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-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-14821
    Namitecan
    Inhibitor 99.25%
    Namitecan is a potent topoisomerase I inhibitor, with antitumor property.
    Namitecan
  • HY-400770
    MC-GGFG-AM-(10Me-11F-Camptothecin) intermediate-1
    Inhibitor
    MC-GGFG-AM-(10Me-11F-Camptothecin) intermediate-1 (compound 19-2) is an intermediate for the synthesis of MC-GGFG-AM-(10Me-11F-Camptothecin) (HY-153360). Modifying groups can be added group. MC-GGFG-AM-(10Me-11F-Camptothecin) is a drug-linker conjugate used in the synthesis of ADCs.
    MC-GGFG-AM-(10Me-11F-Camptothecin) intermediate-1
  • 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-160005
    LMP517
    Inhibitor 99.58%
    LMP517 (NSC 781517) a indenoisoquinoline, is a potent a dual TOP1 and TOP2 inhibitor. LMP517 shows better antitumor activity than its parent compound LMP744 (HY-U00248) against H82 (Small Cell Lung Cancer) xenografts. LMP517 induces TOP1 cleavage complexes (TOP1ccs) and TOP2ccs.
    LMP517
  • HY-18350
    Indimitecan
    Inhibitor 98.30%
    Indimitecan (LMP776) is a topoisomerase I (Top1) inhibitor with anticancer activities.
    Indimitecan
  • 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-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-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-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-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-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
  • HY-N2306A
    Aclacinomycin A hydrochloride
    Inhibitor
    Aclacinomycin A (Aclarubicin) hydrochloride is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A hydrochloride is an inhibitor of topoisomerase I and II. Aclacinomycin A hydrochloride inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A hydrochloride might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis.
    Aclacinomycin A hydrochloride
  • HY-147307
    MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan
    Inhibitor 99.55%
    MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan is a agent-linker conjugate for ADC, contains the ADC linker (MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic acid) and a DNA topoisomerase I inhibitor Exatecan (HY-13631). MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan synthesized ADC can be used in study of cancer.
    MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan
  • HY-148058
    Topoisomerase I inhibitor 8
    Inhibitor 99.87%
    Topoisomerase I inhibitor 8 is a potent topoisomerase I inhibitor. Topoisomerase I inhibitor 8 is a hexacyclic analogue of camptothecin, and displays cytotoxic effect against tumor cells.
    Topoisomerase I inhibitor 8
  • HY-132164
    Gly-7-MAD-MDCPT
    Inhibitor
    Gly-7-MAD-MDCPT (compound 4b) is an anticancer agent. Gly-7-MAD-MDCPT is a Camptothecin (HY-16560) compound, it shows cytotoxicity to various cancer cells with IC50 values of 10-1000 nM.
    Gly-7-MAD-MDCPT
  • HY-160774
    Val-Cit-PABC-DOX
    Inhibitor
    Val-Cit-PABC-DOX (compound 10109), an epsilon-poly-L-lysine-based drug conjugate, is an agent-linker conjugate for ADC by using a DNA topoisomerase I and topoisomerase II inhibitor, Doxorubicin (HY-15142), linked via the linker, Val-Cit-PABC.
    Val-Cit-PABC-DOX
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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