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-17028R
    Besifloxacin Hydrochloride (Standard)
    		Inhibitor
    Besifloxacin (Hydrochloride) (Standard) is a fourth generation fluoroquinolone antibiotic. Besifloxacin Hydrochloride (Standard) is a DNA gyrase and topoisomerase IV inhibitor. Besifloxacin Hydrochloride (Standard) has broad-spectrum antibacterial activity, it is effective against Gram-negative and Gram-positive aerobic and anaerobic strains and reduces the incidence of drug resistance. Besifloxacin Hydrochloride (Standard) has anti-inflammatory activity. Besifloxacin Hydrochloride (Standard) can be used in bacterial conjunctivitis research.
    Besifloxacin Hydrochloride (Standard)
  • HY-13727AS
    Pixantrone-d8
    		Inhibitor
    Pixantrone-d8 (BBR 2778-d8) is deuterium-labeled Pixantrone (HY-13727A).
    Pixantrone-d<sub>8</sub>
  • HY-N12747
    Dichlorogelignate
    		Inhibitor
    Dichlorogelignate (compound 4) is a selective inhibitor of topoisomerase II (Topo II). Dichlorogelignate has 100% inhibition at 50 μM.
    Dichlorogelignate
  • HY-156516A
    10NH2-11F-Camptothecin TFA
    		Inhibitor
    10NH2-11F-Camptothecin TFA is a Camptothecin (HY-16560) analogue that serves as an ADC cytotoxin for the synthesis of antibody-drug conjugates (ADCs). 10NH2-11F-Camptothecin TFA has anticancer effects (WO2022246576A1; compound 140).
    10NH2-11F-Camptothecin TFA
  • HY-13670A
    Lurtotecan dihydrochloride
    		Inhibitor
    Lurtotecan dihydrochloride (GI147211), a semisynthetic Camptothecin analog, is a topoisomerase I inhibitor. Lurtotecan dihydrochloride has anticancer effects.
    Lurtotecan dihydrochloride
  • HY-152187
    Topoisomerase IIα-IN-5
    		Inhibitor
    Topoisomerase IIα-IN-5 is a topoisomerase II (topo II) α catalytic inhibitor. Topoisomerase IIα-IN-5 intercalates into DNA and binds to the DNA minor groove. Topoisomerase IIα-IN-5 exhibits better efficacy and less genotoxicity than Etoposide (HY-13629).
    Topoisomerase IIα-IN-5
  • HY-169261
    7-Methoxy-9-methylfuro[2,3-b]-quinoline-4,5,8(9H)-trione
    		Inhibitor
    7-Methoxy-9-methylfuro[2,3-b]-quinoline-4,5,8(9H)-trione is a synthetic intermediate that can been used in the synthesis of the alkaloid Acronycidine.
    7-Methoxy-9-methylfuro[2,3-b]-quinoline-4,5,8(9H)-trione
  • HY-14780
    Viquidacin
    		Inhibitor
    Viquidacin (NXL 101) is an antibiotic with inhibitory activity against topoisomerase IV and DNA gyrase. Viquidacin exhibits antibacterial activity against gram positive bacterial by inhibiting the supercoiling, decatenation and relaxation in strains Staphylococcus aureus and Escherichia coli in micromolar levels. Viquidacin inhibits S. aureus wildtype and mutants with MIC of 2-128 mg/L.
    Viquidacin
  • HY-B0330BS1
    Levofloxacin-d3 hydrochloride
    		Inhibitor
    Levofloxacin-d3 ((-)-Ofloxacin-d3) hydrochlorideis deuterium labeled Levofloxacin (hydrochloride). 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-d<sub>3</sub> hydrochloride
  • HY-N11698
    Bakuchicin
    		Inhibitor
    Bakuchicin (Allopsoralen) is a compound that can be found in Psoralea corylifolia. It has certain inhibitory activity against topoisomerase II. In the cell model infected with Simian virus 40 (SV40), the IC50 of Bakuchicin against topoisomerase II is 404 μM. Bakuchicin can be used in the research of the anti-infection field.
    Bakuchicin
  • HY-B1050R
    Gemifloxacin (mesylate) (Standard)
    		Inhibitor
    Gemifloxacin (mesylate) (Standard) is the analytical standard of Gemifloxacin (mesylate). This product is intended for research and analytical applications. Gemifloxacin mesylate (SB-265805S; LB-20304a) is an orally active broad-spectrum quinolone antibacterial antibiotic. Gemifloxacin mesylate inhibits DNA synthesis by inhibiting DNA gyrase and Topoisomerase IV activities. Gemifloxacin mesylate has potent antibacterial activities against gram-positive bacteria in vitro efficacy study, particularly Streptococci and Staphylococci. Gemifloxacin mesylate has been used in the research of respiratory tract infections.
    Gemifloxacin (mesylate) (Standard)
  • HY-16742C
    Gepotidacin hydrochloride
    		Inhibitor
    Gepotidacin hydrochloride is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor.
    Gepotidacin hydrochloride
  • HY-122481
    Thaspine acetate
    		Inhibitor
    Thaspine acetate, an alkaloid, is a topoisomerase I and II inhibitor. Thaspine acetate induces cancer cell apoptosis. Thaspine acetate induces Bak and Bax activation, mitochondrial cytochrome c release and mitochondrial membrane permeabilization. Thaspine acetate can be isoalted from the cortex of the South American tree Croton lechleri.
    Thaspine acetate
  • HY-400316
    Exatecan intermediate 8
    		Inhibitor
    Exatecan intermediate 8 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 8
  • HY-173634
    Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan
    		Inhibitor
    Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan (LP1) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB (HY-173635) to make antibody agent conjugate (ADC), AZD0516.
    Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan
  • HY-46081
    Exatecan Intermediate 3
    		Inhibitor
    Exatecan Intermediate 3 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 3 can be used to synthesize Antibody-Drug Conjugates (ADCs).
    Exatecan Intermediate 3
  • HY-161813
    Antibacterial agent 229
    		Inhibitor
    Antibacterial agent 229 (compound 8a) is a potent antibacterial agent. Antibacterial agent 229 shows antibacterial and antifungal abilities. Antibacterial agent 229 disrupts the integrity of the bacterial membrane, intercalates into DNA. Antibacterial agent 229 inhibits topoisomerase IV with an IC50 value of 10.88 µM.
    Antibacterial agent 229
  • HY-117657
    (-)-BO 2367
    		Inhibitor
    (-)-BO 2367, an antimicrobial quinolone, is a strong mammalian and bacterial topoisomerase II inhibitor. (-)-BO 2367 shows IC50 values with 3.8 μM, 0.5 μM, and 1 μM against the DNA relaxation activity of L1210 topoisomerase II and the supercoiling activities of Escherichia coli gyrase and Micrococcus luteus gyrase, respectively. (-)-BO 2367 is a potent antitumor agent.
    (-)-BO 2367
  • 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-W178011
    Topoisomerase IIα-IN-9
    		Inhibitor
    Topoisomerase IIα-IN-9 (NSC85582) is a bisphenol compound that has a moderate inhibitory effect on DNA topoisomerase Topoisomerase II (IC50: 571 μM). Topoisomerase IIα-IN-9 also exhibits a certain cell growth inhibitory effect, with IC50s of 117 μM and 218 μM for K562 and CHO, respectively.
    Topoisomerase IIα-IN-9
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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