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-173625
    P5(PEG12)-VC-PAB-Exatecan
    		Inhibitor
    P5(PEG12)-VC-PAB-Exatecan (LP3) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker P5(PEG24)-VC-PAB to make antibody agent conjugate (ADC). P5(PEG12)-VC-PAB-Exatecan can be used for the research of tumor.
    P5(PEG12)-VC-PAB-Exatecan
  • HY-149348
    DiPT-4
    		Inhibitor
    DiPT-4 is a dual TOP1/PARP1 inhibitor that induces massive DNA double-strand breaks (DSBs), cell cycle arrest, and apoptosis in cancer cells. DiPT-4 has the potential to overcome cancer drug resistance.
    DiPT-4
  • HY-101647R
    Intoplicine (Standard)
    		Inhibitor
    Intoplicine (Standard) is the analytical standard of Intoplicine (HY-101647). This product is intended for research and analytical applications. Intoplicine (RP 60475), an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA.
    Intoplicine (Standard)
  • HY-177495
    LD-38
    		Inhibitor
    LD-38 is a drug-linker conjugate for ADC. LD-38 consists of a topoisomerase 1 inhibitor (Exatecan) (HY-13631) and a highly hydrophilic stable and cleavable linker. LD-38 can be used for synthesis of ADCs, such as KA-3123-LD38.
    LD-38
  • 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-183700
    DNA gyrase/Topo IV-IN-3
    		Inhibitor
    DNA gyrase/Topo IV-IN-3 is an inhibitor of Escherichia coli DNA gyrase and Topoisomerase IV, with IC50 values of 1.75 μM and 3.47 μM, respectively. DNA gyrase/Topo IV-IN-3 acts as a biofilm inhibitor and exhibits antibacterial activity against both Gram-negative and Gram-positive bacteria. DNA gyrase/Topo IV-IN-3 can be used in studies related to bacterial infections.
    DNA gyrase/Topo IV-IN-3
  • 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-178330
    IKE16
    		Inhibitor
    IKE16 is a fungi-selective eukaryotic topoisomerase II inhibitor, with an IC50 value of 13.68 μM. IKE16 suppresses both the DNA relaxation activity and the decatenation activity of yTOPOII selectively. IKE16 shows moderate activity against standard fungal strains (Candida albicans ATCC 10231, Saccharomyces cerevisiae ATCC 89763) with a minimum inhibitory concentration (MIC) of 2 μg/mL against S. cerevisiae ATCC 89763. IKE16 exhibits high cytotoxicity against human cells, with an EC50 of 0.07 μM in HepG2 and 0.045 μM in HEK-293. IKE16 can be used for the study of antifungal infection.
    IKE16
  • 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-181819
    Antibacterial agent 327
    		Inhibitor
    Antibacterial agent 327 (Compound 6f) is an Antibacterial agent. Antibacterial agent 327 potently inhibits the supercoiling activity of Staphylococcus aureus DNA gyrase with an IC50 of 0.28 μM. It also inhibits the ATPase activities of DNA gyrase and Topoisomerase IV, as well as the decatenation activity of Topoisomerase IV (IC50: 0.43 μM, 0.73 μM, and 2.31 μM, respectively). Antibacterial agent 327 potently inhibits Clostridioides difficile and methicillin-resistant Staphylococcus aureus (HY-121544), with an MIC of 0.78 μg/mL for both. Antibacterial agent 327 inhibits Escherichia coli with an MIC50 of 0.78 μg/mL.
    Antibacterial agent 327
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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