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-13727A
    Pixantrone
    		Inhibitor 98.75%
    Pixantrone (BBR 2778) dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
    Pixantrone
  • HY-13725A
    Pirarubicin Hydrochloride
    		Inhibitor 99.14%
    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.
    Pirarubicin Hydrochloride
  • HY-N2331
    Proscillaridin A
    		Inhibitor 99.74%
    Proscillaridin A is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively.
    Proscillaridin A
  • HY-B0356B
    Ciprofloxacin hydrochloride monohydrate
    		Inhibitor 99.88%
    Ciprofloxacin (Bay-09867) hydrochloride monohydrate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin hydrochloride monohydrate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin hydrochloride monohydrate has anti-proliferative activity and induces apoptosis. Ciprofloxacin hydrochloride monohydrate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
    Ciprofloxacin hydrochloride monohydrate
  • HY-15753
    Ellipticine
    		Inhibitor 99.56%
    Ellipticine (NSC 71795) is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.
    Ellipticine
  • HY-N0095
    (S)-10-Hydroxycamptothecin
    		Inhibitor 99.67%
    (S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment.
    (S)-10-Hydroxycamptothecin
  • HY-100875
    Bisantrene
    		Inhibitor 98.06%
    Bisantrene is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene targets eukaryotic type II topoisomerases. Bisantrene is a substrate of MDR1.
    Bisantrene
  • HY-148819A
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT hydrochloride
    		Inhibitor 98.46%
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT (compound I) hydrochloride 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 hydrochloride
  • HY-N0716A
    Berberine hemisulfate
    		Inhibitor 99.63%
    Berberine hemisulfate is the hemisulfate form of Berberine (HY-N0716). Berberine hemisulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian. Berberine hemisulfate exhibits anti-inflammatory, antibiobic, antitumor, cardiovascular protective and neuroprotective activity.
    Berberine hemisulfate
  • HY-10581
    Gatifloxacin
    		Inhibitor 99.69%
    Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin 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 can be used to treat bacterial conjunctivitis in vivo.
    Gatifloxacin
  • HY-13631F
    Gly-Gly-Phe-Gly-NH-O-CO-Exatecan hydrochloride
    		Inhibitor 99.89%
    Gly-Gly-Phe-Gly-NH-O-CO-Exatecan, as a drug-linker conjugate composed of linker Gly-Gly-Phe-Gly-NH-O-CO and Exatecan, can be used to prepare antibody conjugate drugs. Exatecan is a DNA topoisomerase I inhibitor that can be used in cancer research.
    Gly-Gly-Phe-Gly-NH-O-CO-Exatecan hydrochloride
  • HY-153892
    Gly-Mal-GGFG-Deruxtecan 2-hydroxypropanamide
    		Inhibitor 99.79%
    Gly-Mal-GGFG-Deruxtecan 2-hydroxypropanamide is the drug-linker conjugate for ADC, containing ADC linker Gly-Mal-GGFG and ADC cytotoxin Deruxtecan 2-hydroxypropanamide.
    Gly-Mal-GGFG-Deruxtecan 2-hydroxypropanamide
  • HY-164152
    ADC Control Human IgG1-Deruxtecan (DAR 4)
    		Inhibitor
    ADC Control Human IgG1-Deruxtecan (DAR 4) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E).
    ADC Control Human IgG1-Deruxtecan (DAR 4)
  • HY-13631AG
    Exatecan (mesylate) (GMP)
    		Inhibitor
    Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan 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) (GMP)
  • HY-13704S
    SN-38-d3
    		Inhibitor 99.07%
    SN-38-d3 is the deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively.
    SN-38-d<sub>3</sub>
  • HY-118590
    ICRF-193
    		Inhibitor 99.64%
    ICRF-193 is an TopoII inhibitor. (S,S)- and (R,R)-isomers ICRF-193 make up an racemic mixture, ICRF-196 (HY-118590A). ICRF-196 can be used for the research of cancer.
    ICRF-193
  • HY-153360
    MC-GGFG-AM-(10Me-11F-Camptothecin)
    		Inhibitor 98.99%
    MC-GGFG-AM-(10Me-11F-Camptothecin) is a linker-payload conjugate used to synthesize ZW251. ZW251 an antibody-drug conjugate (ADC) targeting human GPC3. ZW251 consists of a humanized IgG1 antibody conjugated to a novel camptothecin-based topoisomerase 1 inhibitor, ZD06519, via a linker. The linker is the maleimide anchor and a glycyl glycyl phenylalanyl glycine (GGFG)-aminomethyl (AM) cleavable linker. ZW251 has high affinity with human and cynomolgus monkey GPC3. ZW251 displays rapid internalization in GPC3-expressing HCC cell lines, and bystander-mediated killing of GPC3 negative cancer cells.
    MC-GGFG-AM-(10Me-11F-Camptothecin)
  • HY-13551
    Amsacrine
    		Inhibitor 99.95%
    Amsacrine (m-AMSA; acridinyl anisidide) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
    Amsacrine
  • HY-122550
    Artemisitene
    		Inhibitor 99.93%
    Artemisitene, a natural derivative of Artemisinin, is a Nrf2 activator with antioxidant and anticancer activities. Artemisitene activates Nrf2 by decreasing Nrf2 ubiquitination and increasing its stability.
    Artemisitene
  • HY-164152A
    ADC Control Human IgG1-Deruxtecan (DAR 8)
    		Inhibitor
    ADC Control Human IgG1-Deruxtecan (DAR 8) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E).
    ADC Control Human IgG1-Deruxtecan (DAR 8)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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