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-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-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-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-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-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-B1099R
    Hycanthone (Standard)
    		Inhibitor
    Hycanthone (Standard) is the analytical standard of Hycanthone. This product is intended for research and analytical applications. Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent.
    Hycanthone (Standard)
  • HY-N15319
    Eupolauridine
    		Inhibitor
    Eupolauridine (Canangine) is a selective DNA topoisomerase II inhibitor with IC50 values of 20 μM for fungal topoisomerase I and 33 μM for human topoisomerase I. Eupolauridine exerts antifungal activity by inhibiting the catalytic activity of topoisomerase II and stabilizing its cleavage complex with DNA, leading to DNA damage. Eupolauridine is promising for research of fungal infectious diseases.
    Eupolauridine
  • 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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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