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-W897655
    20-O-Acetylcamptothecin
    		Inhibitor ≥98.0%
    20-O-Acetylcamptothecin (O-Acetylcamptothecin) is a derivative of Camptothecin (HY-16560) and an inhibitor of Topoisomerase I.
    20-O-Acetylcamptothecin
  • HY-158329
    Alloc-DOX
    		Inhibitor 98.40%
    Alloc-DOX (N-Alloc doxorubicin) is a Doxorubicin (HY-15142A) prodrug. The combination of a catalyst (such as nano-palladium) and alloc-DOX leads to a decrease in cell viability and tumour growth.
    Alloc-DOX
  • HY-164836
    Deruxtecan-Eribulin
    		Inhibitor
    Deruxtecan-Eribulin is a Drug-Linker Conjugates for ADC, which is composed of a linker and a toxic molecule Exatecan (HY-13631) (DNA topoisomerase I inhibitor) and Eribulin (HY-13442) (Microtubule inhibitor). Deruxtecan-Eribulin can be used for ADC synthesis.
    Deruxtecan-Eribulin
  • HY-13618
    Edotecarin
    		Inhibitor 98.39%
    Edotecarin is a potent inhibitor of topoisomerase I that can induces single-strand DNA cleavage, with IC50 of 50 nM.
    Edotecarin
  • HY-107096B
    CH-0793076 TFA
    		Inhibitor 98.71%
    CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein).
    CH-0793076 TFA
  • HY-162959
    BWC0977
    		Inhibitor
    BWC0977 is a potent bacterial topoisomerase inhibitor that inhibits bacterial DNA replication via inhibition of DNA gyrase and topoisomerase IV. BWC0977 exhibits a minimum inhibitory concentration (MIC90) of 0.03-2 µg/mL against MDR (Multi-Drug Resistant) Gram-negative bacteria.
    BWC0977
  • HY-106410
    Zabofloxacin
    		Inhibitor 98.02%
    Zabofloxacin (DW-224a Free base) is a potent and seletive inhibitor of the bacterial type II and IV topoisomerases. Zabofloxacin has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia. Zabofloxacin is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP).
    Zabofloxacin
  • HY-171931
    Aminocaproyl-Val-Cit-PABC-Exatecan
    		Inhibitor
    Aminocaproyl-Val-Cit-PABC-Exatecan is a drug-linker conjugate for ADC, consiting of a cleavable linker (Aminocaproyl-Val-Cit-PABC) and Exatecan (HY-13631) (topoisomerase I inhibitor). Aminocaproyl-Val-Cit-PABC-Exatecan can be used for ADC molecues synthesis.
    Aminocaproyl-Val-Cit-PABC-Exatecan
  • HY-18351A
    Indotecan hydrochloride
    		Inhibitor 99.80%
    Indotecan hydrochloride, an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan hydrochloride prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis.
    Indotecan hydrochloride
  • HY-132164B
    Gly-7-MAD-MDCPT TFA
    		Inhibitor
    Gly-7-MAD-MDCPT (Compound 4b) TFA is an anticancer agent. Gly-7-MAD-MDCPT TFA is a Camptothecin (HY-16560) compound, which shows cytotoxicity to various cancer cells with IC50 values of 10-1000 nM.
    Gly-7-MAD-MDCPT TFA
  • HY-43565B
    Exatecan intermediate 10
    		Inhibitor 99.92%
    Exatecan intermediate 10 is an intermediate in the synthesis of Exatecan (HY-13631).Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 of 2.2 μM (0.975 μg/mL) for use in cancer research.
    Exatecan intermediate 10
  • HY-106582
    Sobuzoxane
    		Inhibitor 98.05%
    Sobuzoxane (MST-16) is an orally active topoisomerase II inhibitor. Sobuzoxane causes irreversible inhibition of cell division. Sobuzoxane can be used in the study of non-Hodgkin's lymphoma that is resistant to conventional chemotherapy or has recurred.
    Sobuzoxane
  • HY-B0067A
    Amrubicin hydrochloride
    		Inhibitor 98.78%
    Amrubicin (SM-5887) hydrochloride is a DNA topoisomerase II inhibitor, used for the research of cancer.
    Amrubicin hydrochloride
  • HY-13727
    Pixantrone free base
    		Inhibitor
    Pixantrone (BBR 2778 (free base)), a mitoxantrone analog, is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
    Pixantrone free base
  • HY-W010800R
    Cholesteryl hemisuccinate (Standard)
    		Inhibitor
    Cholesteryl hemisuccinate (Standard) is the analytical standard of Cholesteryl hemisuccinate. This product is intended for research and analytical applications. Cholesteryl hemisuccinate is a with hepatoprotective an anticancer activity. Cholesteryl hemisuccinate inhibits Acetaminophen (AAP, HY-66005) hepatotoxicity, and prevents AAP-induced hepatic apoptosis and necrosis. Cholesteryl hemisuccinate inhibits DNA polymerase and DNA topoisomerase to inhibit DNA replication and repair and cell division. Thus, Cholesteryl hemisuccinate inhibits tumor growth[1][2].
    Cholesteryl hemisuccinate (Standard)
  • HY-13758
    TAS-103
    		Inhibitor
    TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
    TAS-103
  • HY-B0398R
    Nalidixic acid (Standard)
    		Inhibitor
    Nalidixic acid (Standard) is the analytical standard of Nalidixic acid. This product is intended for research and analytical applications. Nalidixic acid, a quinolone antibiotic, is effective against both gram-positive and gram-negative bacteria. Nalidixic acid acts in a bacteriostatic manner in lower concentrations and is bactericidal in higher concentrations. Nalidixic acid inhibits a subunit of DNA gyrase and topoisomerase IV and reversibly blocks DNA replication in susceptible bacteria.
    Nalidixic acid (Standard)
  • HY-16261A
    MC-DOXHZN
    		Inhibitor
    MC-DOXHZN ((E/Z)-Aldoxorubicin) is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), with acid-sensitive properties.
    MC-DOXHZN
  • HY-118942
    Topovale
    		Inhibitor 99.94%
    Topovale (ARC 111) is a topoisomerase I inhbitor. Topovale is an antitumor agent, and shows low nM cytotoxicity against a panel of cancer cells. Topovale induces reversible topoisomerase I (TOP1) cleavage complexes in tumor cells.
    Topovale
  • HY-B0356BR
    Ciprofloxacin hydrochloride monohydrate (Standard)
    		Inhibitor
    Ciprofloxacin (hydrochloride monohydrate) (Standard) is the analytical standard of Ciprofloxacin (hydrochloride monohydrate). This product is intended for research and analytical applications. Ciprofloxacin (Bay-09867) hydrochloride monohydrate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin hydrochloride monohydrate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin hydrochloride monohydrate has anti-proliferative activity and induces apoptosis. Ciprofloxacin hydrochloride monohydrate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
    Ciprofloxacin hydrochloride monohydrate (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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