Inhibitors, Agonists, Screening Libraries www.MedChemExpress.com

JAK/STAT Signaling

The (JAK)/signal transducer and activator of transcription (STAT) pathway is central to signaling by receptors, a superfamily of more than 30 transmembrane proteins that recognize specific , and is critical in blood formation and immune response. Canonical JAK/STAT signaling begins with the association of cytokines and their corresponding transmembrane receptors. Activated JAKs then phosphorylate latent STAT monomers, leading to dimerization, nuclear translocation, and DNA binding. In mammals, there are four JAKs (JAK1, JAK2, JAK3, TYK2) and seven STATs (STAT1, STAT2, STAT3, STAT4, STAT5a, STAT5b, STAT6). JAKs are an integral component of the receptor subunit with very little release or exchange into the cytoplasm and as such are located primarily at the plasma membrane. STAT has seven conserved features: an N-terminal domain (NT), a coiled-coil domain (CC), a central DNA-binding domain (DBD), a linker region, an SH2 domain followed by a single conserved tyrosine residue, and a C-terminal transactivation domain (TAD). JAK phosphorylation of the STAT proteins then results in a spatial reorganisation of the dimer complex, and translocates to the nucleus. Once in the nucleus, STAT dimmers are stabilised by NT:NT interactions and bind cooperatively to tandem sequence elements within promoter regions to activate the transcription of specific gene subsets. Aberrant activation of the JAK/STAT pathway has been reported in a variety of diseases, including inflammatory conditions, hematologic malignancies, and solid tumors. More recently, human myeloproliferative neoplasms are discovered to be associated with a unique acquired somatic mutation in JAK2 (JAK2 V617F), rare exon 12 JAK2 mutations, or receptor mutations that constitutively activate wild-type JAK2. As a result, several drug companies have begun to develop therapeutics that inhibit the function of JAK tyrosine kinases. Currently, several JAK-targeting drugs have been used in the clinic for treating diseases including rheumatoid arthritis and myeloproliferative.

References: [1] Kiu H, et al. Growth Factors. 2012 Apr;30(2):88-106. [2] Quintás-Cardama A, et al. Clin Cancer Res. 2013 Apr 15;19(8):1933-40. [3] Villarino AV, et al. J Immunol. 2015 Jan 1;194(1):21-7.

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Target List in JAK/STAT Signaling

• EGFR 3

• JAK 16

• Pim 26

• STAT 30

www.MedChemExpress.com 3 EGFR Epidermal growth factor receptor;ErbB-1;HER1

The EGFR family of receptor tyrosine kinases (RTK) comprises four distinct receptors: the EGFR (also known as ErbB-1/HER1), ErbB-2 (neu, HER2), ErbB-3 (HER3) and ErbB-4 (HER4). All EGFR family members are characterized by a modular structure consisting of an extracellular ligand-binding domain, a single hydrophobic transmembrane region, and the intracellular part harbouring the highly conserved tyrosine kinase domain. The ErbB family of receptor tyrosine kinases (RTKs) couples binding of extracellular growth factor ligands to intracellular signaling pathways regulating diverse biologic responses, including proliferation, differentiation, cell motility, and survival. Ten growth factors and their ErbB specificities are: EGF, amphiregulin (AR), and TGF bind ErbB-1; betacellulin, and epiregulin bind both ErbB-1 and ErbB-4; the neuregulins (also called heregulins and Neu differentiation factors) NRG-1 and NRG-2 bind ErbB-3 and ErbB-4; and NRG-3 and NRG-4 bind ErbB-4. No known ligand binds ErbB-2. The three best characterized signaling pathways induced through ErbBs are Ras-mitogen-activated protein kinase (Ras-MAPK), phosphatidylinositol 3 kinase-protein kinase B (PI3K-PKB/Akt), and phospholipase C-protein kinase C (PLC-PKC) pathways.

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(E)-AG 99 AEE788 ((E)-Tyrphostin 46; (E)-Tyrphostin AG 99) Cat. No.: HY-100962 (NVP-AEE 788) Cat. No.: HY-10045

Bioactivity: (E)-AG 99 ((E)-Tyrphostin 46; (E)-Tyrphostin AG 99) is a Bioactivity: AEE788 is an inhibitor of the EGFR and ErbB2 with IC50 [1] potent EGFR inhibitor . values of 2 and 6 nM, respectively.

Purity: 99.41% Purity: 99.91% 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 5 mg, 10 mg, 50 mg

Afatinib dimaleate (BIBW 2992) Cat. No.: HY-10261 (BIBW 2992MA2) Cat. No.: HY-10261A

Bioactivity: Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor Bioactivity: Afatinib dimaleate is an irreversible EGFR family inhibitor wt wt with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR , with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR , EGFR L858R, EGFR L858R/T790M and HER2, respectively. EGFR L858R, EGFR L858R/T790M and HER2, respectively.

Purity: 99.99% Purity: 99.31% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg, 200 mg 10 mg, 50 mg, 100 mg, 200 mg

AG 555 AG-1478 (Tyrphostin AG 555) Cat. No.: HY-15336 (Tyrphostin AG-1478; NSC 693255) Cat. No.: HY-13524

Bioactivity: AG 555 is an EGFR tyrosine kinase inhibitor. Bioactivity: AG-1478 is a selective EGFR tyrosine kinase inhibitor with

IC50 of 3 nM.

Purity: 98.0% 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 5 mg, 10 mg, 50 mg

AG-490 Allitinib (Tyrphostin AG 490) Cat. No.: HY-12000 (AST-1306; ALS 1306) Cat. No.: HY-15375

Bioactivity: AG-490 is a tyrosine kinase inhibitor that inhibits EGFR, Bioactivity: Allitinib (AST1306) is a selective, irreversible EGFR and

Stat-3 and JAK2/3. ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively.

Purity: 99.84% 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 10 mg, 50 mg, 100 mg, 200 mg

Allitinib tosylate ARRY-380 analog (AST-1306 (TsOH)) Cat. No.: HY-13427 Cat. No.: HY-10531

Bioactivity: Allitinib tosylate (AST-1306 TsOH) is a novel irreversible Bioactivity: ARRY-380 analog is the analog of ARRY-380, ARRY-380 is a inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also potent and selective HER2 inhibitor with IC50 of 8 nM, effective in mutation EGFR T790M/L858R, more potent to equipotent against truncated p95-HER2, 500-fold more selective ErbB2-overexpressing cells, 3000-fold selective for ErbB for HER2 versus EGFR family than other kinases. IC50 value: 0.5/3 nM (EGFR/Erb2)[1]… Purity: 99.23% Purity: 96.42% 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 5 mg, 10 mg, 50 mg, 100 mg

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AST2818 mesylate Astragaloside VI Cat. No.: HY-112870A Cat. No.: HY-N6577

Bioactivity: AST2818 mesylate is an EGFR inhibitor. Bioactivity: Astragaloside VI could activate EGFR/ERK signalling pathway to improve wound healing.

Purity: 99.99% Purity: 98.0% 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

AV-412 AV-412 free base (MP412) Cat. No.: HY-10346 (MP-412 free base) Cat. No.: HY-10346A

Bioactivity: AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, Bioactivity: AV-412 free base (MP-412 free base) is an EGFR inhibitor with L858R L858R T790M IC s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR , 0.79, 2.3, 19 nM for EGFR, EGFR , EGFR , EGFR 50 L858R/T790M and ErbB2, respectively. EGFR T790M, EGFR L858R/T790M and ErbB2, respectively.

Purity: 99.26% Purity: 98.49% 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 5 mg, 10 mg, 50 mg, 100 mg

Avitinib maleate AZ-5104 Cat. No.: HY-19816A Cat. No.: HY-B0793

Bioactivity: Avitinib maleate is a pyrrolopyrimidine-based irreversible Bioactivity: AZ-5104 is an active, demethylated metabolite of AZD 9291.

epidermal growth factor receptor ( EGFR) inhibitor with an AZ-5104 is an EGFR inhibitor with IC50s of 1, 6, 1, 25 and 7 IC of 7.68 nM. 50 nM for EGFR L858R/T790M, EGFR L858R, EGFR L861Q, EGFR and ErbB4, respectively. Purity: 98.0% Purity: 99.70% 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, 200 mg

AZD3759 BGB-102 Cat. No.: HY-18750 (JNJ-26483327) Cat. No.: HY-15732

Bioactivity: AZD3759 is a potent, oral active, central nervous Bioactivity: BGB-102 is a potent multi-kinase inhibitor against EGFR, system-penetrant, EGFR inhibitor. At K ATP m HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM,

concentrations, the IC50s are 0.3, 0.2, and 0.2 nM for EGFR respectively. wt, EGFR L858R, and EGFR exon 19Del, respectively. Purity: 99.49% Purity: >98% Clinical Data: Phase 2 Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 50 mg, 100 mg

BMS-599626 BMS-599626 Hydrochloride (AC480) Cat. No.: HY-10251 (AC480 (Hydrochloride)) Cat. No.: HY-12010

Bioactivity: AC480 (BMS-599626) is a selective and efficacious inhibitor of Bioactivity: BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc. and 30 nM, ~8-fold less potent to HER4, >100-fold to IC50 value: 20 nM (HER1); 30 nM (HER2) [1] Target: HER1/HER2 VEGFR2, c-Kit, Lck, MET etc. IC50 value: 20 nM (HER1); 30 nM in vitro: BMS-599626 inhibited HER1 and HER2 with IC50 of 20… (HER2) [1] Target: HER1/HER2 in vitro: BMS-599626 inhibited… Purity: >98% Purity: 99.82% Clinical Data: Phase 1 Clinical Data: Phase 1 Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 5 mg, 50 mg, 100 mg

