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Topoisomerase 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. Type I topoisomerase 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 1 Topoisomerase Inhibitors & Agonists (S)-10-Hydroxycamptothecin (±)-10-Hydroxycamptothecin (10-HCPT; 10-Hydroxycamptothecin) Cat. No.: HY-N0095 ((±)-10-HCPT) Cat. No.: HY-N0275 (S)-10-Hydroxycamptothecin (±)-10-Hydroxycamptothecin, an indole alkaloid (10-HCPT;10-Hydroxycamptothecin) is a DNA isolated from Camptotheca acuminate, inhibits the topoisomerase I inhibitor of isolated from the activity of topoisomerase I and has a broad Chinese plant Camptotheca accuminata. spectrum of anticancer activity. Purity: 99.38% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 50 mg, 100 mg Size: 1 mg, 5 mg 9-amino-CPT 9-Hydroxyellipticine hydrochloride (9-amino-20(S)-camptothecin) Cat. No.: HY-100309 Cat. No.: HY-101775A 9-amino-CPT (9-amino-20(S)-camptothecin) is a 9-Hydroxyellipticine hydrochloride is a inhibitor topoisomerase I inhibitor with potent anticancer of Topo II and RyR. 9-Hydroxyellipticine activity. hydrochloride exhibits antitumor, antioxidant and catecholamine-releasing activities. Purity: 98.89% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 2 mg, 5 mg, 10 mg, 25 mg Size: 1 mg, 5 mg 9-Methoxycamptothecin Aclacinomycin A hydrochloride Cat. No.: HY-N6011 (Aclarubicin hydrochloride) Cat. No.: HY-N2306A 9-Methoxycamptothecin (MCPT), isolated from Aclacinomycin A hydrochloride (Aclarubicin Nothapodytes foetida, has antitumor activities hydrochloride), a fluorescent molecule and the through topoisomerase inhibition. first described non-peptidic inhibitor showing 9-Methoxycamptothecin (MCPT) induces strong G2/M discrete specificity for the CTRL arrest and apoptosis in cancer. (chymotrypsin-like) activity of the 20S proteasome. Purity: >98% Purity: 95.16% Clinical Data: No Development Reported Clinical Data: Launched Size: 5 mg, 10 mg, 20 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg Aldoxorubicin Alternariol (INNO-206; DOXO-EMCH) Cat. No.: HY-16261 Cat. No.: HY-N6714 Aldoxorubicin (INNO-206) is an albumin-binding Alternariol is a mycotoxin produced by Alternaria prodrug of Doxorubicin (DNA topoisomerase II species. AOH inhibits the catalytic activity of inhibitor), which is released from albumin under topoisomerase I and topoisomerase II enzymes. acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models. Purity: 95.99% 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 Amonafide Amsacrine (AS1413) Cat. No.: HY-10982 (m-AMSA; acridinyl anisidide) Cat. No.: HY-13551 Amonafide is a topoisomerase II inhibitor and Amsacrine (m-AMSA; acridinyl anisidide) is an DNA intercalator that induces apoptotic signaling inhibitor of topoisomerase II, and acts as an by blocking the binding of Topo II to DNA. antineoplastic agent which can intercalates into the DNA of tumor cells. Purity: 99.92% Purity: 99.98% Clinical Data: Phase 3 Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg, 500 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Amsacrine hydrochloride ARN-21934 (m-AMSA hydrochloride; acridinyl anisidide hydrochloride) Cat. No.: HY-13551A Cat. No.: HY-137466 Amsacrine hydrochloride (m-AMSA hydrochloride; ARN-21934 is a potent, highly selective, acridinyl anisidide hydrochloride) is an inhibitor blood-brain barrier (BBB) penetrant inhibitor for of topoisomerase II, and acts as an human topoisomerase II α over β. ARN-21934 antineoplastic agent which can intercalates into inhibits DNA relaxation with an IC50 of 2 μM as the DNA of tumor cells. compared to the anticancer agent Etoposide (IC50=120 μM). Purity: 98.98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg, 500 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Aurintricarboxylic acid Banoxantrone (D12) Cat. No.: HY-122575 (AQ4N D12) Cat. No.: HY-13562S Aurintricarboxylic acid is a nanomolar-potency, Banoxantrone D12 (AQ4N D12) is the deuterium allosteric antagonist with selectivity towards labeled banoxantrone. Banoxantrone is a novel αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, bioreductive agent that can be reduced to a with IC50s of 8.6 nM and 72.9 nM for rP2X1R and stable, DNA-affinic compound AQ4, which is a rP2X3R, respectively. potent topoisomerase II inhibitor. