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-149002
    Topoisomerase I/II inhibitor 4
    Inhibitor
    Topoisomerase I/II inhibitor 4 (compound F16) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 4 inhibits cell proliferation, invasion and migration and induces apoptosis. Topoisomerase I/II inhibitor 4 can be used for liver cancer research.
    Topoisomerase I/II inhibitor 4
  • HY-14871
    Tenifatecan
    Inhibitor
    Tenifatecan (SN2310) is an injectable emulsion composed of vitamin E, a succinate derivative, as well as 7-ethyl-10-hydroxycamptothecin (SN-38, the active metabolite of irinotecan). Tenifatecan (SN2310) possesses anticancer activity.
    Tenifatecan
  • HY-175741
    IID432
    Inhibitor
    IID432 is a Trypanosoma cruzi Topoisomerase II inhibitor with an EC50 of 8  nM for Trypanosoma cruzi. IID432, a single dose of 25 mg/kg, can achieve relapse-free parasite clearance in mouse models of chronic Chagas disease. IID432 can be used for Chagas disease research.
    IID432
  • HY-148380
    Mal-PEG8-Phe-Lys-PAB-Exatecan
    Inhibitor
    Mal-PEG8-Phe-Lys-PAB-Exatecan (compound 15) is a agent-linker conjugate for ADC, composed of degradable linker Mal-PEG8-Phe-Lys-PAB and toxin molecule Exatecan (HY-13631) composition.
    Mal-PEG8-Phe-Lys-PAB-Exatecan
  • HY-168848
    KT32
    Inhibitor
    KT32 (10c) is a potent dual inhibitor of HDAC and Topo II α. KT32 induces cell death through apoptosis.
    KT32
  • HY-17460AR
    Garenoxacin Mesylate hydrate (Standard)
    Inhibitor
    ACHE-IN-38 (hydrochloride) (Standard) is the analytical standard of ACHE-IN-38 (hydrochloride). This product is intended for research and analytical applications. ACHE-IN-38 hydrochloride (Compound 13b) inhibits the metabolic breakdown of the neurotransmitter acetylcholine (ACh) by the enzyme acetylcholinesterase (AChE) and hence alleviates memory deficits in patients with Alzheimer’s Disease by potentiating cholinergic transmission.
    Garenoxacin Mesylate hydrate (Standard)
  • HY-178315
    Exatecan analog 38
    Inhibitor
    Exatecan analog 38 is a camptothecin derivative with potent topoisomerase I inhibitory activity. Exatecan analog 38 can be connected to monoclonal antibodies via linkers to form antibody-drug conjugate (ADC) molecules. Exatecan analog 38 can be used for cancer research.
    Exatecan analog 38
  • HY-B0330BR
    Levofloxacin hydrochloride (Standard)
    Inhibitor
    Levofloxacin (hydrochloride) (Standard) is the analytical standard of Levofloxacin hydrochloride (HY-B0330B). This product is intended for research and analytical applications. Levofloxacin hydrochloride is an orally active antibiotic. Levofloxacin inhibits DNA gyrase and topoisomerase IV activity, inducing Apoptosis. Levofloxacin hydrochloride has antibacterial activity against both Gram-positive and Gram-negative bacteria. Levofloxacin hydrochloride exhibits anticancer activity against lung cancer. Levofloxacin hydrochloride has anti-acnegenic, anxiogenic, and analgesic effects. Levofloxacin hydrochloride shortens sleep duration in mice. Levofloxacin hydrochloride can be used in the research of infectious diseases (such as tuberculosis, chronic periodontitis, bacterial infections associated with stable COPD, and BK viremia) and lung cancer.
    Levofloxacin hydrochloride (Standard)
  • HY-171138
    Mal-VC-PAB-DMEA-PNU-159682
    Inhibitor
    Mal-VC-PAB-DMEA-PNU-159682 is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-topoisomerase II agent, PNU-159682, linked via the lysosomally cleavable dipeptide, Mc-VC-PAB. Mal-VC-PAB-DMEA-PNU-159682 can be used in the synthesis of Anti-CD22-NMS249 (HY-164761).