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

BMS-690514 Butein Cat. No.: HY-10333 (2’,3,4,4’-tetrahydroxy Chalcone) Cat. No.: HY-16558

Bioactivity: BMS-690514 is a potent and orally active inhibitor of EGFR Bioactivity: Butein, a plant polyphenol isolated from Rhus verniciflua, inhibit the activation of protein tyrosine kinase and EGFR. and VEGFR; has IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively. target: EGFR [1] In vitro: 1) Butein inhibited the activation of AKT, extracellular signal-regulated kinase (ERKs) and p38 kinases in the presence of cisplatin.[2] 2) FoxO3a and its… Purity: 99.37% Purity: 99.95% 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 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

Canertinib Canertinib dihydrochloride (CI-1033; PD-183805) Cat. No.: HY-10367 (CI-1033 dihydrochloride; PD-183805 dihydrochloride) Cat. No.: HY-10367A

Bioactivity: Canertinib (CI-1033;PD-183805) is a potent and irreversible Bioactivity: Canertinib dihydrochloride (CI-1033;PD-183805) is a potent and EGFR inhibitor; inhibits cellular EGFR and ErbB2 irreversible EGFR inhibitor; inhibits cellular EGFR and

autophosphorylation with IC50s of 7.4 and 9 nM. ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM.

Purity: 99.10% Purity: 98.51% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg, 200 mg 10 mg, 50 mg, 100 mg, 200 mg

Cetuximab Chrysophanol (C225) Cat. No.: HY-P9905 (Chrysophanic acid) Cat. No.: HY-13595

Bioactivity: is a monoclonal antibody that inhibits epidermal Bioactivity: Chrysophanol (Chrysophanic acid) is a natural anthraquinone,

growth factor receptor ( EGFR), with a Kd of 0.201 nM for which inhibits EGF-induced phosphorylation of EGFR and soluble EGFR by SPR. Cetuximab has potent antitumor activity. suppresses activation of AKT and mTOR/ p70S6K.

Purity: 99.70% Purity: 99.63% Clinical Data: Launched Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 50 mg, 100 mg

CL-387785 CNX-2006 (EKI-785; WAY-EKI 785) Cat. No.: HY-10325 Cat. No.: HY-13897

Bioactivity: CL-387785(EKI785; WAY-EKI 785) is an irreversible inhibitor of Bioactivity: CNX-2006 is a mutant-selective and irreversible EGFR EGFR with IC of 370 pM. T790M 50 inhibitor with an IC50 below 20 nM for EGFR .

Purity: 97.06% 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, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

CP-724714 CUDC-101 Cat. No.: HY-14674 Cat. No.: HY-10223

Bioactivity: CP-724,714 is a potent, selective inhibitor of HER2/ErbB2 with Bioactivity: CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with

IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IC50s of 4.4, 2.4, and 15.7 nM, respectively. IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc. Phase 2.

Purity: 99.62% Purity: 99.59% 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

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Dacomitinib Daphnetin (PF-00299804; PF-299804) Cat. No.: HY-13272 (7,8-Dihydroxycoumarin) Cat. No.: HY-N0281

Bioactivity: is a specific and irreversible inhibitor of the Bioactivity: Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative

ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 isolated from plants of the Genus Daphne, is a protein kinase inhibitor, with IC s of 7.67 μM, 9.33 μM and 25.01 μM for nM for EGFR, ERBB2, and ERBB4, respectively. 50 EGFR, PKA and PKC in vitro, respectively [1] [2]. Daphne… Purity: 99.83% Purity: 99.55% 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 10 mg, 50 mg, 100 mg

Desmethyl EAI045 (OSI-420; CP-473420) Cat. No.: HY-13256 Cat. No.: HY-100213

Bioactivity: Desmethyl Erlotinib (OSI-420) is an active metabolite of Bioactivity: EAI045 is an allosteric inhibitor of mutant EGFR with IC50s erlotinib, which is a potent EGFR tyrosin kinase inhibitor. of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFR L858R, EGFR T790M and EGFR L858R/T790M at 10 μM ATP, respectively.

Purity: 98.90% 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 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

EGFR-IN-2 EGFR-IN-3 Cat. No.: HY-100520 Cat. No.: HY-19815

Bioactivity: EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective Bioactivity: EGFR-IN-3 is an epidermal growth factor receptor (EGFR) second generation EGFR inhibitor. inhibitor.

Purity: >98% Purity: 99.94% 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, 100 mg

EGFR-IN-5 Epertinib Cat. No.: HY-111415 (S-22611) Cat. No.: HY-107367

Bioactivity: EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, Bioactivity: Epertinib is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with 7.2 nM for EGFR, EGFR L858R, EGFR L858R/T790M, and EGFR IC s of 1.48 nM, 7.15 nM and 2.49 nM, respectively; Epertinib L858R/T790M/C797S, respectively. 50 shows potent antitumor activity.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 100 mg, 250 mg, 500 mg Size: 1 mg

Erlotinib Erlotinib Hydrochloride (CP-358774 (Hydrochloride); NSC (CP-358774; NSC 718781; OSI-774) Cat. No.: HY-50896 718781 (Hydrochloride); OSI-774 (Hydrochloride)) Cat. No.: HY-12008

Bioactivity: Erlotinib is a for the treatment of non-small cell Bioactivity: Erlotinib Hydrochloride inhibits purified EGFR kinase with an

lung cancer. It inhibits purified EGFR kinase with an IC50 of IC50 of 2 nM. 2 nM.

Purity: 99.99% Purity: 99.93% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 100 mg, 500 mg

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Erlotinib mesylate (CP-358774 (mesylate); NSC 718781 Falnidamol (mesylate); OSI-774 (mesylate)) Cat. No.: HY-12008A (BIBX 1382) Cat. No.: HY-10322

Bioactivity: Erlotinib mesylate inhibits purified EGFR kinase with an IC50 Bioactivity: Falnidamol (BIBX 1382) is a potent, selective inhibitor of of 2 nM. EGFR tyrosine kinase (IC 50 = 3 nM); displays > 1000-fold

lower potency against ErbB2 (IC 50 = 3.4 μM) and a range of

other related tyrosine kinases (IC 50 > 10 μM). Purity: >98% Purity: 98.07% Clinical Data: Launched Clinical Data: Phase 1 Size: 100 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

FIIN-3 Cat. No.: HY-18603 (ZD1839) Cat. No.: HY-50895

Bioactivity: FIIN-3 is an irreversible inhibitor of FGFR with an IC50 of Bioactivity: Gefitinib (ZD1839) is a EGFR tyrosine kinase inhibitor, with IC of 2-37 nM in NR6wtEGFR cells. 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, 50 respectively.

Purity: 98.24% Purity: 99.70% 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, 50 mg, 100 mg 100 mg, 500 mg, 1 g, 5 g

Gefitinib hydrochloride Gefitinib-based PROTAC 3 (ZD-1839 hydrochloride) Cat. No.: HY-50895A Cat. No.: HY-123921

Bioactivity: Gefitinib hydrochloride is an inhibitor that specifically Bioactivity: Gefitinib-based PROTAC 3, conjugating an EGFR binding element

binds and inhibits the EGFR tyrosine kinase, with the IC50 to a VHL ligand via a linker, induces EGFR degradation with DC s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and value of 2-37 nM in NR6wtEGFR cells. 50 H3255 (L858R mutantion) cells, respectively [1]. Purity: 99.80% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg, 1 g, 5 g 5 mg, 10 mg

Genistein HS-10296 hydrochloride (NPI 031L) Cat. No.: HY-14596 Cat. No.: HY-112823B

Bioactivity: Genistein, a soy isoflavone, is a multiple tyrosine kinases Bioactivity: HS-10296 hydrochloride is an orally available and inhibitor which acts as a chemotherapeutic agent against third-Generation inhibitor of epidermal growth factor receptor different types of cancer, mainly by altering , the (EGFR)-activating mutations and T790M-resistant mutation cell cycle, and angiogenesis and inhibiting metastasis. with limited activity against wild-type EGFR.

Purity: 99.68% Purity: 98.05% 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 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Icotinib Hydrochloride (BPI-2009) Cat. No.: HY-15164A (BPI-2009H) Cat. No.: HY-15164

Bioactivity: Icotinib (BPI-2009) is a potent and specific EGFR inhibitor Bioactivity: Icotinib Hydrochloride (BPI-2009) is a potent and specific L858R EGFR inhibitor with an IC of 5 nM; also inhibits mutant with an IC50 of 5 nM; also inhibits mutant EGFR , EGFR 50 L858R L858R/T790M T790M L858R/T790M, EGFR T790M and EGFR L861Q. EGFR , EGFR , EGFR and EGFR L861Q. Purity: 99.80% Purity: 99.99% Clinical Data: Launched 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

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Lapatinib ditosylate (GW572016) Cat. No.: HY-50898 (GW-572016 ditosylate) Cat. No.: HY-50898A

Bioactivity: Lapatinib (GW572016) is a potent EGFR and ErbB2 inhibitor Bioactivity: Lapatinib ditosylate is a potent EGFR and ErbB2 inhibitor

with IC50s of 10.2 and 9.8 nM, respectively. with IC50 of 10.2 and 9.8 nM, respectively.

