioactivity: Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1. Purity: 99.22% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 1 g, 5 g

OSS_128167 PROTAC Sirt2 Degrader-1 Cat. No.: HY-107454 Cat. No.: HY-103636

Bioactivity: OSS_128167 is a selective SIRT6 inhibitor with IC50s of 89, Bioactivity: PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively. Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2

Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect… Purity: 98.22% Purity: 98.76% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg

Salermide Selisistat Cat. No.: HY-101073 (EX-527) Cat. No.: HY-15452

Bioactivity: Salermide is an inhibitor of Sirt1 and Sirt2; can cause strong Bioactivity: Selisistat (EX-527) is a potent and selective SIRT1 inhibitor

cancer-specific apoptotic cell death. with IC50 of 98 nM.

Purity: 98.0% Purity: 99.82% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg

Selisistat S-enantiomer SIRT-IN-1 (EX-527 (S-enantiomer)) Cat. No.: HY-15452A Cat. No.: HY-16615

Bioactivity: Selisistat S-enantiomer (EX-527 S-enantiomer) is the Bioactivity: SIRT-IN-1 is a potent inhibitor of SIRT1/2/3, with IC50s of 15, S-enantiomer of Selisistat, with an IC of 123 nM for SIRT1. 50 10, 33 μM, respectively. Selisistat S-enantiomer is much more potent than Selisistat R-enantiomer.

Purity: 98.50% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 5 mg, 10 mg

SIRT-IN-2 Sirt2-IN-1 Cat. No.: HY-16616 Cat. No.: HY-112427

Bioactivity: SIRT-IN-2 is a potent inhibitor of SIRT1/2/3, with IC50s of 4, Bioactivity: Sirt2-IN-1 (Compound 9) is a sirtuin 2 ( Sirt2) inhibitor with [1] 4, 7 μM, respectively. an IC50 of 163 nM .

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

146 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

SIRT5 inhibitor 1 Sirtinol Cat. No.: HY-112634 Cat. No.: HY-13515

Bioactivity: SIRT5 inhibitor 1 is a potent Human Sirtuin 5 deacylase Bioactivity: Sirtinol is a sirtuin inhibitor, with IC50s of 48 μM, 57.7 μM inhibitor, with an IC of 0.11 μM. 50 and 131 μM for ySir2, hSIRT2 and hSIRT2, respectively.

Purity: 99.36% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Sirtuin modulator 1 SRT 1460 Cat. No.: HY-19758A Cat. No.: HY-124037

Bioactivity: Sirtuin modulator 1 is a modulator of SIRTl, a homolog of SIRT3, Bioactivity: SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 with EC 1.5 of < 1 μM, extracted from patent WO 2010071853 value of 2.9 μM, shows good selectivity for activation of A1, Compound No.4. SIRT1 versus SIRT2 and SIRT3 (EC1.5 > 300 μM), and is more potent than Resveratrol and the closest sirtuin homolog…

Purity: 99.44% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg, 100 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

SRT 1720 SRT 1720 Hydrochloride Cat. No.: HY-10532 Cat. No.: HY-15145

Bioactivity: SRT 1720 is a selective activator of human SIRT1 with an Bioactivity: SRT 1720 Hydrochloride is a selective activator of SIRT1 with

EC1.5 of 0.16 μM, and shows less potent activities agaiinst an EC1.5 of 0.16 μM, and shows less potent activities on

SIRT2 and SIRT3 with EC 1.5s of 37 μM and > 300 μM, SIRT2 and SIRT3 with EC 1.5s of 37 μM and 300 μM, respectively. respectively. Purity: >98% Purity: 99.92% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

SRT 2104 SRT 2183 Cat. No.: HY-15262 Cat. No.: HY-19759

Bioactivity: SRT 2104 is a first-in-class, highly selective and Bioactivity: SRT 2183 is a selective Sirtuin-1 (SIRT1) activator with an brain-permeable activator of the NAD + dependent deacetylase [1] EC1.5 value of 0.36 μM . SRT 2183 induces growth arrest Sirt1, increases Sirt1 protein, but shows no effect on Sirt1 and apoptosis, concomitant with deacetylation of STAT3 and mRNA. Used in the research of diabetes mellitus … NF-κB, and reduction of c-Myc protein levels [2]. Purity: 98.87% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g Size:

Tenovin-1 Tenovin-6 Cat. No.: HY-13423 Cat. No.: HY-15510

Bioactivity: Tenovin-1 is an inhibitor of sirtuin 1 and sirtuin 2, an Bioactivity: Tenovin-6 is an inhibitor of SIRT1 and SIRT2, slightly inhibits

activator of p53 and may have potential in the management of HDAC8, and is also a potent activator of p53, with IC50s of cancer. 21 μM, 10 μM, and 67 μM for SirT1, SirT2, and SirT3, respectively.

Purity: 99.39% Purity: 98.24% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 147

Tenovin-6 Hydrochloride Thiomyristoyl Cat. No.: HY-15510B Cat. No.: HY-101278

Bioactivity: Tenovin-6 Hydrochloride is an inhibitor of SIRT1 and SIRT2, Bioactivity: Thiomyristoyl is a potent and specific SIRT2 inhibitor with an

slightly inhibits HDAC8, and is also a potent activator of IC50 of 28 nM. p53, with IC50s of 21 μM, 10 μM, and 67 μM for SirT1, SirT2, and SirT3, respectively.

Purity: 98.0% Purity: 98.84% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

UBCS039 Cat. No.: HY-115453

Bioactivity: UBCS039 is the first synthetic, specific Sirtuin 6 (SIRT6) activator, inducing autophagy in human tumor cells, with an [1] EC50 of 38 μM .

Purity: 98.55% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

148 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] SRPK Serine-arginine protein kinases

SRPKs is a critical enzyme family that regulates splicing activity in the cell. The first serine-arginine (SR) protein kinase identified is SRPK1, which is isolated from mitotic cells, and it is described to phosphorylate SR proteins and to promote their release from nuclear speckles during the G2/M phase of the cell cycle. SRPK1 is the prototype of the SRPK family, which also includes the two homologous SRPK2 and SRPK3 proteins. SRPKs are characterized by a bipartite catalytic domain separated by a unique spacer sequence and are mainly localized in the cytoplasm of mammalian cells. SRPKs can translocate into the nucleus of cells under several conditions, such as during the G2/M phase of the cell cycle, or after osmotic stress, or as a consequence of activation of the epidermal growth factor (EGF) signal transduction pathway.

www.MedChemExpress.com 149 SRPK Inhibitors & Modulators

SPHINX31 SRPIN340 Cat. No.: HY-117661 (SRPK inhibitor) Cat. No.: HY-13949

Bioactivity: SPHINX31 is a potent and selective inhibitor of Bioactivity: SRPIN340 is an ATP-competitive serine-arginine-rich protein

serine/arginine-rich protein kinase 1 (SRPK1), with an IC50 of kinase ( SRPK) inhibitor, with a Ki of 0.89 μM for SRPK1. 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 is a potential topical therapeutic for neovascular eye disease… Purity: 99.17% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

SRPKIN-1 Cat. No.: HY-116856

Bioactivity: SRPKIN-1 is a covalent and irreversible SRPK1/2 inhibitor

with IC50s of 35.6 and 98 nM, respectively. Anti-angiogenesis effect [1].

