1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. Topoisomerase

Topoisomerase

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13566AS
    Belotecan-d7 hydrochloride
    Inhibitor 99.90%
    Belotecan-d7 (hydrochloride) is the deuterium labeled Belotecan hydrochloride. Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic camptothecin derivative.
    Belotecan-d<sub>7</sub> hydrochloride
  • 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-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-14812
    Karenitecin
    Inhibitor 98.02%
    Karenitecin (Cositecan) is a topoisomerase I inhibitor, with potent anti-cancer activity.
    Karenitecin
  • 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-153600
    GGFG-amide-glycol-amide-Exatecan
    Inhibitor 98.73%
    GGFG-amide-glycol-amide-Exatecan (Intermediate 2) is an Exatecan (HY-13631) derivative and can be used in the synthesis of antibody-drug conjugates (ADCs).
    GGFG-amide-glycol-amide-Exatecan
  • 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-17460A
    Garenoxacin Mesylate hydrate
    Inhibitor 99.78%
    Garenoxacin (BMS284756) Mesylate hydrate is an orally active quinolone antibiotic and has a broad spectrum of activity against a wide array of gram-positive and gram-negative bacteria, anaerobes, and fastidious organisms.
    Garenoxacin Mesylate hydrate
  • HY-N8248
    Eleutherin
    99.22%
    Eleutherin is a type of naphthoquinone derivative with the protective effect against the injury ofhuman umbilical vein endothelial cells (HUVECs), which can be isolated from the edible bulbs of Eleutherine americana (Hong-Cong).
    Eleutherin
  • 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-173639
    AZD0516
    Inhibitor
    AZD0516 is a first-in-class antibody-drug conjugate (ADC) targeting six-transmembrane epithelial antigen of the prostate-2 (STEAP2). The anti-STEAP2 monoclonal antibody (mAb) is conjugated via interchain cysteines to a maleimide-reactive, β-glucuronidase-cleavable linker (HY-173635) bearing the topoisomerase 1 inhibitor, Exatecan (HY-13631). AZD0516 can be used for the study of prostate cancer.
    AZD0516
  • 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-14821
    Namitecan
    Inhibitor 98.03%
    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-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-173634
    Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan
    Inhibitor
    Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan (LP1) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB (HY-173635) to make antibody agent conjugate (ADC), AZD0516 (HY-173639).
    Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan
  • 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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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