Purity: 99.83% Purity: 98.58% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 500 mg, 1 g 50 mg, 100 mg, 500 mg, 1 g

Lavendustin A Lazertinib (RG-14355) Cat. No.: HY-18963 (YH25448; GNS-1480) Cat. No.: HY-109061

Bioactivity: Lavendustin A (RG-14355), isolated from Streptomyces Bioactivity: Lazertinib is a potent, highly mutant-selective, blood-brain Griseolavendus, is a potent, specific and ATP-competitive barrier permeable, orally available and irreversible

inhibitor of tyrosine kinase, with an IC50 of 11 ng/mL for third-generation EGFR tyrosine kinase inhibitor, and can be used in the research of non-small cell lung cancer. EGFR-associated tyrosine kinase [1]. It suppres… Purity: >98% Purity: 99.25% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 25 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Lifirafenib MTX-211 (BGB-283) Cat. No.: HY-18957 Cat. No.: HY-107364

Bioactivity: Lifirafenib (BGB-283) is a novel and potent Raf Kinase and Bioactivity: MTX-211 is a dual inhibitor of EGFR and PI3K, used for the

EGFR inhibitor with IC50 values of 23 and 29 nM for treatment of cancer and other diseases. recombinant BRaf V600E and EGFR, respectively.

Purity: 98.00% Purity: 98.65% 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, 100 mg

Mubritinib Mutant EGFR inhibitor (TAK-165) Cat. No.: HY-13501 Cat. No.: HY-13984

Bioactivity: Mubritinib (TAK-165) is a potent and selective EGFR2/HER2 Bioactivity: Mutant EGFR inhibitor is a potent and selective mutant EGFR

inhibitor with an IC50 of 6 nM. inhibitor extracted from patent WO 2013014448 A1; inhibits EGFR L858R, EGFR Exon 19 deletion and EGFR T790M.

Purity: 99.97% Purity: 98.94% 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, 50 mg, 100 mg

Mutated EGFR-IN-1 Naquotinib Cat. No.: HY-78869 (ASP8273) Cat. No.: HY-19729

Bioactivity: Mutated EGFR-IN-1 is a useful intermediate for the inhibitors Bioactivity: Naquotinib (ASP8273) is an orally available, mutant-selective

design for mutated EGFR, such as L858R EGFR, Exonl9 deletion and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward activating mutant and T790M resistance mutant. IC50 value: EGFR mutants and 230 nM for EGFR. Target: Mutated EGFR inhibitor More information can be found in Patent WO 2013014448 A1.2 - (2, 4, 5 - substituted… Purity: 99.88% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

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

Naquotinib mesylate Nazartinib (ASP8273 (mesylate)) Cat. No.: HY-19803 (EGF816) Cat. No.: HY-12872

Bioactivity: Naquotinib mesylate (ASP8273 mesylate) is an orally available, Bioactivity: Nazartinib (EGF816) is a novel, covalent mutant-selective mutant-selective and irreversible EGFR inhibitor; with IC s −1 50 EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min of 8-33 nM toward EGFR mutants and 230 nM for EGFR. on EGFR(L858R/790M) mutant, respectively.

Purity: 98.59% Purity: 99.57% Clinical Data: Phase 3 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

Nazartinib mesylate (EGF816 (mesylate)) Cat. No.: HY-12872A (HKI-272) Cat. No.: HY-32721

Bioactivity: Nazartinib mesylate (EGF816 mesylate) is a novel, covalent Bioactivity: Neratinib is an orally available, irreversible tyrosine kinase mutant-selective EGFR inhibitor, with K and K of 31 nM i inact inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, and 0.222 min −1 on EGFR(L858R/790M) mutant, respectively. respectively.

Purity: >98% Purity: 98.84% Clinical Data: Phase 2 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, 200 mg

NRC-2694 NSC 228155 Cat. No.: HY-19909 Cat. No.: HY-101084

Bioactivity: NRC-2694 is an epidermal growth factor receptor ( EGFR) Bioactivity: NSC 228155 is an activator of EGFR, binds to the antagonist with anti-cancer and anti-proliferative properties. extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR [1]. NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from… Purity: 98.40% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Olmutinib (HM61713, BI 1482694) Cat. No.: HY-19730 (AZD-9291; Mereletinib) Cat. No.: HY-15772

Bioactivity: (HM61713; BI-1482694) is an irreversible EGFR Bioactivity: Osimertinib (AZD-9291) is an irreversible and mutant selective tyrosine kinase inhibitor that binds to a cysteine residue L858R EGFR inhibitor with IC50s of 12 and 1 nM against EGFR near the kinase domain. and EGFR L858R/T790M, respectively.

Purity: 99.95% Purity: 99.95% 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, 200 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g

Osimertinib dimesylate Osimertinib mesylate (AZD-9291 (dimesylate); Mereletinib (dimesylate)) Cat. No.: HY-79077 (AZD-9291 mesylate; Mereletinib mesylate) Cat. No.: HY-15772A

Bioactivity: Osimertinib dimesylate (AZD-9291 dimesylate) is an Bioactivity: Osimertinib mesylate (AZD-9291 mesylate) is an irreversible

irreversible and mutant selective EGFR inhibitor with IC50s and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M, against EGFR L858R and EGFR L858R/T790M, respectively. respectively. Purity: 99.96% Purity: 99.96% Clinical Data: Launched Clinical Data: Launched Size: 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg Size: 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g

www.MedChemExpress.com 11

PD153035 PD153035 Hydrochloride (SU-5271 (Hydrochloride); AG1517 (SU-5271; AG1517; ZM 252868) Cat. No.: HY-14346 (Hydrochloride); ZM 252868 (Hydrochloride)) Cat. No.: HY-12013

Bioactivity: PD153035 (SU-5271; AG1517; ZM 252868) is a potent EGFR Bioactivity: PD153035 Hydrochloride (SU-5271 Hydrochloride) is a potent EGFR inhibitor with K and IC of 6 and 25 pM, respectively. inhibitor with Ki and IC50 of 6 and 25 pM, respectively. i 50

Purity: 98.66% Purity: 98.62% 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 5 mg, 10 mg, 50 mg, 100 mg

PD158780 PD168393 Cat. No.: HY-18609 Cat. No.: HY-13896

Bioactivity: PD158780 is a potent EGFR family inhibitor with IC50s of 8 Bioactivity: PD168393 is an potent, cell-permeable, irreversible EGFR pM, 49, 52, 52 nM for EGFR, ErbB2, ErbB3, and ErbB4, inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773, respectively. inactive against insulin, PDGFR, FGFR and PKC. target: EGFR IC 50: 0.7 nM [1] (1) PD 168393 inhibite EGFr autophosphorylation in A431 human epidermoid carcinoma cells with >9-fold… Purity: 98.04% 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, 10 mg, 50 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg

Pelitinib (EKB-569; WAY-EKB 569) Cat. No.: HY-32718 Cat. No.: HY-P9912

Bioactivity: Pelitinib (EKB-569;WAY-EKB 569) is an irreversible inhibitor Bioactivity: Pertuzumab, a humanized monoclonal antibody, is a HER2

of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, dimerization inhibitor for the treatment of metastatic HER2-positive breast cancer. MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively. Purity: 98.18% Purity: 99.10% Clinical Data: Phase 2 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

PF-06459988 Poziotinib Cat. No.: HY-19985 (HM781-36B; NOV120101) Cat. No.: HY-15730

Bioactivity: PF-06459988 is an irreversible inhibitor of T790M-Containing Bioactivity: Poziotinib(NOV120101; HM781-36B) is an irreversible Pan-HER EGFR Mutants. inhibitor with IC50s of 3/5/23 nM for HER1/HER2/HER4 respectively. IC50 value: 3/5/23 nM(HER1/HER2/HER4) [1] Target: pan-HER inhibitor in vitro: The IC50 levels of HM781-36B for N87 and SNU216 were 0.001 and 0.004 μmol/L,… Purity: 98.72% Purity: 99.92% 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, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Pyrotinib Pyrotinib dimaleate (SHR-1258) Cat. No.: HY-104065 (SHR-1258 dimaleate) Cat. No.: HY-104065B

Bioactivity: Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual Bioactivity: Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and

inhibitor with IC50s of 13 and 38 nM, respectively. selective EGFR/HER2 dual inhibitor with IC50 s of 13 and 38 nM, respectively.

Purity: 98.84% Purity: 98.60% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 25 mg, 50 mg Size: 10mM x 1mL in Water, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

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

RG13022 RG14620 (Tyrphostin RG13022; ) Cat. No.: HY-101429 (Tyrphostin RG14620) Cat. No.: HY-101426

Bioactivity: RG13022 is a tyrosine kinase inhibitor; inhibits the Bioactivity: RG14620 is an EGFR inhibitor with an IC50 of 3 μM. autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.

