1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. Topoisomerase

Topoisomerase

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-172229
    NBTI 5463
    Inhibitor
    NBTI 5463 is a bacterial type II topoisomerases (topoisomerase II) inhibitor with antibacterial activity. NBTI 5463 inhibits GyrA and TopoIV in Pseudomonas aeruginosa and Escherichia coli. NBTI 5463 binds to topoisomerase II to prevent DNA cleavage and religation, inhibiting bacterial DNA replication and transcription. NBTI 5463 is promising for research of Gram-negative bacterial infection.
    NBTI 5463
  • 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-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
  • 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-13704R
    SN-38 (Standard)
    Inhibitor
    SN-38 (Standard) is the analytical standard of SN-38. This product is intended for research and analytical applications. SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. SN-38 is a payload of sacituzumab govitecan (HY -132254).
    SN-38 (Standard)
  • HY-13551R
    Amsacrine (Standard)
    Inhibitor
    Amsacrine (Standard) is the analytical standard of Amsacrine. This product is intended for research and analytical applications. 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 (Standard)
  • HY-106702A
    Fostriecin
    Inhibitor
    Fostriecin is a triene antibiotic. Fostriecin is a topoisomerase II and protein phosphatase PP2A inhibitor.
    Fostriecin
  • HY-13565
    Becatecarin
    Inhibitor
    Becatecarin is a rebeccamycin analog with antitumor effects. Becatecarin intercalates into DNA and inhibites the catalytic activity of topoisomerases I/II.
    Becatecarin
  • HY-134290A
    8-Chloro-ATP tetrasodium
    Inhibitor
    8-Chloro-ATP tetrasodium, an ATP (HY-B2176) analog, is a topoisomerase II (Topo II) inhibitor. 8-Chloro-ATP tetrasodium inhibits DNA synthesis and induces DNA double-stranded breaks (DSBs). 8-Chloro-ATP tetrasodium inhibits Topo II-catalyzed ATP hydrolysis.
    8-Chloro-ATP tetrasodium
  • HY-161937
    Antibacterial agent 236
    Inhibitor
    Antibacterial agent 236 (Compound 4l) is an orally active inhibitor for DNA gyrase and topoisomerase IV (IC50 is 3.2 and 300 nM in Staphylococcus aureus), and exhibits board-spectrum antibacterial activity. Antibacterial agent 236 exhibits good pharmacokinetic properties in mice.
    Antibacterial agent 236
Cat. No. Product Name / Synonyms Species Source
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