Purity: >98% Clinical Data: No Development Reported Size: 500 mg, 250 mg

150 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Telomerase

Telomerase is a ribonucleoprotein that is an enzyme that adds DNA sequence repeats ("TTAGGG" in all vertebrates) to the 3' end of DNA strands in the telomere regions, which are found at the ends of eukaryotic chromosomes. This region of repeated nucleotide called telomeres contains noncoding DNA and hinders the loss of important DNA from chromosome ends. As a result, every time the chromosome is copied, only 100–200 are lost, which causes no damage to the organism's DNA. Telomerase is a reverse transcriptase that carries its own RNA molecule, which is used as a template when it elongates telomeres, which are shortened after each replication cycle. Telomerase, a eukaryotic ribonucleoprotein (RNP) complex, contains both an essential RNA and a protein reverse transcriptase subunit. By reverse transcription, the telomerase RNP maintains telomere length stability in almost all cancer cells.

www.MedChemExpress.com 151 Telomerase Inhibitors & Modulators

360A 360A iodide Cat. No.: HY-15595 (360 A iodide) Cat. No.: HY-15595A

Bioactivity: 360A is a selective stabilizer of G-quadruplex, and also Bioactivity: 360A iodide is a selective stabilizer of G-quadruplex, and also

inhibits telomerase activity with an IC50 of 300 nM for inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay. telomerase in TRAP-G4 assay.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

BIBR 1532 Telomerase-IN-1 Cat. No.: HY-17353 Cat. No.: HY-U00268

Bioactivity: BIBR 1532 is a potent, selective and non-competitive Bioactivity: Telomerase-IN-1 is a Telomerase inhibitor with an IC50 of telomerase inhibitor with IC of 100 nM in 50 0.19 μM. a cell-free assay.

Purity: 99.55% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 10 mg, 50 mg, 100 mg

TMPyP4 tosylate (TMP 1363) Cat. No.: HY-108477

Bioactivity: TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand, which inhibits the interaction between G-quadruplexes and IGF-1 [1]. TMPyP4 tosylate (TMP 1363) is a telomerase inhibitor with antitumor effects in osteosarcoma cell li…

Purity: 98.0% Clinical Data: No Development Reported Size: 100 mg

152 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] TOPK T-LAK cell-originated protein kinase

TOPK (T-lymphokine-activated killer cell–originated protein kinase, also known as PBK or PDZ-binding kinase) is a Ser/Thr protein kinase that is highly expressed in many types of human cancer, including breast and lung cancers. TOPK is included in the “consensus stemness ranking signature” gene list that is up-regulated in cancer -enriched tumors and is associated with poor prognosis in multiple types of cancer. TOPK/PBK is an oncogenic kinase upregulated in most human cancers. TOPK is important for mitotic cell division and that phosphorylation by Cdk1 is needed for its activation. TOPK, a member of the MEK3/6-related MAPKK family, is expressed in a wide range of proliferating cells and tissues, including cancer cells and testis. TOPK negatively regulates the activity of p38α by phosphorylating the p38α-specific phosphatase MKP1 and enhancing the stability of MKP1. The MAPK phosphatase MKP1, an archetypal member of the MKP family, plays a pivotal role in the deactivation of p38 through a dephosphorylation reaction.

www.MedChemExpress.com 153 TOPK Inhibitors & Modulators

HI-TOPK-032 OTS-964 Cat. No.: HY-101550 Cat. No.: HY-12467

Bioactivity: HI-TOPK-032 is a potent and specific TOPK inhibitor. Bioactivity: OTS-964 is a potent T-lymphokine-activated killer

cell-originated protein kinase (TOPK) inhibitor ( IC50=28 nM), which inhibits TOPK kinase activity with high affinity and selectivity.

Purity: 99.36% Purity: 99.05% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

OTS514 Cat. No.: HY-18621

Bioactivity: OTS514 is a highly potent TOPK inhibitor, which inhibits TOPK

kinase activity with a median inhibitory concentration ( IC50) value of 2.6 nM.