Purity: 98.0% Purity: 98.98% 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

Rociletinib hydrobromide (CO-1686 (hydrobromide); AVL-301 (CO-1686; AVL-301; CNX-419) Cat. No.: HY-15729 hydrobromide; CNX-419 hydrobromide) Cat. No.: HY-15729A

Bioactivity: Rociletinib (CO-1686) is an orally delivered kinase inhibitor Bioactivity: Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally that specifically targets the mutant forms of EGFR including delivered kinase inhibitor that specifically targets the

T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are mutant forms of EGFR including T790M, and the Ki values for 21.5 nM and 303.3 nM, respectively. EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively. Purity: 99.08% Purity: 97.45% Clinical Data: Phase 3 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, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

Sapitinib TAK-285 (AZD-8931) Cat. No.: HY-13050 Cat. No.: HY-15196

Bioactivity: Sapitinib (AZD-8931) is a reversible, ATP competitive EGFR Bioactivity: TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively. than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc.

Purity: 99.99% Purity: 99.16% 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 tarloxotinib bromide TAS0728 (TH-4000; PR-610) Cat. No.: HY-17632 Cat. No.: HY-111553

Bioactivity: Tarloxotinib bromide is an irreversible EGFR/HER2 inhibitor. Bioactivity: TAS0728 is a potent, selective, oral active, irreversible and covalent-binding HER2 inhibitor, binds to HER2 at C805,

inhibits its kinase activity, with an IC50 of 13 nM. TAS0728

shows IC50s of 4.9, 8.5, 31, 65, 33, 25, 86 and 36 nM for B… Purity: 98.97% 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

TAS6417 Tesevatinib Cat. No.: HY-112299 (XL-647; EXEL-7647; KD-019) Cat. No.: HY-13314

Bioactivity: TAS6417 is an EGFR inhibitor and an efficacious drug Bioactivity: Tesevatinib (XL-647) is an orally available, multi-target

candidate for patients with NSCLC, with IC50 values ranging tyrosine kinase inhibitor; inhibits EGFR, ErbB2, KDR, Flt4 and EphB4 kinase with IC s of 0.3, 16, 1.5, 8.7, and 1.4 nM. from 1.1-8.0 nM. 50

Purity: 99.55% Purity: 99.21% 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, 25 mg, 50 mg, 100 mg 5 mg, 10 mg

www.MedChemExpress.com 13

Trastuzumab (Anti-Human HER2, Humanized Antibody) Cat. No.: HY-P9907 (Irbinitinib; ARRY-380; ONT-380) Cat. No.: HY-16069

Bioactivity: is a humanized monoclonal antibody for patients Bioactivity: Tucatinib (Irbinitinib; ARRY-380; ONT-380) is a potent and

with invasive breast cancers that overexpress HER2. selective HER2 inhibitor with an IC50 of 8 nM. Trastuzumab has been clinically used to treat HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer.

Purity: 99.30% Purity: 98.53% Clinical Data: Launched Clinical Data: Phase 1 Size: 1 mg, 5 mg, 25 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

TX1-85-1 Tyrphostin 23 Cat. No.: HY-100848 (Tyrphostin A23; RG-50810; AG 18) Cat. No.: HY-15644

Bioactivity: TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an Bioactivity: Tyrphostin 23 (Tyrphostin A23) is an EGFR inhibitor with an

IC50 of 23 nM and is also the first selective Her3 ligand, IC50 and Kiof 35 and 11 μM, respectively. which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradat…

Purity: 98.0% 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, 1 mg, 5 mg, 10 mg 10 mg, 50 mg

Tyrphostin AG 528 Tyrphostin AG 879 (Tyrphostin B66; AG 528) Cat. No.: HY-100499 (AG 879) Cat. No.: HY-20878

Bioactivity: Tyrphostin AG 528 is an inhibitor of EGFR and ErbB2 with Bioactivity: TyrphostinAG879 is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation, but not TrKB and TrKC.[1] also a ErbB2 IC50s of 4.9 and 2.1 μM, respectively. kinase inhibitor, has at least 500-fold higher selectivity to ErbB2 (IC50 = 1 μmol/L) than EGFR (IC50 >500 μmol/L). target: TrKA [1], ErbB2 [2]. IC 50: ErbB2 1 μmol/L [2]. In… Purity: 98.0% 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, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg

Varlitinib WHI-P154 (ARRY-334543; ASLAN001) Cat. No.: HY-10530 Cat. No.: HY-13895

Bioactivity: Varlitinib (ARRY-334543; ASLAN001) is a potent, reversible, Bioactivity: WHI-P154 is a potent EGFR inhibitor, and also modestly blocks small molecule pan- EGFR inhibitor with IC s of 7, 2, 4 nM 50 JAK3, with IC50s of 4 nM and 1.8 μM, respectively. for HER1, HER2 and HER4, respectively.

Purity: 98.0% Purity: 98.60% 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 10 mg, 50 mg

WHI-P180 WHI-P180 hydrochloride (Janex 3) Cat. No.: HY-15769 (Janex 3 hydrochloride; ) Cat. No.: HY-15769A

Bioactivity: WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, Bioactivity: WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET,

KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively. respectively.

Purity: >98% Purity: >98% 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 2 mg, 5 mg, 10 mg, 50 mg

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

WZ-3146 WZ4002 Cat. No.: HY-12001 Cat. No.: HY-12026

Bioactivity: WZ3146 is a mutant selective EGFR inhibitor with IC50s of 2, Bioactivity: WZ4002 is a mutant selective EGFR inhibitor with IC50s of 2, 2, 5, 14 and 66 nM for EGFR L858R, EGFR L858R/T790M, EGFR 8, 3 and 2 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750, EGFR E746_A750/T790M and EGFR, respectively. E746_A750 and EGFR E746_A750/T790M, respectively.

Purity: 99.07% 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, 50 mg 10 mg, 50 mg, 100 mg

WZ8040 ZD-4190 Cat. No.: HY-12029 Cat. No.: HY-U00002

Bioactivity: WZ8040 is a novel mutant-selective irreversible EGFRT790M Bioactivity: ZD-4190 is a potent, orally available inhibitor of the inhibitor, does not inhibit ERBB2 phosphorylation (T798I). vascular endothelial cell growth factor receptor 2 ( VEGFR2) and of epidermal growth factor receptor ( EGFR) signalling, used for the treatment of cancer.

Purity: >98% Purity: 99.20% 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

www.MedChemExpress.com 15 JAK Janus kinase

Janus kinase (JAK) is a family of intracellular, nonreceptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway. Since members of the type I and type II families possess no catalytic kinase activity, they rely on the JAK family of tyrosine kinases to phosphorylate and activate downstream proteins involved in their signal transduction pathways. The receptors exist as paired polypeptides, thus exhibiting two intracellular signal-transducing domains. JAKs associate with a proline-rich region in each intracellular domain, which is adjacent to the cell membrane and called a box1/box2 region. After the receptor associates with its respective cytokine/ligand, it goes through a conformational change, bringing the two JAKs close enough to phosphorylate each other. The JAK autophosphorylation induces a conformational change within itself, enabling it to transduce the intracellular signal by further phosphorylating and activating transcription factors called STATs. The activated STATs dissociate from the receptor and form dimers before translocating to the cell nucleus, where they regulate transcription of selected genes.

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

(3R,4S)- (3S,4R)-Tofacitinib Cat. No.: HY-40354D Cat. No.: HY-40354B

Bioactivity: (3R,4S)-Tofacitinib is an enantiomer of Tofacitinib. Bioactivity: (3S,4R)-Tofacitinib is an enantiomer of Tofacitinib.

Tofacitinib inhibits JAK3 with IC50 of 1 nM. Tofacitinib inhibits JAK3 with IC50 of 1 nM.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg Size: 5 mg

(3S,4S)-Tofacitinib Abrocitinib Cat. No.: HY-40354C (PF-04965842) Cat. No.: HY-107429

Bioactivity: (3S,4S)-Tofacitinib is the S-enantiomer of Tofacitinib. Bioactivity: Abrocitinib (PF-04965842) is a potent, orally active and

Tofacitinib inhibits JAK3 with IC50 of 1 nM. selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842)

exhibits less active effect on TYK2 ( IC50, 1.253 μM), … Purity: >98% Purity: 99.79% 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

AT9283 Atractylenolide I Cat. No.: HY-50514 Cat. No.: HY-N0201

Bioactivity: AT9283 is a multitargeted kinase inhibitor which potently Bioactivity: Atractylenolide I is a sesquiterpene derived from the rhizome

inhibits aurora kinase A/B, JAK2/3 ( IC50=1.2 nM, 1.1 nM). of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and… Purity: 99.13% Purity: 99.08% 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

AZ-3 AZ960 Cat. No.: HY-112442 Cat. No.: HY-10411

Bioactivity: AZ-3 is a potent and selective JAK1 inhibitor with an IC50 of Bioactivity: AZ960 is a potent and specific inhibitor of the JAK2 kinase with a K of 0.45 nM. 34 nM. i

Purity: >98% Purity: 98.04% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 1 mg, 2 mg, 5 mg, 10 mg, 50 mg

AZD-1480 Cat. No.: HY-10193 (INCB028050; LY3009104) Cat. No.: HY-15315

Bioactivity: AZD-1480 is an ATP-competitive inhibitor of JAK1 and JAK2 Bioactivity: Baricitinib is a selective and orally bioavailable JAK1 and

with IC50s of 1.3 and <0.4nM, respectively. JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.

Purity: 99.37% Purity: 99.93% 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, 200 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

www.MedChemExpress.com 17

Baricitinib phosphate BMS-066 (INCB028050 (phosphate); LY3009104 (phosphate)) Cat. No.: HY-15315A Cat. No.: HY-18710

Bioactivity: Baricitinib phosphate is a selective orally bioavailable Bioactivity: BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 JAK1/ JAK2 inhibitor with IC of 5.9 nM and 5.7 nM, 50 nM and 72 nM, respectively. respectively.

