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-B0330B
    Levofloxacin hydrochloride
    		Inhibitor ≥98.0%
    Levofloxacin ((-)-Ofloxacin) hydrochloride is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin hydrochloride inhibits the DNA gyrase and topoisomerase IV. Levofloxacin hydrochloride can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin hydrochloride shows anti-orthopoxvirus activity.
    Levofloxacin hydrochloride
  • HY-100620
    RPR121056
    		Inhibitor 99.88%
    RPR121056 (APC) is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE.
    RPR121056
  • HY-160015
    CB07-Exatecan
    		Inhibitor 98.97%
    CB07-Exatecan is an ADC drug-Linker conjugate that can be used for the synthesis of ADCs. ADC conjugated with CB07-Exatecan and trastuzumab inhibits the growth of HER2-positive cancer cells. CB07-Exatecan can be used in cancer research.
    CB07-Exatecan
  • HY-160409
    TopBP1-IN-1
    		Inhibitor 98.35%
    TopBP1-IN-1 is a TopBP1 inhibitor. TopBP1-IN-1 has a synergistic effect with PARP inhibitors. TopBP1-IN-1 has antitumor activity .
    TopBP1-IN-1
  • HY-14812
    Karenitecin
    		Inhibitor 98.02%
    Karenitecin (Cositecan) is a topoisomerase I inhibitor, with potent anti-cancer activity.
    Karenitecin
  • HY-13670
    Lurtotecan
    		Inhibitor 98.01%
    Lurtotecan (GI147211; OSI-211), a semisynthetic Camptothecin analog, is a topoisomerase I inhibitor. Lurtotecan has anticancer effects.
    Lurtotecan
  • HY-N6011
    9-Methoxycamptothecin
    		Inhibitor 99.13%
    9-Methoxycamptothecin (MCPT), isolated from Camptotheca acuminata, has antitumor activities through topoisomerase inhibition. 9-Methoxycamptothecin (MCPT) induces strong G2/M arrest and apoptosis in cancer.
    9-Methoxycamptothecin
  • HY-U00248
    LMP744
    		Inhibitor 98.85%
    LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
    LMP744
  • HY-43564
    Exatecan Intermediate 5
    		Inhibitor 99.98%
    Exatecan Intermediate 5 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 5 can be used to synthesize Antibody-Drug Conjugates (ADCs).
    Exatecan Intermediate 5
  • HY-14821
    Namitecan
    		Inhibitor 99.25%
    Namitecan is a potent topoisomerase I inhibitor, with antitumor property.
    Namitecan
  • HY-N6865
    Groenlandicine
    		Agonist 99.87%
    Groenlandicine is a protoberberine alkaloid isolated from Coptidis Rhizoma. Groenlandicine exhibits moderate inhibitory effect with IC50 value of 154.2 μM for human recombinant aldose reductase (HRAR). Groenlandicine selectively induces topoisomerase I-mediated DNA cleavage.
    Groenlandicine
  • HY-N0114A
    (±)-Evodiamine
    		Inhibitor 99.74%
    (±)-Evodiamine, a quinazolinocarboline alkaloid, is a Top1 inhibitor. Evodiamine exhibits anti-inflammatory, antiobesity, and antitumor effects. (±)-Evodiamine inhibits the proliferation of a wide variety of tumor cells by inducing their apoptosis.
    (±)-Evodiamine
  • HY-148819
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT
    		Inhibitor 98.71%
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT (compound I) is a topoisomerase I inhibitor, which can be delivered to cells through conjugated antibody targeting, and has good ADC activity in vivo and in vitro.
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT
  • HY-N2063
    12-Ethyl-9-hydroxycamptothecin
    		99.89%
    12-Ethyl-9-hydroxycamptothecin is a derivative of Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM.
    12-Ethyl-9-hydroxycamptothecin
  • HY-153069
    GGFG-PAB-Exatecan
    		Inhibitor 99.71%
    GGFG-PAB-Exatecan consists of an ADC toxin Exatecan (HY-13631) and a linker GGFG-PAB, and can be used as a drug-linker conjugate for the synthesis of ADC molecules.
    GGFG-PAB-Exatecan
  • HY-137466
    ARN-21934
    		Inhibitor 98.08%
    ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research.
    ARN-21934
  • HY-N2198
    Podocarpusflavone A
    		Inhibitor 99.62%
    Podocarpusflavone A is a DNA topoisomerase I inhibitor. Podocarpusflavone A has moderated anti-proliferative activity and induces cell apoptosis in MCF-7. Podocarpusflavone A is developing anti-tumor agents.
    Podocarpusflavone A
  • HY-160005
    LMP517
    		Inhibitor 99.58%
    LMP517 (NSC 781517) a indenoisoquinoline, is a potent a dual TOP1 and TOP2 inhibitor. LMP517 shows better antitumor activity than its parent compound LMP744 (HY-U00248) against H82 (Small Cell Lung Cancer) xenografts. LMP517 induces TOP1 cleavage complexes (TOP1ccs) and TOP2ccs.
    LMP517
  • HY-18350
    Indimitecan
    		Inhibitor 98.30%
    Indimitecan (LMP776) is a topoisomerase I (Top1) inhibitor with anticancer activities.
    Indimitecan
  • HY-100777
    DACA
    		Inhibitor ≥98.0%
    DACA inhibits two essential nuclear enzymes in vitro, DNA topoisomerase I and DNA topoisomerase (topo) II. DACA stabilises topo I, topo II alpha, and topo II beta cleavable complexes in human leukaemia CCRF-CEM cells.
    DACA
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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