Purity: 95.63% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

154 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Topoisomerase

Topoisomerases are enzymes that regulate the overwinding or underwinding of DNA. The winding problem of DNA arises due to the intertwined nature of its double-helical structure. Topoisomerases are isomerase enzymes that act on the topology of DNA. cuts one strand of a DNA double helix, relaxation occurs, and then the cut strand is reannealed. Type I topoisomerases are subdivided into two subclasses: type IA topoisomerases, which share many structural and mechanistic features with the type II topoisomerases, and type IB topoisomerases, which utilize a controlled rotary mechanism. Type II topoisomerase cuts both strands of one DNA double helix, pass another unbroken DNA helix through it, and then reanneal the cut strands. This class is also split into two subclasses: type IIA and type IIB topoisomerases, which possess similar structure and mechanisms.

www.MedChemExpress.com 155 Topoisomerase Inhibitors & Modulators

9-amino-CPT Aclacinomycin A hydrochloride (9-amino-20(S)-) Cat. No.: HY-100309 ( hydrochloride) Cat. No.: HY-N2306A

Bioactivity: 9-Aminocamptothecin is a topoisomerase I inhibitor with Bioactivity: Aclacinomycin A hydrochloride (Aclarubicin hydrochloride), a potent anticancer activity. fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome [1]. Aclacinomycin A hydrochloride is also a dual inhibitor of… Purity: 98.89% Purity: 98.08% Clinical Data: Phase 2 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 25 mg, 50 mg

Aldoxorubicin Amonafide (INNO-206; DOXO-EMCH) Cat. No.: HY-16261 (AS1413) Cat. No.: HY-10982

Bioactivity: Aldoxorubicin (INNO-206) is an albumin-binding prodrug of Bioactivity: Amonafide is a topoisomerase II inhibitor and DNA , which is released from albumin under acidic intercalator that induces apoptotic signaling by blocking the conditions. Aldoxorubicin (INNO-206) has potent antitumor binding of Topo II to DNA. activities in various cancer cell lines and in murine tumor models. Purity: 92.43% Purity: 99.75% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Amrubicin hydrochloride (SM-5887; AMR) Cat. No.: HY-B0067 (SM-5887 (hydrochloride); AMR (hydrochloride)) Cat. No.: HY-B0067A

Bioactivity: Amrubicin (SM-5887) is a DNA topoisomerase II inhibitor, Bioactivity: Amrubicin (hydrochloride) (SM-5887 (hydrochloride)) is a DNA used for the research of cancer. topoisomerase II inhibitor, used for the research of cancer.

Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Amsacrine hydrochloride (m-AMSA; acridinyl anisidide) Cat. No.: HY-13551 (m-AMSA hydrochloride; acridinyl anisidide hydrochloride) Cat. No.: HY-13551A

Bioactivity: Amsacrine (m-AMSA) is an inhibitor of topoisomerase II, and Bioactivity: Amsacrine hydrochloride (mAMSA hydrochloride) is an inhibitor acts as an antineoplastic agent which can intercalates into of topoisomerase II, and acts as an antineoplastic agent the DNA of tumor cells. which can intercalates into the DNA of tumor cells.

Purity: 99.98% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg, 500 mg

Banoxantrone D12 Banoxantrone D12 dihydrochloride (AQ4N D12) Cat. No.: HY-13562S (AQ4N D12 dihydrochloride) Cat. No.: HY-13562AS

Bioactivity: Banoxantrone D12 (AQ4N D12) is the deuterium labeled Bioactivity: Banoxantrone D12 dihydrochloride (AQ4N D12 dihydrochloride) is banoxantrone. Banoxantrone is a novel bioreductive agent that the deuterium labeled banoxantrone dihydrochloride. can be reduced to a stable, DNA-affinic compound AQ4, which is Banoxantrone is a novel bioreductive agent that can be reduced a potent topoisomerase II inhibitor. to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor. Purity: >98% Purity: 98.02% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg

156 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Banoxantrone dihydrochloride hydrochloride (AQ4N dihydrochloride) Cat. No.: HY-13562A (CKD-602) Cat. No.: HY-13566A

Bioactivity: Banoxantrone dihydrochloride is a novel bioreductive agent Bioactivity: Belotecan hydrochloride (CKD-602 hydrochloride), a that can be reduced to a stable, DNA-affinic compound AQ4, Topoisomerase I inhibitor, is a synthetic and water-soluble which is a potent topoisomerase II inhibitor. camptothecin derivative.

