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-W744739
    Betulinic acid-d3
    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-d<sub>3</sub>
  • HY-174227
    Topoisomerase inhibitor 6
    		Inhibitor
    Topoisomerase inhibitor 6 (Compound REDX05931) is a dual irreversible inhibitor of DNA gyrase and topoisomerase IV (MIC=0.06 μg/mL against fluoroquinolone-resistant S. aureus). Topoisomerase inhibitor 6 blocks DNA strand break-reunion, inducing lethal DNA damage. Topoisomerase inhibitor 6 is promising for research of Gram-positive bacterial infections (e.g., S. aureus, S. pneumoniae).
    Topoisomerase inhibitor 6
  • HY-13725R
    Pirarubicin (Standard)
    		Inhibitor
    Pirarubicin (Standard) is the analytical standard of Pirarubicin. This product is intended for research and analytical applications. Pirarubicin 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 (Standard)
  • HY-13721R
    Phenoxodiol (Standard)
    		Inhibitor
    Phenoxodiol (Standard) is the analytical standard of Phenoxodiol. This product is intended for research and analytical applications. Phenoxodiol (Idronoxil), a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21WAF1 via a p53 independent manner.
    Phenoxodiol (Standard)
  • HY-49861
    Exatecan intermediate 11
    		Inhibitor
    Exatecan intermediate 11 is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM).
    Exatecan intermediate 11
  • HY-101064S4
    Fmoc-leucine-15N
    		Inhibitor 98.5%
    Fmoc-leucine-15N is a 15N-labeled and 15N-labled Fmoc-leucine (HY-101064).
    Fmoc-leucine-<sup>15</sup>N
  • HY-42487R
    Exatecan Intermediate 1 (Standard)
    		Inhibitor
    Exatecan Intermediate 1 (Standard) is the analytical standard of Exatecan Intermediate 1. This product is intended for research and analytical applications. Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor with anticancer effects.
    Exatecan Intermediate 1 (Standard)
  • HY-119425R
    Razoxane (Standard)
    		Inhibitor
    Razoxane (Standard) is the analytical standard of Razoxane. This product is intended for research and analytical applications. Razoxane (ICRF 159) is an antiangiogenic topoisomerase II inhibitor, can be used for the research of renal cell carcinoma (RCC).
    Razoxane (Standard)
  • HY-114684
    A20832
    		Inhibitor
    A20832 is a specific resolvase inhibitor that blocks both the recombination and topoisomerase activities of resolvase. A20832 inhibits the site-specific recombination reaction mediated by the Tn3-encoded resolvase protein at the strand cleavage step and has no effect on synapsis.
    A20832
  • HY-19024R
    Merbarone (Standard)
    		Inhibitor
    Merbarone (Standard) is the analytical standard of Merbarone. This product is intended for research and analytical applications. Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage without stabilizing topo II-DNA covalent complexes. Merbarone is an anticancer agent.
    Merbarone (Standard)
  • HY-106662R
    Chloroquinoxaline sulfonamide (Standard)
    		Inhibitor
    Chloroquinoxaline sulfonamide (Standard) is the analytical standard of Chloroquinoxaline sulfonamide. This product is intended for research and analytical applications. Chloroquinoxaline sulfonamide (Chloroquinoxaline), a structural analogue of sulfaquinoxaline, is a topoisomerase II alpha/beta poison. Chloroquinoxaline sulfonamide is used to control coccidiosis in poultry, rabbit, sheep, and cattle. Antitumor activity.
    Chloroquinoxaline sulfonamide (Standard)
  • HY-N6054R
    Niranthin (Standard)
    		Inhibitor
    Niranthin (Standard) is the analytical standard of Niranthin. This product is intended for research and analytical applications. Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis research.
    Niranthin (Standard)
  • HY-156464
    Topoisomerase I inhibitor 10
    		Inhibitor
    Topoisomerase I inhibitor 10 (compound 13) is a leishmanial topoisomerase IB inhibitor. Topoisomerase I inhibitor 10 has antileishmanial activity against L. donovani promastigotes, with the IC50 of 27.91 μM.
    Topoisomerase I inhibitor 10
  • HY-10581B
    Gatifloxacin mesylate
    		Inhibitor
    Gatifloxacin mesylate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin mesylate 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 mesylate can be used to treat bacterial conjunctivitis in vivo.
    Gatifloxacin mesylate
  • HY-W781148
    Suptopin-2
    		Inhibitor
    Sutopin-2 is a topoisomerase II inhibitor. Suptopin-2 affects cell cycle progression and stability of microtubules. Sutopin-2 induces cell cycle arrest by regulating the nucleocytoplasmic transport of cyclin B1.
    Suptopin-2
  • HY-167671
    BE-10988
    		Inhibitor
    BE-10988 is a DNA topoisomerase inhibitor. BE-10988 inhibits the growth of Doxorubicin (HY-15142A)-resistant and vincristine-resistant P388 mouse leukemia cell lines by increasing the formation of DNA topoisomerase complexes.
    BE-10988
  • HY-N2306R
    Aclacinomycin A (Standard)
    		Inhibitor
    Aclacinomycin A (Standard) is the analytical standard of Aclacinomycin A. This product is intended for research and analytical applications. Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis.
    Aclacinomycin A (Standard)
  • HY-N0095S
    (S)-10-Hydroxycamptothecin-d5
    (S)-10-Hydroxycamptothecin-d5 (10-HCPT-d5) is the deuterium labeled (S)-10-Hydroxycamptothecin. (S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia research.
    (S)-10-Hydroxycamptothecin-d5
  • HY-132545S
    RPR132595A-d3
    RPR132595A-d3 is the deuterium labeled RPR132595A. RPR132595A is an active metabolite of Irinotecan (CPT-11), which is generated by cytochrome P-450 3A4 (CYP3A4) and finally excreted through urine.
    RPR132595A-d3
  • HY-B0395D
    (1R,2S,7R)-Sitafloxacin
    		Inhibitor
    (R)-Sitafloxacin (DU-6857), a stereoisomer of Sitafloxacin (DU-6859a), is also an inhibitor of topoisomerases, with an IC50 of 0.18 μg/mL of DNA gyrase.
    (1R,2S,7R)-Sitafloxacin
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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