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-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
  • 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-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-d<sub>5</sub>
  • 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-d<sub>3</sub>
  • 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
  • HY-108969R
    Pyrazoloacridine (Standard)
    		Inhibitor
    Pyrazoloacridine (Standard) is the analytical standard of Pyrazoloacridine. This product is intended for research and analytical applications. Pyrazoloacridine (NSC 366140), an intercalating agent with anti-cancer activity, inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine (NSC 366140) exhibits an IC50 of 1.25 μM in K562 myeloid leukemia cells for 24 h treatment.
    Pyrazoloacridine (Standard)
  • HY-10581AS1
    Gatifloxacin-d4 hydrochloride
    		Inhibitor
    Gatifloxacin-d4 (AM-1155-d4; BMS-206584-d4; PD135432-d4) hydrochloride is deuterium-labeled Gatifloxacin (hydrochloride) (HY-10581A).
    Gatifloxacin-d<sub>4</sub> hydrochloride
  • HY-105387
    Heliquinomycin
    		Inhibitor
    Heliquinomycin is an inhibitor of DNA helicase (Ki: 6.8 μM) and inhibits DNA and RNA synthesis. Heliquinomycin is effective against Gram-positive bacteria strains. Heliquinomycin inhibits cancer cell growth.
    Heliquinomycin
  • HY-106410AR
    Zabofloxacin hydrochloride (Standard)
    		Inhibitor
    Zabofloxacin hydrochloride (Standard) is the analytical standard of Zabofloxacin hydrochloride (HY-106410A). This product is intended for research and analytical applications. Zabofloxacin hydrochloride (DW-224a) is a potent and seletive inhibitor of the bacterial type II and IV topoisomerases. Zabofloxacin hydrochloride has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia. Zabofloxacin hydrochloride is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP).
    Zabofloxacin hydrochloride (Standard)
  • HY-N0114AR
    (±)-Evodiamine (Standard)
    		Inhibitor
    (±)-Evodiamine (Standard) is the analytical standard of (±)-Evodiamine. This product is intended for research and analytical applications. (±)-Evodiamine, a quinazolinocarboline alkaloid, is a Top1 inhibitor. Evodiamine exhibits anti-inflammatory, antiobesity, and antitumor effects. (±)-Evodiamine inhibits the proliferation of a wide variety of tumor cells by inducing their apoptosis.
    (±)-Evodiamine (Standard)
  • HY-10534R
    Voreloxin (Standard)
    		Inhibitor
    Voreloxin (Standard) is the analytical standard of Voreloxin (HY-10534). This product is intended for research and analytical applications. Voreloxin (SNS-595; Vosaroxin; AG 7352) is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.
    Voreloxin (Standard)
  • HY-13551AR
    Amsacrine hydrochloride (Standard)
    		Inhibitor
    Amsacrine (hydrochloride) (Standard) is the analytical standard of Amsacrine (hydrochloride). This product is intended for research and analytical applications. Amsacrine hydrochloride (m-AMSA hydrochloride; acridinyl anisidide hydrochloride) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
    Amsacrine hydrochloride (Standard)
  • 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-108988
    Albicidin
    		Inhibitor
    Albicidin is a peptide antibiotic with phytotoxic activity. Albicidin potently inhibits bacterial and plant DNA gyrase at nanomolar concentrations, blocks DNA replication, and exhibits excellent antibacterial efficacy against multidrug-resistant bacteria. Albicidin possesses bactericidal activity against Gram-positive and Gram-negative microorganisms, and acts as a virulence factor for the systemic plant infection by Xanthomonas albilineans. Albicidin can be used in studies related to bacterial infections and sugarcane leaf blight.
    Albicidin
  • HY-13727AS
    Pixantrone-d8
    		Inhibitor
    Pixantrone-d8 (BBR 2778-d8) is deuterium-labeled Pixantrone (HY-13727A).
    Pixantrone-d<sub>8</sub>
  • HY-N0095R
    (S)-10-Hydroxycamptothecin (Standard)
    		Inhibitor
    (S)-10-Hydroxycamptothecin (Standard) is the analytical standard of (S)-10-Hydroxycamptothecin. This product is intended for research and analytical applications. (S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment.
    (S)-10-Hydroxycamptothecin (Standard)
  • 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-B0147B
    Pefloxacin mesylate dihydrate
    		98.11%
    Pefloxacin (Pefloxacinium) mesylate dihydrate is a broad spectrum antibiotic. Pefloxacin mesylate dihydrate blocks DNA replication by inhibiting DNA gyrase. Pefloxacin mesylate dihydrate inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin mesylate dihydrate exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin mesylate dihydrate has anti-Plasmodium yoelii infection activity. Pefloxacin mesylate dihydrate increase UVA-induced edema and immunesuppression. Pefloxacin mesylate dihydrate can be used for infection studies.
    Pefloxacin mesylate dihydrate
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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