Purity: 99.49% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

BMS-911543 CEP-33779 Cat. No.: HY-15270 Cat. No.: HY-15343

Bioactivity: BMS-911543 is a selective JAK2 inhibitor, with IC50s of 1.1 Bioactivity: CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC50 of 1.8±0.6 nM. nM, less selective at JAK1, JAK3 and TYK2 ( IC50, 75, 360, 66 nM, respectively).

Purity: 98.12% Purity: 98.04% 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

Cerdulatinib CHZ868 (PRT062070; PRT2070) Cat. No.: HY-15999 Cat. No.: HY-18960

Bioactivity: Cerdulatinib (PRT062070) is a dual JAK and SYK inhibitor Bioactivity: CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in with IC s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, 50 EPOR JAK2 WT Ba/F3 cell. respectively.

Purity: 99.00% Purity: 98.33% 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, 200 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Cucurbitacin I (Elatericin B; JSI-124; NSC-521777) Cat. No.: HY-N1405 (VX-509; VRT-831509) Cat. No.: HY-12469

Bioactivity: I is a natural selective inhibitor of Bioactivity: Decernotinib is a potent, orally active JAK3 inhibitor, with JAK2/STAT3, with potent anti-cancer activity. Kis of 2.5, 11, 13 and 11 nM for JAK3, JAK1, JAK2, and TYK2, respectively.

Purity: 98.0% Purity: 98.91% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg

Delgocitinib (JTE-052) Cat. No.: HY-109053 (TG-101348; SAR 302503) Cat. No.: HY-10409

Bioactivity: Delgocitinib is a novel and specific JAK inhibitor with IC50s Bioactivity: Fedratinib (TG-101348) is a selective inhibitor of JAK2 with an IC of 3 nM, showing 35- and 334-fold selectivity over of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, 50 respectively. JAK1 and JAK3, respectively.

Purity: 99.14% Purity: 98.62% 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, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

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

Filgotinib FLLL32 (GLPG0634) Cat. No.: HY-18300 Cat. No.: HY-100544

Bioactivity: (GLPG0634) is a selective JAK1 inhibitor with IC50 Bioactivity: FLLL32, a synthetic analog of curcumina, is a JAK2/STAT3 dual [1] [2] of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and inhibitor with anti-tumor activity . TYK2, respectively.

Purity: 99.64% Purity: 99.78% 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, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

FM381 Gandotinib Cat. No.: HY-102046 (LY2784544) Cat. No.: HY-13034

Bioactivity: FM381 is a potent covalent reversible inhibitor of JAK3 Bioactivity: Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 targeting the unique Cys909 at the gatekeeper position +7 in of 3 nM. Gandotinib (LY2784544) also inhibits FLT3, FLT4, JAK3. FM-381 has an IC of 127 pM for JAK3, with 410, 2700 50 FGFR2, TYK2, and TRKB with IC 50 of 4, 25, 32, 44, and 95 nM. and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively. Purity: 98.41% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

GLPG0634 analog Gusacitinib Cat. No.: HY-13961 (ASN-002) Cat. No.: HY-103018

Bioactivity: GLPG0634 (analog) (compound176)is a pan JAK inhibitor with Bioactivity: Gusacitinib (ASN-002) is a potent dual inhibitor of spleen

IC50s of 50-200 nM for JAK1/JAK2/JAK3; more information can be tyrosine kinase ( SYK) and janus kinase ( JAK) with IC50 found in the reference patents. values of 5-46 nM.

Purity: 98.00% Purity: 99.41% 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 5 mg, 10 mg, 50 mg

Ilginatinib Ilginatinib hydrochloride (NS-018) Cat. No.: HY-19631A (NS-018 hydrochloride) Cat. No.: HY-19631B

Bioactivity: Ilginatinib (NS-018) is a highly active and orally Bioactivity: Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly

bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, active and orally bioavailable JAK2 inhibitor, with an IC50

54-, and 31-fold selectivity for JAK2 over JAK1 ( IC50, 33 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 ( IC50, 33 nM), JAK3 ( IC50, 39 nM), and Tyk2 ( IC50,… nM), JAK3 ( IC50, 39 nM), and Tyk2 ( IC50, 22 nM). Purity: 95.88% Purity: 98.02% 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

Ilginatinib maleate Itacitinib (NS-018 (maleate)) Cat. No.: HY-19631 (INCB039110) Cat. No.: HY-16997

Bioactivity: Ilginatinib (maleate) (NS-018 (maleate)) is a highly active Bioactivity: Itacitinib is a potent and selective inhibitor of JAK1, with

and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 >20-fold selectivity for JAK1 over JAK2 and >100-fold nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 ( over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis. IC50, 33 nM), JAK3 ( IC50, 39 nM), and Tyk2 ( IC50, 22 nM). Purity: 97.04% Purity: 99.87% Clinical Data: Phase 2 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 1 mg, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

www.MedChemExpress.com 19

Itacitinib adipate JAK-IN-1 Cat. No.: HY-16997A Cat. No.: HY-13827

Bioactivity: Itacitinib adipate is a selective JAK1 inhibitor which has Bioactivity: JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and been tested for efficacy and safety in a phase II trial in 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for myelofibrosis. JAK3 over JAK1.

Purity: 99.37% 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, 50 mg, 100 mg

JAK-IN-3 JAK-IN-4 Cat. No.: HY-111750 Cat. No.: HY-111749

Bioactivity: JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC50 Bioactivity: JAK-IN-4 is a prodrug of a JAK inhibitor, effective in murine [1] values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and collagen induced arthritis model . JAK2, respectively [1].

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

JAK-IN-5 JAK/HDAC-IN-1 Cat. No.: HY-111471 Cat. No.: HY-126141

Bioactivity: JAK inhibitor 1 is an inhibitor of JAK extracted from patent Bioactivity: JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits US20170121327A1, compound example 283. antiproliferative and proapoptotic activities in several

hematological cell lines. JAK/HDAC-IN-1 shows IC50s of 4 and 2 nM for JAK2 and HDAC, respectively [1]. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 100 mg, 250 mg, 500 mg

JAK1-IN-3 JAK1-IN-4 Cat. No.: HY-107361 Cat. No.: HY-116505

Bioactivity: JAK1-IN-3 is a selective JAK1 inhibitor, with an IC50 of 73 Bioactivity: JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and nM, weakly inhibits JAK2, and shows little inhibition on JAK3 50

( IC50, >14.7, >30 μM, respectively). JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation [1] in NCI-H 1975 cells (IC 50, 227 nM) . Purity: 99.32% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 250 mg, 500 mg

JAK3 covalent inhibitor-1 JAK3-IN-1 Cat. No.: HY-119935 Cat. No.: HY-19544

Bioactivity: JAK3 covalent inhibitor-1 is a potent and selective janus Bioactivity: JAK3-IN-1 is a potent JAK3 inhibitor with IC50 of 4.8 nM, also

kinase 3 (JAK3) covalent inhibitor with an IC50 of 11 nM and inhibits JAK1 (IC50 = 896 nM) and JAK2 (IC50 = 1050 nM). IC50 value: 4.8 nM [1] Target: JAK3 in vitro: JAK3-IN-1 provides a shows 246-fold selectivity vs other JAKs [1]. set of useful tools to pharmacologically interrogate JAK3-dependent biology. JAK3-IN-1 completely inhibits IL-4… Purity: >98% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

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

JAK3-IN-6 JAK3-IN-7 Cat. No.: HY-101976 Cat. No.: HY-U00390

Bioactivity: JAK3-IN-6 is a potent, selective irreversible Janus Associated Bioactivity: JAK3-IN-7 is a potent and selective JAK3 inhibitor extracted Kinase 3 (JAK3) inhibitor, with an IC of 0.15 nM. 50 from patent WO2011013785A1, has an IC50 of <0.01 μM.

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

JANEX-1 (WHI-P131; Jak3 inhibitor I) Cat. No.: HY-15508 (CEP-701; KT-5555) Cat. No.: HY-50867

Bioactivity: JANEX-1 is a potent and specific JAK3 inhibitor (estimated Bioactivity: Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor Ki=2.3 μM). JANEX-1 (WHI-P131) shows potent JAK3-inhibitory tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA activity ( IC50 of 78 μM), does not inhibit JAK1 and JAK2. with IC50s of 0.9, 3 and less than 25 nM, respectively.

Purity: 99.84% 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, 50 mg 1 mg, 5 mg

LFM-A13 Cat. No.: HY-18009 (CYT387) Cat. No.: HY-10961

Bioactivity: LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits Bioactivity: Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC a of 11 nM and 18 nM,respectively. CYT387 recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 50 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family shows much less activity against JAK3. kinase HCK, EGFR and IRK.

Purity: 99.70% Purity: 98.11% 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 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

Momelotinib Mesylate Momelotinib sulfate (CYT387 (Mesylate)) Cat. No.: HY-10963 (CYT387 (sulfate salt)) Cat. No.: HY-10962

Bioactivity: Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive Bioactivity: Momelotinib sulfate (CYT387 sulfate) is an ATP-competitive

inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold

selectivity versus JAK3. selectivity versus JAK3 (IC 50=155 nM).