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg Size: 1 mg, 5 mg Banoxantrone D12 dihydrochloride Banoxantrone dihydrochloride (AQ4N D12 dihydrochloride) Cat. No.: HY-13562AS (AQ4N dihydrochloride) Cat. No.: HY-13562A Banoxantrone D12 dihydrochloride (AQ4N D12 Banoxantrone dihydrochloride is a novel dihydrochloride) is the deuterium labeled bioreductive agent that can be reduced to a banoxantrone dihydrochloride. Banoxantrone is a stable, DNA-affinic compound AQ4, which is a novel bioreductive agent that can be reduced to a potent topoisomerase II inhibitor. stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor. Purity: 98.02% Purity: 99.17% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg Belotecan hydrochloride Berberine (CKD-602) Cat. No.: HY-13566A (Natural Yellow 18) Cat. No.: HY-N0716 Belotecan hydrochloride (CKD-602 hydrochloride), a Berberine (Natural Yellow 18) is an alkaloid Topoisomerase I inhibitor, is a synthetic isolated from the Chinese herbal medicine camptothecin derivative. Huanglian, as an antibiotic. Berberine (Natural Yellow 18) induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Purity: 98.82% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 1 mg, 5 mg Berberine chloride Berberine chloride hydrate (Natural Yellow 18 chloride) Cat. No.: HY-18258 (Natural Yellow 18 chloride hydrate) Cat. No.: HY-17577 Berberine chloride is an alkaloid isolated from Berberine chloride hydrate (Natural Yellow 18 the Chinese herbal medicine Huanglian, as an chloride hydrate) is an alkaloid isolated from the antibiotic. Berberine chloride induces reactive Chinese herbal medicine Huanglian, as an oxygen species (ROS) generation and inhibits DNA antibiotic. Berberine chloride hydrate induces topoisomerase. Antineoplastic properties. reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Purity: 99.16% Purity: 99.84% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 100 mg, 1 g, 5 g Size: 10 mM × 1 mL, 100 mg, 1 g, 5 g www.MedChemExpress.com 3 Betulinic acid Bisantrene (Lupatic acid; Betulic acid) Cat. No.: HY-10529 (CL216942) Cat. No.: HY-100875 Betulinic acid is a natural pentacyclic Bisantrene is a highly effective antitumor drug, triterpenoid, acts as a eukaryotic targets eukaryotic type II topoisomerases. topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties. Betulinic acid acts as a new activator of NF-kB. Purity: ≥98.0% Purity: 95.44% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 10 mM × 1 mL, 100 mg, 200 mg, 500 mg Size: 10 mg, 25 mg, 50 mg Camptothecin Camptothecin-20(S)-O-propionate (Campathecin; (S)-(+)-Camptothecin; CPT) Cat. No.: HY-16560 (Camptothecin-20-O-propionate) Cat. No.: HY-114668 Camptothecin (Campathecin) is a potent DNA enzyme Camptothecin-20(S)-O-propionate (CZ48), the topoisomerase I inhibitor, with an IC50 of 679 C20-propionate ester of CPT, is a highly effective nM. anticancer agent. Camptothecin-20(S)-O-propionate (CZ48) is a topoisomerase-Ι inhibitor. Purity: 99.69% Purity: 98.43% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg CH-0793076 CH-0793076 TFA (TP3076) Cat. No.: HY-107096 (TP3076 TFA) Cat. No.: HY-107096B CH-0793076 (TP3076), a hexacyclic camptothecin CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious with an IC50 of 2.3 μM. CH-0793076 TFA is against cells expressing BCRP (breast cancer efficacious against cells expressing BCRP (breast resistance protein). cancer resistance protein). Purity: >98% Purity: 98.92% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg Chloroquinoxaline sulfonamide Coralyne chloride (Chloroquinoxaline; NSC-339004) Cat. No.: HY-106662 Cat. No.: HY-118581 Chloroquinoxaline sulfonamide (Chloroquinoxaline), Coralyne chloride is a protoberberine alkaloid a structural analogue of sulfaquinoxaline, is a with potent anti-cancer activities. Coralyne topoisomerase II alpha/beta poison. chloride acts as a potent topoisomerase I poison Chloroquinoxaline sulfonamide is used to control and induces Top I mediated DNA cleavage. coccidiosis in poultry, rabbit, sheep, and cattle.
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