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-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-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-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-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-167671
    BE-10988
    		Inhibitor
    BE-10988 is a DNA topoisomerase inhibitor. BE-10988 inhibits the growth of Doxorubicin (HY-15142A)-resistant and vincristine-resistant P388 mouse leukemia cell lines by increasing the formation of DNA topoisomerase complexes.
    BE-10988
  • 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-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-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-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-122575R
    Aurintricarboxylic acid (Standard)
    		Inhibitor
    Aurintricarboxylic acid (Standard) is the analytical standard of Aurintricarboxylic acid. This product is intended for research and analytical applications. Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway. Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM. Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 μM.
    Aurintricarboxylic acid (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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