Purity: >98% Purity: 96.0% 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, 100 mg

NSC 42834 NVP-BSK805 (JAK2 Inhibitor V; Z3) Cat. No.: HY-15480 (BSK 805) Cat. No.: HY-14722

Bioactivity: NSC 42834 a novel specific inhibitor of Jak2, inhibits Bioactivity: NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC50s Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK manner but was not cytotoxic to cells at concentrations that homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively. inhibited kinase activity.

Purity: 95.5% 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

www.MedChemExpress.com 21

NVP-BSK805 dihydrochloride maleate (BSK805 dihydrochloride) Cat. No.: HY-14722A (PF-03394197 maleate) Cat. No.: HY-13577A

Bioactivity: NVP-BSK805 dihydrochloride is an ATP-competitive JAK2 Bioactivity: Oclacitinib maleate is a novel JAK inhibitor. Oclacitinib is

inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and most potent at inhibiting JAK1 ( IC50=10 nM). 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.

Purity: 99.36% Purity: 99.53% 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

Pacritinib PF-06651600 (SB1518) Cat. No.: HY-16379 Cat. No.: HY-100754

Bioactivity: is a potent inhibitor of both wild-type JAK2 (IC Bioactivity: PF-06651600 is a potent JAK3-selective inhibitor with an IC50 V617F 50=23 nM) and JAK2 mutant (IC 50=19 nM). Pacritinib of 33.1 nM. D835Y also inhibits FLT3 (IC 50=22 nM) and its mutant FLT3

(IC 50=6 nM). Purity: 99.66% Purity: 99.98% 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

PF-06700841 PF-06700841 P-Tosylate Cat. No.: HY-112708 Cat. No.: HY-112708A

Bioactivity: PF-06700841 is a dual JAK1 and TYK2 inhibitor with IC50s of Bioactivity: PF-06700841 P-Tosylate is a dual JAK1 and TYK2 inhibitor with IC s of 17 and 23 nM, respectively. Anti-inflammatory 17 and 23 nM, respectively. Anti-inflammatory activity [1]. 50 activity [1].

Purity: >98% Purity: 99.66% 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

Protosappanin A Pyridone 6 (PTA) Cat. No.: HY-113573 (CMP 6; JAK Inhibitor) Cat. No.: HY-14435

Bioactivity: Protosappanin A (PTA), an immunosuppressive ingredient and Bioactivity: Pyridone 6 is a pan-JAK inhibitor, which potently inhibits major biphenyl compound isolated from Caesalpinia sappan L, the JAK kinase family, with IC50s of 1 nM for JAK2 and TYK2, suppresses JAK2/STAT3-dependent inflammation pathway through 5 nM for JAK3, and 15 nM for JAK1, while displaying [1] down-regulating the phosphorylation of JAK2 and STAT3 . significantly weaker affinities (130 nM to >10 mM) for other protein tyrosine kinases. Purity: 98.88% Purity: 98.04% Clinical Data: Clinical Data: No Development Reported Size: 5 mg Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 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

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

Ruxolitinib phosphate (INCB018424) Cat. No.: HY-50856 (INCB018424 phosphate) Cat. No.: HY-50858

Bioactivity: Ruxolitinib is a potent and selective JAK1/2 inhibitor with Bioactivity: Ruxolitinib phosphate is a potent JAK1/2 inhibitor with IC50s IC s of 3.3 nM and 2.8 nM in cell-free assays, and has 50 of 3.3 nM/2.8 nM, respectively, showing more than 130-fold 130-fold selectivity for JAK1/2 over JAK3. selectivity over JAK3.

Purity: 99.99% Purity: 99.89% 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, 1 g 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g

Ruxolitinib S enantiomer Ruxolitinib sulfate (S-Ruxolitinib; INCB18424) Cat. No.: HY-50856A (INCB018424 sulfate) Cat. No.: HY-50859

Bioactivity: Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib. Bioactivity: Ruxolitinib sulfate is the first potent, selective JAK1/2 Ruxolitinib is the first potent, selective JAK1/2 inhibitor inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and to enter the clinic with IC of 3.3 nM/2.8 nM in cell-free 50 has > 130-fold selectivity for JAK1/2 versus JAK3. assays.

Purity: 99.88% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg

SAR-20347 SB1317 Cat. No.: HY-100895 (TG02) Cat. No.: HY-15166

Bioactivity: SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 Bioactivity: SB1317 is a potent inhibitor of CDK2, JAK2, and FLT3 for

with IC50s of 0.6, 23, 26 and 41 nM, respectively. the treatment of cancer, with IC50 of 13, 73, and 56 nM for CDK2, JAK2 and FLT3, respectively.

Purity: 97.00% 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, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Solcitinib TG101209 (GSK-2586184; GLPG-0778) Cat. No.: HY-16755 Cat. No.: HY-10410

Bioactivity: Solcitinib is an orally active, competitive, potent, selective Bioactivity: TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, JAK1 inhibitor, with an IC50 of 9.8 nM, and 11-, 55- and less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 23-fold selectivity over JAK2, JAK3 and TYK2, respectively; 30-fold selective for JAK2 than JAK3, and sensitive to Solcitinib is used in the research of moderate-to-severe JAK2V617F and MPLW515L/K mutations. plaque-type psoriasis. Purity: 99.42% Purity: 98.94% 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, 100 mg, 200 mg 5 mg, 10 mg, 50 mg, 100 mg

Tofacitinib Tofacitinib citrate (Tasocitinib; CP-690550) Cat. No.: HY-40354 (Tasocitinib citrate; CP-690550 citrate) Cat. No.: HY-40354A

Bioactivity: Tofacitinib is a JAK3/2/1 inhibitor with IC50s of 1, 20, and Bioactivity: Tofacitinib citrate is a JAK1/2/3 inhibitor with IC50s of 1, 112 nM, respectively. 20, and 112 nM, respectively.

Purity: 99.96% Purity: 99.92% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

www.MedChemExpress.com 23

TyK2-IN-2 Tyk2-IN-3 Cat. No.: HY-101762 Cat. No.: HY-18709

Bioactivity: TyK2-IN-2 is an inhibitor of TYK2, used for treatment of Bioactivity: Tyk2-IN-3 is a Tyk2 pseudokinase inhibitor, with an IC50 of inflammatory and autoimmune diseases. 485 nM.

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, 50 mg, 100 mg

Tyk2-IN-4 Tyk2-IN-5 Cat. No.: HY-117287 Cat. No.: HY-111745

Bioactivity: Tyk2-IN-4 is a selective, potent, allosteric inhibitor of Bioactivity: Tyk2-IN-5 (compound 6) is a highly potent, selective and ( Tyk2). orally active Tyk2 inhibitor and targets the JH2 domain, with

a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα. Highly effective in inhibiting IFNγ production in a rat pharmacodynamics model and fully efficacious in a rat adjuvant… Purity: 99.76% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 500 mg, 250 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Upadacitinib WHI-P154 (ABT-494) Cat. No.: HY-19569 Cat. No.: HY-13895

Bioactivity: (ABT-494) is a potent and selective Janus kinase Bioactivity: WHI-P154 is a potent EGFR inhibitor, and also modestly blocks ( JAK) 1 inhibitor with an IC of 43 nM, being developed for 50 JAK3, with IC50s of 4 nM and 1.8 μM, respectively. the treatment of several autoimmune disorders.

Purity: 99.96% Purity: 98.60% Clinical Data: Phase 3 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, 200 mg, 10 mg, 50 mg 500 mg, 1 g, 5 g, 10 g

WHI-P97 WP1066 Cat. No.: HY-11067 Cat. No.: HY-15312

Bioactivity: WHI-P97 is a rationally designed potent inhibitor of JAK-3. Bioactivity: WP1066 is an inhibitor of JAK2 and STAT3, and also shows IC50 value: Target: JAK3 Treatment of mast cells with WHI-P97 effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3. inhibited the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE… Purity: 99.48% Purity: 99.67% 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 10 mg, 50 mg

XL019 ZM39923 Cat. No.: HY-13775 Cat. No.: HY-12589A

Bioactivity: XL019 is a potent and selective JAK2 inhibitor with IC50 of Bioactivity: ZM39923 is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 2.2 nM, 100 fold selectivity over JAK1; shows good biochemical also potently inhibits tissue transglutaminase ( TGM2) with and cellular potency against JAK2 with good selectivity an IC of 10 nM. against the Janus Kinase family as well as a broad kinase 50 panel. IC50 Value: 2.2 nM (JAK2); 214.2 nM (JAK3) [1] XL019… Purity: 98.0% Purity: >98% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

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

ZM39923 hydrochloride Cat. No.: HY-12589

Bioactivity: ZM39923 hydrochloride is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 hydrochloride also potently inhibits tissue

transglutaminase ( TGM2) with an IC50 of 10 nM.

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

www.MedChemExpress.com 25 Pim Pim kinases

Pim kinases are a small family of serine/threonine kinases regulating several signaling pathways that are fundamental to cancer development and progression. They were first recognized as pro-viral integration sites for the Moloney Murine virus. Pim kinases possess a hinge region which creates a unique binding pocket for ATP. Absence of a regulatory domain means that these proteins are constitutively active once transcribed. Pim kinases are critical downstream effectors of the ABL (ableson), JAK2 (), and Flt-3 (FMS related tyrosine kinase 1) oncogenes and are required by them to drive tumorigenesis. Recent investigations have established that the Pim kinases function as effective inhibitors of apoptosis and when overexpressed, produce resistance to the mTOR (mammalian target of rapamycin) inhibitor, rapamycin . Overexpression of the PIM kinases has been reported in several hematological and solid tumors (PIM 1), myeloma, , leukemia (PIM 2) and adenocarcinomas (PIM 3). As such, the Pim kinases are a very attractive target for pharmacological inhibition in cancer therapy. Novel small molecule inhibitors of the human Pim kinases have been designed and are currently undergoing preclinical evaluation.

