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-14812
    Karenitecin
    		Inhibitor 98.02%
    Karenitecin (Cositecan) is a topoisomerase I inhibitor, with potent anti-cancer activity.
    Karenitecin
  • HY-N2063
    12-Ethyl-9-hydroxycamptothecin
    		99.89%
    12-Ethyl-9-hydroxycamptothecin is a derivative of Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM.
    12-Ethyl-9-hydroxycamptothecin
  • HY-14821
    Namitecan
    		Inhibitor 99.25%
    Namitecan is a potent topoisomerase I inhibitor, with antitumor property.
    Namitecan
  • HY-N5038
    Mauritianin
    		Inhibitor 99.83%
    Mauritianin is an orally active kaempferol glycoside. Mauritianin can be isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor. Mauritianin has hepatoprotective, neuroprotective, and renoprotective activities. Mauritianin increases vascular tone when used in combination with Alcesefoliside (HY-N5049).
    Mauritianin
  • HY-125331
    DRF-1042
    		Inhibitor 98.06%
    DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-agent resistance (MDR) phenotype.
    DRF-1042
  • HY-N2198
    Podocarpusflavone A
    		Inhibitor 99.62%
    Podocarpusflavone A is a DNA topoisomerase I inhibitor. Podocarpusflavone A has moderated anti-proliferative activity and induces cell apoptosis in MCF-7. Podocarpusflavone A is developing anti-tumor agents.
    Podocarpusflavone A
  • HY-164835
    VcMMAE-Deruxtecan
    		Inhibitor 98.10%
    VcMMAE-Deruxtecan is a Drug-Linker Conjugates for ADC, which is composed of a linker and a toxic molecule MMAE (HY-15162) (Microtubule inhibitor) and Exatecan (HY-13631) (DNA topoisomerase I inhibitor). VcMMAE-Deruxtecan can be used for ADC synthesis.
    VcMMAE-Deruxtecan
  • HY-160005
    LMP517
    		Inhibitor 99.58%
    LMP517 (NSC 781517) is a potent and non-camptothecin Topoisomerase I and II (TOP1 and TOP2) dual inhibitor. LMP517 can induce TOP1 and TOP2 cleavage complexes (TOP1ccs and TOP2ccs). LMP517 can induce cancer cells DNA damage and γH2AX production. LMP517 can be used for the research of cancer, such as small cell lung cancer.
    LMP517
  • HY-18350
    Indimitecan
    		Inhibitor 98.30%
    Indimitecan (LMP776) is a topoisomerase I (Top1) inhibitor with anticancer activities.
    Indimitecan
  • HY-160807
    DBM-GGFG-NH-O-CO-Exatecan
    		Inhibitor
    DBM-GGFG-NH-O-CO-Exatecan is an inhibitor for topoisomerase I. DBM-GGFG-NH-O-CO-Exatecan can be used as a drug-linker conjugate for synthesis of ADC molecule.
    DBM-GGFG-NH-O-CO-Exatecan
  • HY-164143
    T638
    		Inhibitor 98.61%
    T638 is a topoisomerase II (TOP2) inhibitor. T638 inhibits TOP2A activity with a IC50 of 0.7 uM. T638 strongly inhibits cancer cell growth.
    T638
  • HY-100777
    DACA
    		Inhibitor 98.0%
    DACA inhibits two essential nuclear enzymes in vitro, DNA topoisomerase I and DNA topoisomerase (topo) II. DACA stabilises topo I, topo II alpha, and topo II beta cleavable complexes in human leukaemia CCRF-CEM cells.
    DACA
  • HY-13670
    Lurtotecan
    		Inhibitor 98.01%
    Lurtotecan (GI147211; OSI-211), a semisynthetic Camptothecin analog, is a topoisomerase I inhibitor. Lurtotecan has anticancer effects.
    Lurtotecan
  • HY-171124
    Tilatamig samrotecan
    		Inhibitor
    Tilatamig samrotecan (AZD9592) is an antibody-drug conjugate (ADC) used to deliver topoisomerase I inhibitors (TOP1i), targeting the epidermal growth factor receptor (EGFR) and c-MET, with anti-tumor activity. Tilatamig samrotecan (AZD9592) can induce DNA double-strand breaks, increase the expression of pRAD50 and γH2AX, and inhibit the growth of non-small cell lung cancer.
    Tilatamig samrotecan
  • HY-122594
    BNS-22
    		Inhibitor 99.50%
    BNS-22 is a DNA topoisomerase II (TOP2) catalytic inhibitor with the IC50 values of 2.8 μM and 0.42 μM for human TOP2α and TOP2β, respectively. BNS-22 induces abnormal division and has anti-proliferative activity.
    BNS-22
  • HY-N10495
    Seconeolitsine
    		Inhibitor
    Seconeolitsine, an antibiotic, and is an inhibitor of targeting topoisomerase I (TopA). Seconeolitsine also is a new antimicrobial agent that can inhibit S. pneumoniae growth. Seconeolitsine can inhibit TopA relaxation activity with an IC50 value of 17 μM. Seconeolitsine can be used for the research of S. pneumoniae infections resistant to other antibiotics.
    Seconeolitsine
  • HY-153797
    Dox-btn2
    		Inhibitor
    Dox-btn2 is a biotin labeled Doxorubicin (HY-15142A), with a biotin label at the point of conjugation to doxorubicin at 3'-NH2. Dox-btn2 can be used for cell imaging. While Doxorubicin is mainly accumulated in the nucleus, while Dox-btn2 is mainly located in the cytoplasm.
    Dox-btn2
  • HY-160788
    DBCO-β-Glu-PEG12-Exatecan
    		Inhibitor
    DBCO-β-Glu-PEG12-Exatecan (Compound 107) is an inhibitor for topoisomerase I. DBCO-β-Glu-PEG12-Exatecan can be used as a Drug-Linker Conjugate for ADC molecule.
    DBCO-β-Glu-PEG12-Exatecan
  • HY-43565
    Exatecan intermediate 9
    		Inhibitor 99.80%
    Exatecan intermediate 9 is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM).
    Exatecan intermediate 9
  • HY-45157
    Exatecan Intermediate 7
    		Inhibitor 99.24%
    Exatecan Intermediate 7 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 7 can be used to synthesize Antibody-Drug Conjugates (ADCs).
    Exatecan Intermediate 7
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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