    Mal-VC-PAB-DMEA-PNU-159682
  • HY-105387
    Heliquinomycin
    Inhibitor
    Heliquinomycin is an inhibitor of DNA helicase (Ki: 6.8 μM) and inhibits DNA and RNA synthesis. Heliquinomycin is effective against Gram-positive bacteria strains. Heliquinomycin inhibits cancer cell growth.
    Heliquinomycin
  • HY-157402
    Topoisomerase II/EGFR-IN-1
    Topoisomerase II/EGFR-IN-1 is topoisomerase II/EGFR dual inhibitor. Topoisomerase II/EGFR-IN-1 has superior cytotoxic activity to MCF-7, A549 and HCT-116 cell lines, displays strong apoptotic activity and can be used for the research of cancer.
    Topoisomerase II/EGFR-IN-1
  • HY-106031A
    F-14512 hydrochloride
    Inhibitor
    F-14512 hydrochloride is an anticancer agent that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 hydrochloride enhances the affinity of polyamines for DNA, thereby inhibiting topoisomerase II and achieving selective cellular uptake. F-14512 hydrochloride exhibits significant cytotoxicity against cells with high PTS activity and induces DNA damage. F-14512 hydrochloride demonstrates potent antitumor activity in the MX1 breast tumor xenograft model. F-14512 hydrochloride could be used to study breast cancer.
    F-14512 hydrochloride
  • HY-175216
    Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6
    Inhibitor
    Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6 is a drug-linker conjugate for ADC. Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6 consists of a topoisomerase 1 inhibitor (Topi MF-6) (HY-175203) and a cleavable linker (Maleimide-Ph(3,5-F)-PEG4-Val-Ala) (HY-175218). Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6 can be used for synthesis of ADCs.
    Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6
  • HY-148696A
    Gly-Cyclopropane-Exatecan
    Inhibitor
    Gly-Cyclopropane-Exatecan involves in the synthesis of anti-B7-H4 ADC, containing Exatecan (HY-13631), a DNA Topoisomerase I inhibitor. Gly-Cyclopropane-Exatecan participated in the formation of the ADC hu2F7-Exatecan (compound 34), which showed antitumor activity in vivo and in vitro.
    Gly-Cyclopropane-Exatecan
  • HY-122014
    S 39625
    Inhibitor
    39625 is a camptothecin ketone analogue, a stable, potent and selective topoisomerase I inhibitor, active against purified topoisomerase I and cytotoxic to cancer cells.
    S 39625
  • HY-174151
    XSJ110
    Inhibitor
    XSJ110 is a potent irreversible topoisomerase I (Topo I) inhibitor with an IC50 value of 0.133 μM. XSJ110 blocks DNA topoisomerization, induces DNA double-strand breaks, and triggers cell cycle arrest at G0/G1 phase, inducing tumor cell apoptosis. XSJ110 is promising for research of ampullary carcinoma (AC).
    XSJ110
  • HY-120173
    Ro 47-3359
    Ro 47-3359 is a pyrimido[1,6-a]benzimidazole compound with the activity of enhancing eukaryotic topoisomerase II-mediated DNA cleavage and being toxic to Kc cells.
    Ro 47-3359
  • HY-155645
    Topoisomerase II inhibitor 15
    Inhibitor
    Topoisomerase II inhibitor 15 (compound 2g) is a Topoisomerase II inhibitor. Topoisomerase II inhibitor 15 potently is an apoptotic inducer with greater selectivity against head and neck tumors.
    Topoisomerase II inhibitor 15
  • HY-145397A
    (R)-(4-NH2)-Exatecan
    Inhibitor
    (R)-(4-NH2)-Exatecan is the R enantiomer of (4-NH2)-Exatecan (Compound A). (R)-(4-NH2)-Exatecan, a topoisomerase inhibitor, is a derivative of Exatecan. (R)-(4-NH2)-Exatecan can be used in the synthesis of antibody-drug conjugates (ADCs).
    (R)-(4-NH2)-Exatecan
  • HY-156723
    9-Chloromethyl-10-hydroxy-11-F-Camptothecin
    9-Chloromethyl-10-hydroxy-11-F-Camptothecin is a novel camptothecin derivatives. 9-Chloromethyl-10-hydroxy-11-F-Camptothecin is a DNA topoisomerase I (Topo I) inhibitor, can be used in anticancer research.
    9-Chloromethyl-10-hydroxy-11-F-Camptothecin
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