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-10581
    Gatifloxacin
    		Inhibitor 99.69%
    Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic that can cross the blood-brain barrier, with broad-spectrum antibacterial activity. Gatifloxacin 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 can be used to treat bacterial conjunctivitis in vivo.
    Gatifloxacin
  • HY-N0095
    (S)-10-Hydroxycamptothecin
    		Inhibitor 99.74%
    (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
  • HY-13566
    Belotecan
    		Inhibitor 99.86%
    Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer.
    Belotecan
  • HY-156617
    Cyclopropaneacetamide-Exatecan
    		Inhibitor 99.60%
    Cyclopropaneacetamide-Exatecan is an Exatecan (HY-13631) analogue and an ADC Cytotoxin. Cyclopropaneacetamide-Exatecan can be used to synthesize ADC molecules for cancer research.
    Cyclopropaneacetamide-Exatecan
  • HY-148819A
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT hydrochloride
    		Inhibitor 98.46%
    NH2-bicyclopentane-7-MAD-MDCPT hydrochloride (Formula I) is a topoisomerase I (TOP1) inhibitor. NH2-bicyclopentane-7-MAD-MDCPT hydrochloride is applicable to the synthesis of the ADC ABBV-969. NH2-bicyclopentane-7-MAD-MDCPT hydrochloride is used in research on lung adenocarcinoma and melanoma.
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT hydrochloride
  • HY-164792
    DBCO-PEG3-VC-Exatecan
    		Inhibitor
    DBCO-PEG3-VC-Exatecan (compound 25) is a Drug-Linker Conjugate for ADC. DBCO-PEG3-VC-Exatecan contains the ADC linker (DBCO-PEG3-VC) and a DNA topoisomerase I inhibitor Exatecan (HY-13631).
    DBCO-PEG3-VC-Exatecan
  • HY-W010800A
    Cholesterol hemisuccinate Tris salt
    		Inhibitor 99.98%
    Cholesterol hemisuccinate (Cholesterol hydrogen succinate) Tris salt is a compound with hepatoprotective and anticancer activity. Cholesterol hemisuccinate Tris salt inhibits Acetaminophen (AAP) (HY-66005) hepatotoxicity, and prevents AAP-induced hepatic apoptosis and necrosis. Cholesterol hemisuccinate Tris salt inhibits DNA polymerase and DNA topoisomerase to inhibit DNA replication and repair and cell division. Cholesterol hemisuccinate Tris salt inhibits tumor growth. Cholesterol hemisuccinate Tris salt can be used for buffer preparation.
    Cholesterol hemisuccinate Tris salt
  • HY-177442
    DS-3939a
    		Inhibitor 99.15%
    DS-3939a (DS-3939) is an anti-TA-MUC1 (tumor-associated mucin-1) antibody-drug conjugate (ADC). DS-3939a consists of a humanized anti-TA-MUC1 IgG1 monoclonal antibody Gatipotuzumab ( HY-P99634), a stable and cleavable tetrapeptide-based linker (Gly-Gly-Phe-Gly), and a DNA topoisomerase I inhibitor payload (DXd) (HY-13631D), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). DS-3939a inhibits the growth of TA-MUC1-positive cancer cells (CFPAC-1, NCI-H2110) by inducing DNA damage and apoptosis. DS-3939a exhibits significant antitumor activity in a variety of TA-MUC1-expressing advanced solid tumors. DS-3939a can be used for the study of TA-MUC1-expressing advanced cancers.
    DS-3939a
  • HY-153795
    Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan
    		Inhibitor 98.62%
    Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan is a bioactive drug-linker conjugate for ADC (Drug-Linker Conjugates for ADC). Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan consists of Exatecan (HY-13631) and a linker. Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan is applicable to ADC synthesis and cancer research. Exatecan acts as a DNA Topoisomerase I inhibitor.
    Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan
  • HY-148819
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT
    		Inhibitor 98.71%
    NH2-bicyclopentane-7-MAD-MDCPT (Formula I) is a topoisomerase I (TOP1) inhibitor. NH2-bicyclopentane-7-MAD-MDCPT is applicable to the synthesis of the ADC ABBV-969. NH2-bicyclopentane-7-MAD-MDCPT is used in research on lung adenocarcinoma and melanoma.
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT
  • HY-170554
    ABBV-706
    		Inhibitor 99.71%
    ABBV-706 is a SEZ6-targeted topoisomerase 1 inhibitor Antibody-Drug Conjugates (ADCs), which is composed of the Linker-Payload conjugation (HY-148820) and the Anti-SEZ6 Antibody (SC17) (HY-P991041). ABBV-706 can inhibit cancer cells proliferation and induce DNA damage and G2/M arrest. ABBV-706 exhibits high efficacy against small cell lung cancer (SCLC), neuroendocrine tumors (NENs) and central nervous system (CNS) tumors.
    ABBV-706
  • HY-13768
    Topotecan
    		Inhibitor 98.04%
    Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity.
    Topotecan
  • HY-13551
    Amsacrine
    		Inhibitor 99.95%
    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
  • HY-100875
    Bisantrene
    		Inhibitor 98.06%
    Bisantrene is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene targets eukaryotic type II topoisomerases. Bisantrene is a substrate of MDR1.
    Bisantrene
  • HY-13704S
    SN-38-d3
    		Inhibitor 98.79%
    SN-38-d3 is the deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively.
    SN-38-d<sub>3</sub>
  • HY-153360
    MC-GGFG-AM-(10Me-11F-Camptothecin)
    		Inhibitor 98.99%
    MC-GGFG-AM-(10Me-11F-Camptothecin) is a linker-payload conjugate used to synthesize ZW251. ZW251 an antibody-drug conjugate (ADC) targeting human GPC3. ZW251 consists of a humanized IgG1 antibody conjugated to a novel camptothecin-based topoisomerase 1 inhibitor, ZD06519, via a linker. The linker is the maleimide anchor and a glycyl glycyl phenylalanyl glycine (GGFG)-aminomethyl (AM) cleavable linker. ZW251 has high affinity with human and cynomolgus monkey GPC3. ZW251 displays rapid internalization in GPC3-expressing HCC cell lines, and bystander-mediated killing of GPC3 negative cancer cells.
    MC-GGFG-AM-(10Me-11F-Camptothecin)
  • HY-19024
    Merbarone
    		Inhibitor 99.49%
    Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage without stabilizing topo II-DNA covalent complexes. Merbarone is an anticancer agent.
    Merbarone
  • HY-B0526
    Flumequine
    		Inhibitor 99.65%
    Flumequine (R-802) is a quinolone antibiotic, and acts as a topoisomerase II inhibitor, with an IC50 of 15 μM (3.92 μg/mL).
    Flumequine
  • HY-122550
    Artemisitene
    		Inhibitor 99.93%
    Artemisitene, a natural derivative of Artemisinin, is a Nrf2 activator with antioxidant and anticancer activities. Artemisitene activates Nrf2 by decreasing Nrf2 ubiquitination and increasing its stability.
    Artemisitene
  • HY-147095
    Val-Ala-PABC-Exatecan
    		Inhibitor 99.90%
    Val-Ala-PABC-Exatecan is a Drug-Linker Conjugates for ADC, consiting of a cleavable Tesirine linker (Val-Ala-PABC) and Exatecan (HY-13631) (topoisomerase I inhibitor). Val-Ala-PABC-Exatecan can be used for ADC molecues synthesis, such as Mal-PEGn-amide-va-Exatecan.
    Val-Ala-PABC-Exatecan
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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