Topoisomerases are enzymes that regulate the overwinding or underwinding of DNA.DNA's double-helical structure is entwined, which leads to the winding issue. Isomerization enzymes called topoisomerases work on DNA's topology. One strand of a DNA double helix is cut by type I topoisomerase, which is followed by relaxation and reannealing of the cut strand. Type I topoisomerases are divided into two subclasses: type IB topoisomerases, which employ a controlled rotary mechanism, and type IA topoisomerases, which share many structural and mechanistic features with the type II topoisomerases. One DNA double helix's two strands are cut by Type II topoisomerase, which then reanneals the cut strands after passing through another DNA double helix that hasn't been broken. Type IIA and type IIB topoisomerases, two subclasses of this class with related structures and mechanisms, are further divided.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V1421 | (S)-10-Hydroxycamptothecin | 19685-09-7 | 10-Hydroxycamptothecin (also abbreviated as 10HCPT; 10OHCPT; HCPT; 10 HCPT), the 10-hydroxylated form of camptothecin, is a natural product and topoisomerase I inhibitor with potential anticancer activity. |
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V1397 | SN-38 (NK012) | 86639-52-3 | SN-38 (NK012; SN-38; NK-012; SN 38; 10-hydroxy-7-ethylcamptothecin) is the active metabolite of Irinotecan (CPT-11) which is a Topoisomerase I inhibitor approved for use as an anticancer drug. |
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V11052 | Aminocamptothecin | 91421-43-1 | Aminocamptothecin (9-amino Camptothecin, 9-AC, 9-amino CPT), an analog of camptothecin (CPT) with higher water solubility, is a potent inhibitor of topoisomerase I with anti-tumor activity. |
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V7168 | AQ4 | 70476-63-0 | AQ4 is a topoisomerase II inhibitor and DNA intercalator, and is a stable cytotoxic molecule in many human tumor cell lines. |
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V1398 | Beta-Lapachone (ARQ-501) | 4707-32-8 | Beta-Lapachone (also known as ARQ-501; NSC 26326;ARQ501;NSC-26326) is a novel, naturally occurring, potent and selective DNA topoisomerase I inhibitor with potential antineoplastic activity. |
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V75881 | Camptothecin-20(S)-O-propionate hydrate (Camptothecin-20-O-propionate hydrate) | 1147090-70-7 | Camptothecin-20(S)-O-propionate (Camptothecin-20-O-propionate) hydrate is an analog of camptothecin (CPT) and a potent anti-tumor compound. |
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V32536 | Dxd | 1599440-33-1 | Dxd,an exatecan analog, is a novel and potent DNA topoisomerase I inhibitor(IC50=0.31 μM) with anticancer activity, and is used as a conjugated drug of HER2-targeting ADC (DS-8201a). |
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V1420 | GSK-J1 | 1373422-53-7 | GSKJ1 (GSK-J1; GSK-J 1; GSK-J-1) is a novel, highly selective and potent inhibitor of histone demethylase (H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A) with potential antineoplastic activity. |
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V2336 | PluriSIn #2 | 56563-17-8 | PluriSIn #2 is a selective transcriptional inhibitor of topoisomerase II alpha (TOP2A). |
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V75879 | SDOX | 2921601-78-5 | SDOX is the precursor active molecule of Doxorubicin. |
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V2051 | TAS-103 (BMS-247615) | 174634-08-3 | TAS-103 (also known as BMS-247615) is a potent and dual inhibitor of DNA topoisomerase I/II. |
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V2860 | TAS-103 dihydrochloride | 174634-09-4 | TAS-103 dihydrochloride (also known as BMS-247615) is a potent and dual inhibitor of DNA topoisomerase I/II. |
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V75882 | Topoisomerase I inhibitor 9 | 1228150-86-4 | Topoisomerase I inhibitor 9 (compound 3d) is a leishmanial topoisomerase IB inhibitor. |
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V75884 | Topoisomerase I/II inhibitor 2 | 2770804-58-3 | Topoisomerase I/II inhibitor 2 (compound 1a) is a potent topoisomerase inhibitor (antagonist) with IC50 of 9.82 μM and 6.83 μM in Huh7 and LM9 cells respectively. |
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V1393 | Irinotecan (CPT-11) | 97682-44-5 | Irinotecan (also known as CPT-11; Camptosar; Irinophore C; CPT11; Irinotecan lactone; Irinotecanum), a semisynthetic analog of camptothecin and the prodrug of 7-ethyl-10-hydroxy-camptothecin (SN-38), is a topoisomerase I inhibitor approved for use as an anticancer drug. |
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V1390 | Etoposide (VP-16) | 33419-42-0 | Etoposide (formerly VP-16, VP-16213; Toposar; VePesid; Lastet; EPEG), a chemotherapeutic drug used for the treatments of various cancers, is a semisynthetic derivative of the naturally occuring podophyllotoxin which inhibits DNA synthesis via topoisomerase II inhibitory activity. |
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V20873 | Exatecan mesylate (DX8951) | 169869-90-3 | Exatecanmesylate (DX-8951) is the methylate of Exatecan, which is a semisynthetic analog of camptothecin with improved water solubility. |
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V1405 | Enoxacin (AT-2266) | 74011-58-8 | Enoxacin (formerly AT-2266; CI-919; NSC-629661;Penetrex; Comprecin; Enoxacino)is an orally bioavailable and broad-spectrum fluoroquinolone antibiotic used to treat various infections, such as UTIs-urinary tract infections and gonorrhea. |
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V1415 | Clinafloxacin (AM-1091; CI-960) | 105956-97-6 | Clinafloxacin (formerly also known as CI-960; PD-127391; AM-1091; CI 960; PD127391; AM1091)is a broad-spectrum and investigational antibiotic of the fluoroquinolone class with promising antibiotic activity against gram-positive, gram-negative, and anaerobic pathogens. |
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V1399 | Gatifloxacin (AM-1155) | 112811-59-3 | Gatifloxacin (formerly also known as AM-1155, CG5501, BMS-206584; PD135432; Tequin; Zymar; Gatiflo; Zymaxid; AM 1155)is a fourth-generation antibiotic of the fluoroquinolone family used to treat tuberculosis and pneumonia, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. |
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