Purity: 98.17% Purity: 98.80% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Berberine chloride Berberine chloride hydrate (Natural Yellow 18 (chloride)) Cat. No.: HY-18258 (Natural Yellow 18 (chloride hydrate)) Cat. No.: HY-17577

Bioactivity: Berberine chloride is an alkaloid isolated from the Chinese Bioactivity: Berberine chloride hydrate is an alkaloid isolated from the herbal medicine Huanglian, as an antibiotic. Berberine chloride Chinese herbal medicine Huanglian, as an antibiotic. Berberine induces reactive oxygen species ( ROS) generation and chloride hydrate induces reactive oxygen species ( ROS) inhibits DNA topoisomerase. Antineoplastic properties generation and inhibits DNA topoisomerase. Antineoplastic [1]. properties [1]. Purity: >98% Purity: 99.56% Clinical Data: Launched Clinical Data: Launched Size: 100 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 g

Betulinic acid Bisantrene (Lupatic acid; Betulic acid) Cat. No.: HY-10529 (CL216942) Cat. No.: HY-100875

Bioactivity: Betulinic acid is a natural pentacyclic triterpenoid, acts as Bioactivity: Bisantrene is a highly effective antitumor drug, targets

a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 eukaryotic type II topoisomerases. μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties.

Purity: 98.18% Purity: 96.35% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 25 mg, 50 mg 100 mg, 200 mg, 500 mg

Campathecin Daun02 (Camptothecin; (S)-(+)-Camptothecin; CPT) Cat. No.: HY-16560 Cat. No.: HY-13061

Bioactivity: Campathecin is a potent DNA enzyme topoisomerase I Bioactivity: Daun02 is a prodrug of the topoisomerase inhibitor

inhibitor, with an IC50 of 679 nM. Daunorubicin.

Purity: 98.26% Purity: 98.56% Clinical Data: Phase 4 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 2 mg, 5 mg, 10 mg

Daunorubicin Daunorubicin Hydrochloride (RP 13057 (Hydrochloride); (RP 13057; Daunomycin; Rubidomycin) Cat. No.: HY-13062A Daunomycin (Hydrochloride); Rubidomycin (Hydrochloride)) Cat. No.: HY-13062

Bioactivity: Daunorubicin (RP 13057, Daunomycin, Rubidomycin) is a Bioactivity: Daunorubicin Hydrochloride is a topoisomerase II inhibitor topoisomerase II inhibitor with potent antineoplastic with potent antineoplastic activities. Daunorubicin activities. Daunorubicin inhibites DNA and RNA synthesis in Hydrochloride inhibites DNA and RNA synthesis in sensitive and sensitive and resistant Ehrlich ascites tumor cells. resistant Ehrlich ascites tumor cells.

Purity: >98% Purity: 99.27% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg Size: 10mM x 1mL in Water, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

www.MedChemExpress.com 157

Doxorubicin Doxorubicin hydrochloride (Hydroxydaunorubicin) Cat. No.: HY-15142A (Hydroxydaunorubicin (hydrochloride)) Cat. No.: HY-15142

Bioactivity: Doxorubicin is a cytotoxic antibiotic for the Bioactivity: Doxorubicin hydrochloride is a cytotoxic anthracycline treatment of multiple cancers. The possible mechanisms by antibiotic for the treatment of multiple cancers. The possible which doxorubicin acts in the cancer cell are intercalation mechanisms by which doxorubicin acts in the cancer cell are into DNA and disruption of topoisomerase-II-mediated DNA intercalation into DNA and disruption of repair. topoisomerase-II-mediated DNA repair. Purity: >98% Purity: 99.47% Clinical Data: Launched Clinical Data: Launched Size: 50 mg, 100 mg, 200 mg, 500 mg Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 200 mg, 500 mg, 1 g

Dxd Edotecarin ( derivative for ADC) Cat. No.: HY-13631D (J 107088; PF 804950) Cat. No.: HY-13618

Bioactivity: Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of Bioactivity: Edotecarin is a potent inhibitor of topoisomerase I that can induces single-strand DNA cleavage, with IC of 50 nM. 0.31 μM, used as a conjugated drug of HER2-targeting ADC 50 (DS-8201a).

