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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. Nombre del producto Efecto Pureza Chemical Structure
  • HY-162959
    BWC0977
    		Inhibitor
    BWC0977 is an antibacterial agent that inhibits bacterial DNA replication via inhibition of DNA gyrase and topoisomerase IV. BWC0977 exhibits a minimum inhibitory concentration (MIC90) of 0.03-2 µg/mL against MDR (Multi-Drug Resistant) Gram-negative bacteria.
    BWC0977
  • HY-174277
    Antitumor agent-203
    		Inhibitor 99.07%
    Antitumor agent-203 (例7) is a derivative of Exatecan (DX-8951) (HY-13631) and can be used to prepare antibody-drug conjugates (ADCs), as the ADC Cytotoxin.
    Antitumor agent-203
  • HY-106410
    Zabofloxacin
    		Inhibitor 98.02%
    Zabofloxacin (DW-224a Free base) is a potent and seletive inhibitor of the bacterial type II and IV topoisomerases. Zabofloxacin has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia. Zabofloxacin is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP).
    Zabofloxacin
  • HY-157797
    SN-38-CM2
    		Control
    SN-38-CM2 is a split esterase, and shows >95% conversion to SN-38 within 5 min in vitro. SN-38-CM2 induces protein-protein interactions (PPI)-dependent esterase to mediate cell death in MDA-MB-231 cells.
    SN-38-CM2
  • HY-171931
    Aminocaproyl-Val-Cit-PABC-Exatecan
    		Inhibitor
    Aminocaproyl-Val-Cit-PABC-Exatecan is a drug-linker conjugate for ADC, consiting of a cleavable linker (Aminocaproyl-Val-Cit-PABC) and Exatecan (HY-13631) (topoisomerase I inhibitor). Aminocaproyl-Val-Cit-PABC-Exatecan can be used for ADC molecues synthesis.
    Aminocaproyl-Val-Cit-PABC-Exatecan
  • HY-18351A
    Indotecan hydrochloride
    		Inhibitor 99.80%
    Indotecan hydrochloride, an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan hydrochloride prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis.
    Indotecan hydrochloride
  • HY-132164B
    Gly-7-MAD-MDCPT TFA
    		Inhibitor
    Gly-7-MAD-MDCPT (Compound 4b) TFA is an anticancer agent. Gly-7-MAD-MDCPT TFA is a Camptothecin (HY-16560) compound, which shows cytotoxicity to various cancer cells with IC50 values of 10-1000 nM.
    Gly-7-MAD-MDCPT TFA
  • HY-19637
    SW044248
    		Inhibitor 99.60%
    SW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.
    SW044248
  • HY-12888
    AZD5099
    		Inhibitor 98.40%
    AZD5099, an antibacterial agent, is a potent and selective bacterial topoisomerase II inhibitor. AZD5099 potently inhibits the infections caused by Gram-positive and fastidious Gram-negative bacteria.
    AZD5099
  • HY-W744739
    Betulinic acid-d3
    		99.9%
    Betulinic acid-d3 (Lupatic acid-d3) is a deuterium labeled Betulinic acid (HY-10529). Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties. Betulinic acid can cross the blood-brain barrier.
    Betulinic acid-d<sub>3</sub>
  • HY-W087058
    1,4-Di-tert-butylbenzene
    		Inhibitor 99.89%
    1,4-Di-tert-butylbenzene is a volatile compound identified in the hexane extracts of corn cob and green millet. 1,4-Di-tert-butylbenzene shows potent inhibition against receptor proteins of Bacterial type II topoisomerase (4PLB and LpxC) in docking analysis.
    1,4-Di-tert-butylbenzene
  • HY-B0067A
    Amrubicin hydrochloride
    		Inhibitor 98.78%
    Amrubicin (SM-5887) hydrochloride is a DNA topoisomerase II inhibitor, used for the research of cancer.
    Amrubicin hydrochloride
  • HY-13727
    Pixantrone free base
    		Inhibitor
    Pixantrone (BBR 2778 (free base)), a mitoxantrone analog, is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
    Pixantrone free base
  • HY-16562R
    Irinotecan (Standard)
    		Inhibitor
    Irinotecan (Standard) is the analytical standard of Irinotecan. This product is intended for research and analytical applications. Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.
    Irinotecan (Standard)
  • HY-B0879AR
    Suramin sodium salt (Standard)
    		Inhibitor
    Suramin (sodium salt) (Standard) is the analytical standard of Suramin (sodium salt). This product is intended for research and analytical applications. Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor. Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
    Suramin sodium salt (Standard)
  • HY-106702A
    Fostriecin
    		Inhibitor
    Fostriecin is a triene antibiotic. Fostriecin is a topoisomerase II and protein phosphatase PP2A inhibitor.
    Fostriecin
  • HY-17460
    Garenoxacin
    		Inhibitor 98.62%
    Garenoxacin (BMS284756) is an orally active quinolone antibiotic and has a broad spectrum of activity against a wide array of gram-positive and gram-negative bacteria, anaerobes, and fastidious organisms.
    Garenoxacin
  • 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; Doxorubicin(6-maleimidocaproyl)hydrazone) is an albumin-binding proagent of Doxorubicin (HY-15142A) (DNA topoisomerase II inhibitor), with acid-sensitive properties. MC-DOXHZN can be used to synthesize ADC.
    MC-DOXHZN
  • HY-118942
    Topovale
    		Inhibitor 99.94%
    Topovale (ARC 111) is a topoisomerase I inhbitor. Topovale is an antitumor agent, and shows low nM cytotoxicity against a panel of cancer cells. Topovale induces reversible topoisomerase I (TOP1) cleavage complexes in tumor cells.
    Topovale
Cat. No. Nombre del producto / Synonyms Species Source
Cat. No. Nombre del producto / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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