2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Topoisomerase

Topoisomerase

Topoisomerase

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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.

Topoisomerase Isoform Specific Products:

Topoisomerase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13758
    TAS-103
    		Inhibitor
    TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
    TAS-103
  • HY-B0398R
    Nalidixic acid (Standard)
    		Inhibitor
    Nalidixic acid (Standard) is the analytical standard of Nalidixic acid. This product is intended for research and analytical applications. Nalidixic acid, a quinolone antibiotic, is effective against both gram-positive and gram-negative bacteria. Nalidixic acid acts in a bacteriostatic manner in lower concentrations and is bactericidal in higher concentrations. Nalidixic acid inhibits a subunit of DNA gyrase and topoisomerase IV and reversibly blocks DNA replication in susceptible bacteria.
    Nalidixic acid (Standard)
  • HY-16261A
    MC-DOXHZN
    		Inhibitor
    MC-DOXHZN ((E/Z)-Aldoxorubicin) is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), with acid-sensitive properties.
    MC-DOXHZN
  • HY-42487A
    (rac)-Exatecan Intermediate 1
    		99.84%
    (rac)-Exatecan Intermediate 1 is an isomer of Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631), a camptothecin-based anticancer agent. Exatecan inhibits tumor growth by interfering with the proliferation and division of tumor cells by interacting with DNA. Exatecan is primarily used in research into a variety of cancers including ovarian, lung and breast cancer.
    (rac)-Exatecan Intermediate 1
  • HY-13631P
    Exatecan mesylate dihydrate
    		Inhibitor
    Exatecan (DX-8951) mesylate dihydrate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
    Exatecan mesylate dihydrate
  • HY-16261C
    Aldoxorubicin hydrochloride
    		Inhibitor
    Aldoxorubicin (INNO-206) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin hydrochloride (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
    Aldoxorubicin hydrochloride
  • HY-13768C
    Topotecan hydrochloride hydrate
    		Inhibitor
    Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity.
    Topotecan hydrochloride hydrate
  • HY-163487
    Puxitatug samrotecan drug-linker
    Puxitatug samrotecan drug-linker (AZD8205 drug-linker) is a drug-linker conjugate for ADC, which comprises a topoisomerase I inhibitor and a linker. Puxitatug samrotecan drug-linker can be used to synthesis antibody-drug conjugate (ADC), Puxitatug samrotecan (HY-171689).
    Puxitatug samrotecan drug-linker
  • HY-119892
    Batracylin
    		Inhibitor
    Batracylin (NSC320846) is a potent DNA Topoisomerases I and DNA Topoisomerases II inhibitor. Batracylin shows cytotoxicity and antiproliferative activity. Batracylin induces DNA breaks.
    Batracylin
  • HY-13745
    Sabarubicin
    		Inhibitor
    Sabarubicin is a doxorubicin disaccharide analogue with striking antitumor activity. Sabarubicin is more effective than doxorubicin as a topoisomerase II poison and stimulated DNA fragmentation at lower intracellular concentrations.
    Sabarubicin
  • HY-152965
    Biotin-doxorubicin
    		Inhibitor
    Biotin-doxorubicin is a Biotin-labeled Doxorubicin. Doxorubicin, a broad-spectrum anthracycline antibiotic, is a topoisomerase II inhibitor.
    Biotin-doxorubicin
  • HY-16562S
    Irinotecan-d10
    		Inhibitor
    Irinotecan-d10 is a deuterium labeled Irinotecan ((+)-Irinotecan). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.
    Irinotecan-d<sub>10</sub>
  • HY-13630A
    Etoposide phosphate disodium
    		Inhibitor
    Etoposide phosphate disodium (BMY-40481 disodium) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate disodium is the phosphate ester proagent of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate disodium induces cell cycle arrest, apoptosis, and autophagy.
    Etoposide phosphate disodium
  • HY-13611
    Diflomotecan
    		Inhibitor
    Diflomotecan (BN 80915) is a potent and orally active inhibitor of topoisomerase I. Diflomotecan (BN 80915) causes enhanced plasma stability and has the superior preclinical anti-tumour activity compared with other established compounds.
    Diflomotecan
  • HY-10581C
    Gatifloxacin sesquihydrate
    		Inhibitor
    Gatifloxacin sesquihydrate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin sesquihydrate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin sesquihydrate can be used to treat bacterial conjunctivitis in vivo.
    Gatifloxacin sesquihydrate
  • HY-18258S
    Berberine-d6 chloride
    		Inhibitor
    Berberine-d6 (chloride) is the deuterium labeled Berberine chloride. Berberine chloride is an alkaloid that acts as an antibiotic. Berberine chloride induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties.
    Berberine-d<sub>6</sub> chloride
  • HY-19825
    Rebeccamycin
    		Inhibitor
    Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II.
    Rebeccamycin
  • HY-16700G
    PNU-159682 (GMP)
    		Inhibitor
    PNU-159682 GMP is a GMP grade PNU-159682 (HY-16700). PNU-159682, a metabolite of the anthracycline Nemorubicin, is a highly potent DNA topoisomerase II inhibitor with excellent cytotoxicity. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis. PNU-159682 can be used in EDV-nanocell technology to overcome agent resistance.
    PNU-159682 (GMP)
  • HY-148380
    Mal-PEG8-Phe-Lys-PAB-Exatecan
    		Inhibitor
    Mal-PEG8-Phe-Lys-PAB-Exatecan (compound 15) is a agent-linker conjugate for ADC, composed of degradable linker Mal-PEG8-Phe-Lys-PAB and toxin molecule Exatecan (HY-13631) composition.
    Mal-PEG8-Phe-Lys-PAB-Exatecan
  • HY-13502B
    Mitoxantrone diacetate
    		Inhibitor
    Mitoxantrone diacetate is a potent topoisomerase II inhibitor. Mitoxantrone diacetate also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone diacetate induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone diacetate shows antitumor activity. Mitoxantrone diacetate also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.
    Mitoxantrone diacetate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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