Purity: 98.20% Purity: 98.39% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 1 mg, 5 mg, 10 mg

Ellipticine Ellipticine hydrochloride (NSC 71795) Cat. No.: HY-15753 (NSC 71795 (hydrochloride)) Cat. No.: HY-15753A

Bioactivity: Ellipticine (NSC 71795) is a potent antineoplastic agent; Bioactivity: Ellipticine (NSC 71795) hydrochloride is a potent inhibits DNA topoisomerase II activities. antineoplastic agent; inhibits DNA topoisomerase II activities.

Purity: >98% Purity: 98.08% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Epirubicin hydrochloride Cat. No.: HY-13624 (4'-Epidoxorubicin hydrochloride) Cat. No.: HY-13624A

Bioactivity: Epirubicin is a semisynthetic L-arabino derivative of Bioactivity: Epirubicin (hydrochloride) is a semisynthetic L-arabino doxorubicin, and an antineoplastic agent by inhibiting derivative of doxorubicin, and an antineoplastic agent by Topoisomerase. inhibiting Topoisomerase.

Purity: >98% Purity: 98.88% Clinical Data: Launched Clinical Data: Launched Size: 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Etoposide Exatecan (VP-16; VP-16-213) Cat. No.: HY-13629 (DX-8951) Cat. No.: HY-13631

Bioactivity: (VP-16; VP-16-213), a chemotherapy medication used Bioactivity: Exatecan is a water soluble topoisomerase I inhibitor, with

for the treatments of a number of types of cancer, inhibits an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer DNA synthesis by forming a complex with topoisomerase II and research. DNA. Etoposide arrests cell cycle in G2 and induces apoptos…

Purity: 99.65% Purity: >98% Clinical Data: Launched Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 100 mg, 200 mg, 500 mg

158 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Exatecan Mesylate Flumequine (DX8951f) Cat. No.: HY-13631A (R-802) Cat. No.: HY-B0526

Bioactivity: Exatecan Mesylate is a water soluble topoisomerase I Bioactivity: Flumequine (R-802) is a quinolone antibiotic, and acts as a topoisomerase II inhibitor, with an IC of 15 μM (3.92 inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be 50 used in cancer research. μg/mL).

Purity: 99.12% Purity: 99.53% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 250 mg, 500 mg 10 mg, 50 mg

Genz-644282 hydrochloride Cat. No.: HY-16228 (4-Demethoxydaunorubicin hydrochloride) Cat. No.: HY-17381

Bioactivity: Genz-644282 is a non-camptothecin topoisomerase I inhibitor, Bioactivity: Idarubicin hydrochloride is an anthracycline antileukemic used for cancer research. drug. It inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription.

Purity: 98.03% Purity: 99.62% Clinical Data: Phase 1 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

Indotecan Intoplicine (LMP-400; NSC-724998) Cat. No.: HY-18351 Cat. No.: HY-101647

Bioactivity: Indotecan (LMP-400) is a potent topoisomerase 1(Top1) Bioactivity: Intoplicine is a DNA topoisomerase I and II inhibitor.

inhibitor with IC50 values of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively.

Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg

Irinotecan hydrochloride ((+)-Irinotecan; CPT-11) Cat. No.: HY-16562 (CPT-11 hydrochloride; Camptothecin 11 hydrochloride) Cat. No.: HY-16562A

Bioactivity: Irinotecan is a water soluble topoisomerase I inhibitor, Bioactivity: Irinotecan hydrochloride is a water soluble topoisomerase I preventing religation of the DNA strand by binding to inhibitor mainly used to treat colon cancer and rectal cancer. topoisomerase I-DNA complex.