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

(1S,3R,5R)-PIM447 dihydrochloride (Z)-SMI-4a ((1S,3R,5R)-LGH447 dihydrochloride) Cat. No.: HY-19322C Cat. No.: HY-16576A

Bioactivity: (1S,3R,5R)-PIM447 (dihydrochloride) an PIM inhibitor Bioactivity: (Z)-SMI-4a is a selective ATP-competitive Pim-1 kinase extracted from patent US 20100056576 A1, compound example 72, inhibitor with an IC50 of 21 nM for Pim-1 compared to an IC50

has IC50 values of 0.095 μM for Pim1, 0.522 μM for Pim2 and of 100 nM for Pim-2 and with little or no activity against a 0.369 μM for Pim3. panel of 50 other kinases tested. IC50 value: 21 nM (Pim1); 100 nM (Pim2) [1] Target: Pim-1 in vitro: Incubation of… Purity: 96.21% 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

AZD1208 AZD1208 hydrochloride Cat. No.: HY-15604 Cat. No.: HY-15604A

Bioactivity: AZD1208 is a novel, orally bioavailable, highly selective Bioactivity: AZD1208 hydrochloride is a novel, orally bioavailable, highly PIM kinases inhibitor. selective PIM kinases inhibitor.

Purity: 99.67% Purity: >98% Clinical Data: Phase 1 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

CX-6258 CX-6258 hydrochloride hydrate Cat. No.: HY-18095 Cat. No.: HY-18095A

Bioactivity: CX-6258 is a potent, orally efficacious Pim 1/2/3 Bioactivity: CX-6258 hydrochloride hydrate is a potent, orally efficacious kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with biochemical potency and kinase selectivity. excellent biochemical potency and kinase selectivity.

Purity: 99.13% Purity: 99.55% 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

GDC-0339 GNE-955 Cat. No.: HY-16976 Cat. No.: HY-101783

Bioactivity: GDC-0339 is a Pim kinase inhibitor with IC50 of 43.6 nM for Bioactivity: GNE-955 is a potent and orally active pan Pim kinase BaF3 PIM1. IC50 value: 43.6 nM (for BaF3 PIM1), 0.04 nM (Ki, inhibitor with Kis of 0.018, 0.11, 0.08 nM for Pim1, Pim2, for PIM1 LC-3K) Target: Pim Pim3, respectively.

Purity: 99.96% 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, 50 mg

Hispidulin INCB053914 phosphate (Dinatin) Cat. No.: HY-N1950 Cat. No.: HY-101870B

Bioactivity: Hispidulin is a natural flavone with a broad spectrum of Bioactivity: INCB053914 phosphate is an inhibitor of Pim extracted from

biological activities. Hispidulin is a Pim-1 inhibitor with an patent WO 2017044730 A1, compound 1; has an IC50 of less than IC of 2.71 μM. 50 35 nM.

Purity: 99.33% Purity: 99.91% 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 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 27

M-110 PIM-447 dihydrochloride Cat. No.: HY-12830 (LGH447 dihydrochloride) Cat. No.: HY-19322B

Bioactivity: M-110 is a novel and highly selective inhibitor of PIM Bioactivity: PIM447 is a pan-PIM kinase ihibitor with Kis of 6, 18, 9 nM kinases; inhibits the proliferation of prostate cancer cell for PIM1, PIM2 and PIM3, respectively. lines with IC50s of 0.6 to 0.9 uM, with no activity on normal human peripheral blood mononuclear cells up to 40 uM.

Purity: >98% Purity: 99.67% 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 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

PIM1-IN-1 Pim1/AKK1-IN-1 Cat. No.: HY-111552 (LKB1/AAK1 dual inhibitor) Cat. No.: HY-10371

Bioactivity: PIM1-IN-1 is a potent and highly selective PIM1/3 Bioactivity: Pim1/AKK1-IN-1 is a potent multi-kinase inhibitor with Kd inhibitor, with IC s of 7, 5530 and 70 nM for PIM1, PIM2, and 50 values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 PIM3, respectively, inhibits the phosphorylation of BAD, a respectively, and also inhibits MPSK1 and TNIK.

downstream target of PIM, with an EC 50 of 262 nM. PIM1-I… Purity: >98% Purity: 98.10% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

PIM447 Quercetagetin (LGH447) Cat. No.: HY-19322 (6-Hydroxyquercetin) Cat. No.: HY-N4149

Bioactivity: PIM447 is novel pan-PIM kinase inhibitor, including Moloney Bioactivity: Quercetagetin (6-Hydroxyquercetin) is the major flavonoid Murine Leukemia (PIM) 1, 2, and 3 Kinase. isolated from Citrus unshiu ( C. unshiu) peel [1]. Quercetagetin is a moderately potent and selective, cell-permeable pim-1 [2] kinase inhibitor ( IC50, 0.34 μM) . Anti-inflammatory … Purity: >98% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 50 mg, 100 mg Size: 5 mg, 10 mg

SGI-1776 SMI-16a Cat. No.: HY-13287 (PIM1/2 Kinase Inhibitor VI) Cat. No.: HY-101947

Bioactivity: SGI-1776 is an inhibitor of Pim kinases, with IC50s of 7 Bioactivity: SMI-16a is a selective Pim kinase inhibitor with IC50 nM, 363 nM, and 69 nM for Pim-1, -2 and -3, respectively. values of 0.15, 0.02 and 48 μM for Pim1, Pim2 and PC3 cells, respectively.

Purity: 99.94% 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 5 mg, 10 mg, 25 mg, 50 mg

TCS PIM-1 1 TCS-PIM-1-4a (SC 204330) Cat. No.: HY-18086 (SMI-4a) Cat. No.: HY-16576

Bioactivity: TCS PIM-1 1(sc-204330) is a potent and selective Bioactivity: TCS-PIM-1-4a is a Pim inhibitor that blocks mTORC1 activity ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, via activation of AMPK; kills a wide range of both myeloid and displays good selectivity over Pim-2 and MEK1/MEK2(IC50s lymphoid cell lines (with IC50 values ranging from 0.8 to 40 >20,000 nM). IC50 value: 50 nM [1] Target: Pim-1 TCS PIM-1 μM). IC50 value: Target: Pim SMI-4a a novel 1 bound convincingly within the ATP-binding site of Pim-1… benzylidene-thiazolidine-2, 4-dione small molecule inhibitor… Purity: 97.41% 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, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

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

TP-3654 Cat. No.: HY-101126

Bioactivity: TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively.

Purity: 99.71% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 29 STAT

STAT is a family of cytoplasmic protein that regulates many aspects of growth, survival and differentiation in cells. The transcription factors of this family are activated by Janus kinase and dysregulation of this pathway is frequently observed in primary tumours and leads to increased angiogenesis, enhanced survival of tumours and immunosuppression. Gene knockout studies have provided evidence that STAT proteins are involved in the development and function of the immune system and play a role in maintaining immune tolerance and tumour surveillance. STAT proteins were originally described as latent cytoplasmic transcription factors that require phosphorylation for nuclear retention. The unphosphorylated STAT proteins shuttle between cytosol and the nucleus waiting for its activation signal. Once the activated transcription factor reaches the nucleus, it binds to consensus DNA-recognition motif called gamma-activated sites (GAS) in the promoter region of cytokine-inducible genes and activates transcription of these genes.

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

AG-490 Alantolactone (Tyrphostin AG 490) Cat. No.: HY-12000 ((+)-Alantolactone; Alant camphor; Inula camphor) Cat. No.: HY-N0038

Bioactivity: AG-490 is a tyrosine kinase inhibitor that inhibits EGFR, Bioactivity: Alantolactone is a selective STAT3 inhibitor, with potent Stat-3 and JAK2/3. anticancer activity.

Purity: 99.84% 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, 10 mg, 50 mg, 100 mg, 200 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Artesunate AS1517499 Cat. No.: HY-N0193 Cat. No.: HY-100614

Bioactivity: Artesunate is an inhibitor of both STAT-3 and exported Bioactivity: AS1517499 is a potent STAT6 inhibitor with an IC50 of 21 nM. protein 1 ( EXP1).

Purity: 98.0% Purity: 99.17% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Atractylenolide I Balsalazide Cat. No.: HY-N0201 Cat. No.: HY-B0667

Bioactivity: Atractylenolide I is a sesquiterpene derived from the rhizome Bioactivity: Balsalazide could suppress colitis-associated carcinogenesis of Atractylodes macrocephala, possesses diverse bioactivities, through modulation of IL-6/STAT3 pathway. such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and… Purity: 99.08% Purity: 99.20% 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 10 mg, 50 mg, 100 mg

Balsalazide sodium hydrate BP-1-102 (Balsalazide disodium dihydrate) Cat. No.: HY-B0667A Cat. No.: HY-100493

Bioactivity: Balsalazide sodium hydrate could suppress colitis-associated Bioactivity: BP-1-102 is an orally available, small-molecule inhibitor of

carcinogenesis through modulation of IL-6/STAT3 pathway. transcription factor Stat3, with an IC50 of 6.8 μM.

