Topoisomerase

Catalog No.Inhibitor Name TopoisomeraseTopo ITopo IITopo IVOther
A10174Camptothecin
**
A10939Topotecan HCl
****
A10465Idarubicin HCl
***
Multicellular spheroids
A10194Daunorubicin HCl
***
A11999Betulinic acid
**
HIV-1,Aminopeptidase N
A11861Flumequine
*
A14403Doxorubicin
A10373Etoposide
A10478Irinotecan
A10345Epirubicin HCl
A10596Mitoxantrone HCl
A10609Moxifloxacin HCl
A10479Irinotecan HCl Trihydrate
A12011SN-38
A10071Amonafide
A10907Teniposide
A10419Gatifloxacin
A10426Genistein
EGFR
A10595Mitoxantrone
A10735Pirarubicin
A10041Adriamycin
A10557Marbofloxacin
A10666Ofloxacin
A10740Podophyllotoxin
A12663Amrubicin
A13059Beta-Lapachone
IDO1

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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  1. 9-amino-CPT

    Catalog No. A12540
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    Topoisomerase I inhibitor
    9-Aminocamptothecin is a topoisomerase I inhibitor with potent anticancer activity. Learn More
  2. CL2A-SN-38

    Catalog No. A18392
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    DNA Topoisomerase I inhibitor
    CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. Learn More
  3. Namitecan

    Catalog No. A21146
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    topoisomerase I inhibitor
    Namitecan is a potent topoisomerase I inhibitor, with antitumor property. Learn More
  4. GENZ-644282

    Catalog No. A13206
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    topoisomerase 1 inhibitor
    Genz-644282 is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. Learn More
  5. MAC glucuronide phenol-linked SN-38

    Catalog No. A18403
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    DNA topoisomerase I inhibitor
    MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I inhibitor) drug linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively. Learn More
  6. Amsacrine hydrochloride

    Catalog No. A17707
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    topoisomerase II inhibitor
    Amsacrine hydrochloride (m-AMSA hydrochloride; acridinyl anisidide hydrochloride) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells. Learn More
  7. Pirarubicin Hydrochloride

    Catalog No. A18037
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    topoisomerase II inhibitor
    Pirarubicin Hydrochloride is an anthracycline antibiotics, acts as a topoisomerase II inhibitor, and is a widely used for treatment of various cancers, in particular, solid tumors. Learn More
  8. Gepotidacin

    Catalog No. A21086
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    topoisomerase II inhibitor
    Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor. Learn More
  9. Epirubicin

    Catalog No. A12409
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    Topoisomerase inhibitor
    Epirubicin is a cell-permeable antitumor antibiotic. A stereoisomer of Doxorubicin that exhibits reduced cardiotoxicity. Epirubicin’s antitumor actions are mediated by targeting and inhibiting Topo II (topoisomerase II). Learn More
  10. Karenitecin

    Catalog No. A21156
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    topoisomerase I inhibitor
    Karenitecin (Cositecan) is a topoisomerase I inhibitor, with potent anti-cancer activity. Learn More
  11. Edotecarin

    Catalog No. A21233
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    Topoisomerase I inhibitor
    Edotecarin is a potent inhibitor of topoisomerase I that can induces single-strand DNA cleavage, with IC50 of 50 nM. Learn More
  12. Exatecan Mesylate

    Catalog No. A21515
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    DNA topoisomerase I inhibitor
    Exatecan Mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research. Learn More
  13. TAS-103

    Catalog No. A21954
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    DNA topoisomerase I/II inhibitor
    TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research. Learn More
  14. Daunorubicin

    Catalog No. A21903
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    topoisomerase II inhibitor
    Daunorubicin (Daunomycin; RP 13057; Rubidomycin) is a topoisomerase II inhibitor with potent antineoplastic activities. Learn More
  15. Dxd

    Catalog No. A21517
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    DNA topoisomerase I inhibitor
    Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a). Learn More
  16. Daun02

    Catalog No. A21818
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    prodrug of the topoisomerase inhibitor Daunorubicin
    Daun02 is a prodrug of the topoisomerase inhibitor Daunorubicin. Learn More
  17. NK314

    Catalog No. A13993
    Topoisomerase II inhibitor
    NK314 is a novel synthetic benzo[c]phenanthridine alkaloid that shows strong antitumor activity. It inhibited topoisomerase II activity and stabilized topoisomerase II-DNA cleavable complexes. Learn More
  18. BNS-22