Purity: 99.84% Purity: 99.75% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 200 mg, 500 mg 50 mg, 100 mg, 200 mg, 500 mg

Irinotecan hydrochloride trihydrate Karenitecin Cat. No.: HY-16568 (Cositecan; BNP 1350) Cat. No.: HY-14812

Bioactivity: Irinotecan hydrochloride trihydrate is a water soluble Bioactivity: Karenitecin (Cositecan) is a topoisomerase I inhibitor, with topoisomerase I inhibitor with antitumor activity. potent anti-cancer activity.

Purity: 99.78% Purity: 98.30% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 200 mg, 500 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 159

LMP744 LMP744 hydrochloride (MJ-III65; NSC706744) Cat. No.: HY-U00248 (MJ-III65 hydrochloride; NSC706744 hydrochloride) Cat. No.: HY-U00248A

Bioactivity: LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I Bioactivity: LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA (Top1) inhibitor with antitumor activity [1]. intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity [1].

Purity: >98% Purity: >98% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg

MC-DOXHZN MC-DOXHZN hydrochloride (Doxorubicin(6-maleimidocaproyl)hydrazone) Cat. No.: HY-16261A (Doxorubicin(6-maleimidocaproyl)hydrazone hydrochloride) Cat. No.: HY-16261B

Bioactivity: MC-DOXHZN is an albumin-binding prodrug of Doxorubicin, with Bioactivity: MC-DOXHZN hydrochloride is an albumin-binding prodrug of acid-sensitive properties [1]. Doxorubicin, with acid-sensitive properties [1].

Purity: >98% Purity: >98% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

Mitoxantrone dihydrochloride (mitozantrone) Cat. No.: HY-13502 (mitozantrone dihydrochloride) Cat. No.: HY-13502A

Bioactivity: Mitoxantrone is a topoisomerase II inhibitor; also inhibits Bioactivity: Mitoxantrone dihydrochloride is a topoisomerase II

protein kinase C ( PKC) activity with an IC50 of 8.5 μM. inhibitor; also inhibits protein kinase C ( PKC) activity with an IC50 of 8.5 μM.

Purity: 98.0% Purity: 97.02% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 50 mg, 100 mg

Namitecan (ST-1968) Cat. No.: HY-14821 (THP) Cat. No.: HY-13725

Bioactivity: Namitecan is a potent topoisomerase I inhibitor, with Bioactivity: Pirarubicin is an anthracycline antibiotics, acts as a antitumor property. topoisomerase II inhibitor, and is a widely used for treatment of various cancers, in particular, solid tumors.

Purity: >98% Purity: 99.02% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10 mg, 50 mg, 100 mg

Pirarubicin Hydrochloride (THP Hydrochloride) Cat. No.: HY-13725A (BBR 2778) Cat. No.: HY-13727

Bioactivity: Pirarubicin Hydrochloride is an anthracycline antibiotics, Bioactivity: Pixantrone is a topoisomerase II inhibitor and DNA acts as a topoisomerase II inhibitor, and is a widely used intercalator, with anti-tumor activity. for treatment of various cancers, in particular, solid tumors.

Purity: 96.90% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

160 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Pixantrone dimaleate Podocarpusflavone A (BBR 2778 dimaleate) Cat. No.: HY-13727A Cat. No.: HY-N2198

Bioactivity: Pixantrone dimaleate is a topoisomerase II inhibitor and DNA Bioactivity: Podocarpusflavone A is a DNA topoisomerase I inhibitor, have intercalator, with anti-tumor activity. moderated anti-proliferative activity induce cell apoptosis in MCF-7, is developing anti-tumor drugs target: DNA topoisomerase I In vitro: podocarpusflavone-A show significant inhibitions against DLD, KB, MCF-7, HEp-2 tumor cell lines… Purity: 95.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg

SN-38 SW044248 (NK012) Cat. No.: HY-13704 Cat. No.: HY-19637

Bioactivity: SN-38 (NK012) is an active metabolite of the Topoisomerase I Bioactivity: SW044248 is a non-canonical topoisomerase I inhibitor, and inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines. synthesis with IC50s of 0.077 and 1.3 μM, respectively.