Purity: >98% Purity: 99.23% Clinical Data: Launched Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

C188-9 Casticin Cat. No.: HY-112288 (Vitexicarpin) Cat. No.: HY-N0516

Bioactivity: C188-9 is a Stat3 inhibitor, with a Kd of 4.7 nM. Bioactivity: Casticin is a methyoxylated flavonol isolated from Viticis Fructus, with antimitotic and anti-inflammatory effect. Casticin inhibits the activation of STAT3.

Purity: 98.11% Purity: 98.44% 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

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CMD178 Colivelin Cat. No.: HY-P1453 Cat. No.: HY-P1061

Bioactivity: CMD178 is a lead peptide that consistently reduced the Bioactivity: Colivelin is a neuroprotective peptide and activator of expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα STAT3. signaling. CMD178 also is an inhibitor of STAT5 and inhibit T [1] reg cell development . Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 500u g, 1 mg

Colivelin TFA Corylifol A Cat. No.: HY-P1061A (Corylifol-A; Corylinin) Cat. No.: HY-N0897

Bioactivity: Colivelin (TFA) is a neuroprotective peptide and activator of Bioactivity: Corylifol A inhibits IL-6-induced STAT3 activation and STAT3. phosphorylation, with an IC50 of 0.81 μM.

Purity: 95.29% Purity: 99.75% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500u g, 1 mg Size: 5 mg, 10 mg

Cryptotanshinone Cucurbitacin I (Cryptotanshinon; Tanshinone c) Cat. No.: HY-N0174 (Elatericin B; JSI-124; NSC-521777) Cat. No.: HY-N1405

Bioactivity: Cryptotanshinone is a natural compound extracted from the root Bioactivity: Cucurbitacin I is a natural selective inhibitor of of Salvia miltiorrhiza Bunge that shows antitumor JAK2/STAT3, with potent anti-cancer activity.

activities. Cryptotanshinone inhibits STAT3 with an IC50 of 4.6 μM.

Purity: 98.51% 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

Dihydroisotanshinone I Diosgenin Cat. No.: HY-B1919 Cat. No.: HY-N0177

Bioactivity: Dihydroisotanshinone I is a bioactive compound present in a Bioactivity: Diosgenin, a steroidal saponin, can inhibit STAT3 signaling widely used traditional Chinese medicine named danshen. pathway.

Purity: 99.61% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 50 mg 5 mg, 10 mg, 25 mg, 50 mg

ENMD-119 FLLL32 (ENMD 1198; IRC 110160) Cat. No.: HY-16196 Cat. No.: HY-100544

Bioactivity: ENMD-119 is a 2-methoxyestradiol analogue with Bioactivity: FLLL32, a synthetic analog of curcumina, is a JAK2/STAT3 dual antiproliferative and antiangiogenic activity, and is suitable inhibitor with anti-tumor activity [1] [2]. for inhibiting HIF-1α and STAT3 in human HCC cells.

Purity: >98% Purity: 99.78% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

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

Fludarabine HJC0152 hydrochloride (F-ara-A; NSC 118218) Cat. No.: HY-B0069 Cat. No.: HY-100602

Bioactivity: Fludarabine (NSC 118218) is a DNA synthesis inhibitor, which Bioactivity: HJC0152 hydrochloride is a signal transducers and activators of also inhibits phosphorylation of STAT1. transcription 3 ( STAT3) inhibitor.

Purity: 99.28% Purity: 98.86% Clinical Data: Launched 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

HO-3867 Homoharringtonine Cat. No.: HY-100453 (Omacetaxine mepesuccinate; HHT) Cat. No.: HY-14944

Bioactivity: HO-3867 is a selective and potent STAT3 inhibitor and shows Bioactivity: Homoharringtonine (Omacetaxine mepesuccinate;HHT) is a good antitumor activity. cytotoxic alkaloid with antitumor properties which acts by inhibiting translation elongation.

Purity: 99.38% 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, 25 mg, 50 mg 10 mg, 50 mg inS3-54A18 Isocryptotanshinone Cat. No.: HY-103128 Cat. No.: HY-N6651

Bioactivity: inS3-54A18 is a potent STAT3 inhibitor, with anti-cancer Bioactivity: Isocryptotanshinone is a potent signal transducer and properties. activator of transcription 3 ( STAT3) and protein tyrosine

phosphatase 1B PTP1B inhibitor, with an IC50 of 56.1 μM for PTP1B.

Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

Mogrol Morusin Cat. No.: HY-N2312 (Mulberrochromene) Cat. No.: HY-N0622

Bioactivity: Mogrol is a biometabolite of mogrosides, and acts via Bioactivity: Morusin is a prenylated flavonoid isolated from M. australis inhibition of the ERK1/2 and STAT3 pathways, or reducing with various biological activities, such as antitumor, CREB activation and activating AMPK signaling. antioxidant, and anti-bacteria property. Morusin could inhibit NF-κB and STAT3 activity.

Purity: 98.06% 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, 1 mg, 5 mg, 10 mg, 25 mg 2 mg, 5 mg, 10 mg, 25 mg

Napabucasin Niclosamide Cat. No.: HY-13919 (BAY2353) Cat. No.: HY-B0497

Bioactivity: Napabucasin is a STAT3 inhibitor which blocks stem cell Bioactivity: Niclosamide is an orally bioavailable chlorinated activity in cancer cells. salicylanilide, with anthelmintic and potential antineoplastic

activity. Niclosamide inhibits STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.

Purity: 98.0% Purity: 95.00% Clinical Data: Phase 3 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMF, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g 5 g, 10 g

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Niclosamide monohydrate Nifuroxazide (BAY2353 monohydrate) Cat. No.: HY-B0497B Cat. No.: HY-B1436

Bioactivity: Niclosamide monohydrate is an inhibitor of STAT3 with IC50 of Bioactivity: Nifuroxazide is an effective inhibitor of STAT3, also exerts 0.25 μM in HeLa cells and inhibits DNA replication in a potent anti-tumor and anti-metastasis activity. cell-free assay.

Purity: >98% Purity: 99.20% Clinical Data: Launched Clinical Data: Launched Size: 5 g, 10 g Size: 10mM x 1mL in DMSO, 200 mg, 500 mg

NSC 74859 Pimozide (S3I-201) Cat. No.: HY-15146 (R6238) Cat. No.: HY-12987

Bioactivity: NSC 74859 is a selective Stat3 inhibitor with an IC50 of Bioactivity: Pimozide is a dopamine receptor antagonist, with Kis of 86±33 μM. 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at

α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhib… Purity: 98.90% Purity: 99.88% 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 50 mg

Protosappanin A Saikosaponin D (PTA) Cat. No.: HY-113573 Cat. No.: HY-N0250

Bioactivity: Protosappanin A (PTA), an immunosuppressive ingredient and Bioactivity: Saikosaponin D is a triterpene saponin isolated from major biphenyl compound isolated from Caesalpinia sappan L, Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, suppresses JAK2/STAT3-dependent inflammation pathway through and anti-allergic activities; Saikosaponin D inhibits selectin, down-regulating the phosphorylation of JAK2 and STAT3 [1]. STAT3 and NF-kB and activates estrogen receptor-β.

Purity: 98.88% Purity: 98.0% Clinical Data: Clinical Data: No Development Reported Size: 5 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Scutellarin SH-4-54 Cat. No.: HY-N0751 Cat. No.: HY-16975

Bioactivity: Scutellarin, an active flavone isolated from Scutellaria Bioactivity: SH-4-54 is a STAT inhibitor that binds to STAT3 and STAT5 baicalensis, can down-regulates the STAT3/Girdin/Akt signaling with KDs of 300, 464 nM, respectively. in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts.

Purity: 98.0% 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, 10 mg, 25 mg, 50 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

SH5-07 STAT3-IN-3 Cat. No.: HY-100494 Cat. No.: HY-128588

Bioactivity: SH5-07 is a hydroxamic acid based Stat3 inhibitor with an Bioactivity: STAT3-IN-3 is a potent and selective inhibitor of signal [1] IC50 of 3.9 μM in in vitro assay. transducer and activator of transcription 3 (STAT3) .

Purity: 98.0% 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, 50 mg, 100 mg

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

STAT5-IN-1 STAT5-IN-2 Cat. No.: HY-101853 Cat. No.: HY-102048

Bioactivity: STAT5-IN-1 is a STAT5 inhibitor with an IC50 of 47 μM for Bioactivity: STAT5-IN-2 is a STAT5 inhibitor with EC50s of 9 μM and 5 μM STAT5β isoform. in K562 and KU812 cells, respectively. Potent antileukemic effect [1].

Purity: 98.0% 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

Stattic TPCA-1 Cat. No.: HY-13818 Cat. No.: HY-10074

Bioactivity: Stattic is a potent inhibitor of STAT3 activation and Bioactivity: TPCA-1 is a potent and selective inhibitor of IKK-2 with IC50 dimerization. of 17.9 nM. TPCA-1 is a direct dual inhibitor of STAT3 and NF-kB.

Purity: 98.0% 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, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 100 mg

WP1066 Cat. No.: HY-15312

Bioactivity: WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.

Purity: 99.67% Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

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