    Catalog No. A13443
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    Topo II inhibitor
    BNS-22 is a potent small molecule inhibitor of Topo II (IC50 2.8 M and 0.42 M for Topo II alpha and Topo II beta, respectively). Learn More
  19. ABT 492 meglumine (Delafloxacin meglumine)

    Catalog No. A15064
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    ABT 492 was more potent against quinolone-susceptible and -resistant gram-positive organisms, had activity similar to that of ciprofloxacin against certain members of the family Enterobacteriaceae, and had comparable activity against quinolone-susceptible, nonfermentative, gram-negative organisms. in vitro: Learn More
  20. CKD602

    Catalog No. A13656
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    Topoisomerase I inhibitor
    CKD-602 is a topoisomerase I inhibitor. Learn More
  21. Ellipticine

    Catalog No. A13780
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    DNA topoisomerase II inhibitor
    Ellipticine is a DNA intercalating agent and a DNA topoisomerase II inhibitor. Learn More
  22. Nemorubicin

    Catalog No. A14363
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    Topoisomerase II inhibitor
    Nemorubicin is an anticancer drug with IC50 value of 0.08 uM. It is active on tumors resistant to alkylating agents, topoisomerase II inhibitors and platinum derivatives. It works primarily through topoisomerase I inhibition. Learn More
  23. Indotecan

    Catalog No. A20979
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    Top1 inhibitor
    Indotecan (LMP-400) is a potent topoisomerase 1(Top1) inhibitor with IC50 values of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Learn More
  24. Doxorubicin

    Catalog No. A14403
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    Topoisomerase II inhibitor
    Doxorubicin is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis. Learn More
  25. Voreloxin Hydrochloride

    Catalog No. A15280
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    Topoisomerase inhibitor
    Voreloxin Hcl is a small molecule and a naphthyridine analogue with antineoplastic activity; inhibitor of Topo II. Learn More
  26. Clorobiocin

    Catalog No. A15467
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    DNA Gyrase Inhibitor
    Clorobiocin is an aminocoumarin. Learn More
  27. CL2-SN-38

    Catalog No. A18945
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    DNA topoisomerase I inhibitor
    CL2-SN-38 is a part of the antibody drug conjugate (ADC), can conjugate with the anti-Trop-2-humanized antibody hRS7. SN-38 is a DNA topoisomerase I inhibitor. Learn More
  28. Top1 inhibitor 1

    Catalog No. A13304
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    human topoisomerase I (Top1) inhibitor
    Top1 inhibitor 1 (compound 28) is a potent human topoisomerase I (Top1) inhibitor with an IC50 value of 29 nM. Learn More
  29. MAC glucuronide α-hydroxy lactone-linked SN-38

    Catalog No. A18407
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    Topoisomerase I inhibitor
    MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a stabilized lactone MAC glucuronide α-hydroxy lactone-linked SN-38 drug linker. Learn More
  30. Topotecan

    Catalog No. A16815
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    Topoisomerase inhibitor
    Topotecan is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases. Learn More
  31. Pixantrone

    Catalog No. A13022
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    Topoisomerase II inhibitor
    Pixantrone is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity. Learn More
  32. Clinafloxacin

    Catalog No. A16458
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    DNA gyrase and topoisomerase IV inhibitor
    Clinafloxacin is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae. Learn More
  33. Levofloxacin hydrate

    Catalog No. A16167
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    topoisomerase II IV inhibitor
    Levofloxacin is a broad-spectrum, third-generation fluoroquinolone antibiotic and optically active L-isomer of ofloxacin with antibacterial activity. Learn More
  34. Teniposide

    Catalog No. A10907
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    Teniposide is a semisynthetic derivative of podophyllotoxin with antineoplastic activity. Learn More
  35. SW044248

    Catalog No. A15837
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    TOP1 inhibitor‎
    SW044248 is a novel noncanonical Top1 inhibitor with a pattern of selective toxicity for NSCLC cells. Learn More
  36. TAS 103 2HCl

    Catalog No. A14141
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    topoisomerase I/II inhibitor
    TAS 103, also known as BMS-247615, is a quinoline derivative that displays antitumor activity in murine and human tumor models Learn More
  37. Voreloxin