Purity: 99.46% Purity: 99.60% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 200 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

TAS-103 TAS-103 dihydrochloride (BMS-247615) Cat. No.: HY-13758 (BMS-247615 dihydrochloride) Cat. No.: HY-13758A

Bioactivity: TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used Bioactivity: TAS-103 dihydrochloride is a dual inhibitor of DNA for cancer research. topoisomerase I/II, used for cancer research.

Purity: >98% Purity: 99.70% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg, 100 mg

Teniposide Top1 inhibitor 1 (VM26) Cat. No.: HY-13761 Cat. No.: HY-126142

Bioactivity: is a podophyllotoxin derivative, acts as a Bioactivity: Top1 inhibitor 1 (compound 28) is a potent human

topoisomerase II inhibitor, and used as a chemotherapeutic topoisomerase I (Top1) inhibitor with an IC50 value of 29 agent. nM [1].

Purity: 99.84% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 100 mg, 500 mg 25 mg, 50 mg, 100 mg, 200 mg

Topotecan Hydrochloride (SKF 104864A; NSC 609669) Cat. No.: HY-13768 (SKF 104864A (Hydrochloride); NSC 609669 (Hydrochloride)) Cat. No.: HY-13768A

Bioactivity: Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I Bioactivity: Topotecan Hydrochloride (SKF 104864A Hydrochloride; NSC 609669

inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 Hydrochloride) is a Topoisomerase I inhibitor with potent μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of antineoplastic activities. GSCs-U251 and 5.95±0.24 μM of GSCs-U87.

Purity: >98% Purity: 99.20% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 161

Voreloxin Voreloxin Hydrochloride (SNS-595 Hydrochloride; Vosaroxin (SNS-595; Vosaroxin; AG 7352) Cat. No.: HY-10534 Hydrochloride; AG 7352 Hydrochloride) Cat. No.: HY-16518

Bioactivity: Voreloxin is a first-in-class topoisomerase II inhibitor Bioactivity: Voreloxin Hydrochloride is a first-in-class topoisomerase II that intercalates DNA and induces site-selective DNA DSB, G2 inhibitor that intercalates DNA and induces site-selective DNA arrest, and apoptosis. DSB, G2 arrest, and apoptosis.

Purity: >98% Purity: 99.70% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 5 mg, 10 mg, 50 mg Size: 5 mg, 10 mg, 50 mg

β-Lapachone (ARQ-501; NSC-26326) Cat. No.: HY-13555

Bioactivity: β-Lapachone is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.

Purity: 99.98% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

162 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Wee1

Wee1 is a nuclear kinase belonging to the Ser/Thr family of protein kinases in the fission yeast Schizosaccharomyces pombe ( S. pombe). Wee1 has amolecular mass of 96 kDa and it is a key regulator of cell cycle progression. Wee1 influences cell size by inhibiting the entry into mitosis, through inhibiting Cdk1. Wee1 has homologues in many other organisms, including mammals. Wee1 inhibits Cdk1 by phosphorylating it on two different sites, Tyr15 and Thr14. Cdk1 is crucial for the cyclin-dependent passage of the various cell cycle checkpoints. At least three checkpoints exist for which the inhibition

of Cdk1 by Wee1 is important: G 2/M checkpoint, Cell size checkpoint, DNA damage checkpoint. Wee1 is shown to phosphorylate histone H2B at tyrosine 37 residue which regulates global expression of histones.

www.MedChemExpress.com 163 Wee1 Inhibitors & Modulators

Adavosertib PD0166285 (AZD1775; MK-1775) Cat. No.: HY-10993 Cat. No.: HY-13925

Bioactivity: Adavosertib (AZD-1775; MK-1775) is a potent Wee1 inhibitor Bioactivity: PD0166285 is a WEE1 inhibitor and a weak Myt1 inhibitor

with an IC50 of 5.2 nM. with IC50s of 24 and 72 nM, respectively.

Purity: 99.96% Purity: 99.46% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

164 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]