    Catalog No. A14158
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    Topoisomerase II inhibitor
    Voreloxin is a small molecule and a naphthyridine analogue with antineoplastic activity. Vosaroxin intercalates into DNA in a site-specific manner and blocks the re-ligation process carried out by topoisomerase II during DNA replication Learn More
  38. Ametantrone

    Catalog No. A12569
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    topoisomerase II inhibitor
    Ametantrone (AM) is a synthetic 9,10-anthracenedione bearing two (hydroxyethylamino)ethylamino residues at positions 1 and 4 along with other anthraquinones and anthracyclines. Learn More
  39. Idarubicin HCl

    Catalog No. A10465
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    Topoisomerase inhibitor
    Idarubicin is an anthracycline antibiotic that is an anti-leukemia agent with higher DNA binding capacity and greater cytotoxicity than daunorubicin. Learn More
  40. Genistin (Genistoside)

    Catalog No. A10426
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    Genistin is an isoflavone found in a number of dietary plants like soy and kudzu. It was shown to stimulate estrogen-dependent breast cancer cell growth in vivo. Learn More
  41. Etoposide (VP-16)

    Catalog No. A10373
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    Topoisomerase II inhibitor
    Etoposide forms a ternary complex with DNA and the topoisomerase II enzyme (which aids in DNA unwinding), prevents re-ligation of the DNA strands, and by doing so causes DNA strands to break. Therefore, this causes errors in DNA synthesis and promotes apoptosis of the cancer cell. Learn More
  42. Epirubicin HCl

    Catalog No. A10345
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    Topoisomerase II inhibitor
    Epirubicin is a cell-permeable anthracycline antitumor antibiotic. It is a stereoisomer(4′-epi-isomer) of doxorubicin that exhibits reduced cardiotoxicity. It is used to inhibit topoisomerase II and DNA helicase activity. Learn More
  43. Camptothecin

    Catalog No. A10174
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    Topoisomerase I inhibitor
    Camptothecin is a cytotoxic quinoline alkaloid which inhibits the DNA enzyme topoisomerase I (topo I). Learn More
  44. Exatecan mesylate

    Catalog No. A11231
    Topoisomerase I inhibitor
    Exatecan mesylate inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA and inhibiting religation of DNA breaks, thereby inhibiting DNA replication and triggering apoptotic cell death. Learn More
  45. Cerubidine (Daunorubicin HCl, Rubidomycin HCl)

    Catalog No. A10194
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    Topoisomerase inhibitor

    Cerubidine (Daunorubicin HCl, Rubidomycin HCl) interacts with DNA by intercalation and inhibition of macromolecular biosynthesis. This inhibits the progression of the enzyme topoisomerase II, which relaxes supercoils in DNA for transcription. It stabilizes the topoisomerase II complex after it has broken the DNA chain for replication, preventing the DNA double helix from being resealed and thereby stopping the process of replication.

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  46. Amonafide (AS1413)

    Catalog No. A10071
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    Topoisomerase inhibitor

    Amonafide is a DNA intercalator and topoisomerase II inhibitor for the treatment of neoplastic diseases, one of Antitumor agent.

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  47. Adriamycin

    Catalog No. A10041
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    topoisomerase II inhibitor

    Adriamycin is an anthracycline antibiotic, it works by intercalating DNA, while most serious adverse effect being life-threatening heart damage. It is commonly used in the treatment of a wide range of cancers, including hematological malignancies, many types of carcinoma, and soft tissue sarcomas.

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  48. ABT-492 (Delafloxacin)

    Catalog No. A10023
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    Fluoroquinolone antibiotic
    ABT-492 is a new fluoroquinolone against 155 aerobic and 171 anaerobic pathogens. Learn More
  49. Irinotecan HCl Trihydrate (Campto)

    Catalog No. A10479
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    Topoisomerase inhibitor
    Irinotecan (CPT 11), a compound within the camptothecin family, is an inhibitor of topoisomerase 1 involved in cellular DNA replication and transcription. Learn More
  50. Topotecan HCl (Hycamtin)

    Catalog No. A10939
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    DNA topoisomerase I inhibitor
    Topotecan HCl (Hycamtin) is a chemotherapeutic agent that is a topoisomerase inhibitor. Learn More

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