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-150044
    Type II topoisomerase inhibitor 1
    		Inhibitor
    Type II topoisomerase inhibitor 1 is a potent and selective E. coli DNA gyrase inhibitor (IC50: 1.7 nM), and forms hydrogen bonds with Asp73 residue. Type II topoisomerase inhibitor 1 inhibits topoisomerase IV activity (IC50: 0.98 μM). Type II topoisomerase inhibitor 1 can be used in the research of antibacterial area.
    Type II topoisomerase inhibitor 1
  • HY-105178A
    Galarubicin hydrochloride
    		Inhibitor
    Galarubicin hydrochloride (DA 125) is a novel Anthracycline derivative. Galarubicin hydrochloride shows high-affinity DNA binding and topoisomerase II inhibitory activities. Galarubicin hydrochloride induces Apoptosis. Galarubicin hydrochloride exerts cytotoxicity via JNK pathway. Galarubicin hydrochloride can be used in the research of hepatocellular carcinoma.
    Galarubicin hydrochloride
  • HY-143280
    Topoisomerase II inhibitor 4
    		Inhibitor
    Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect.
    Topoisomerase II inhibitor 4
  • HY-P992356
    GENA-104A16
    		Inhibitor
    GENA-104A16 is a humanized monoclonal antibody targeting CNTN4, with multiple functions including immunostimulation, cytotoxicity and immunoregulation. By binding to CNTN4, GENA-104A16 blocks its interaction with APP, thereby restoring T cell function, inducing tumor cell death and regulating tumor-infiltrating immune cell populations. GENA-104A16 also exerts topoisomerase I inhibitory activity via the payload Exatecan (HY-13631). GENA-104A16 can be used in research related to colon cancer liver metastasis and other CNTN4-expressing solid tumors.
    GENA-104A16
  • HY-182926
    Topoisomerase I/II-IN-9
    		Inhibitor
    Topoisomerase I/II-IN-9 is a topoisomerase I/II inhibitor (IC50<10 μM) and a DNA damage inducer. Topoisomerase I/II-IN-9 blocks the interaction between the enzyme and DNA by binding to the DNA-binding pocket of the enzyme. Topoisomerase I/II-IN-9 activates the cGAS-STING pathway and promotes the accumulation of cytoplasmic double-stranded DNA. This further drives the production of type I interferons, CCL5, CXCL10 and interferon-stimulated genes, and induces anti-tumor immune responses in vivo. Topoisomerase I/II-IN-9 can be applied to the research of related diseases such as triple-negative breast cancer, colorectal cancer and gastric cancer.
    Topoisomerase I/II-IN-9
  • HY-13768D
    Topotecan acetate
    		Inhibitor
    Topotecan acetate is a topoisomerase inhibitor.
    Topotecan acetate
  • HY-152473
    Topoisomerase IIα-IN-6
    		Inhibitor
    Topoisomerase IIα-IN-6 (Compound 47d) is an inhibitor of DNA topoisomerase IIα/β. Topoisomerase IIα-IN-6 inhibits human topoisomerase IIα and human topoisomerase IIβ with IC50 values of 0.67 µM and 0.55 µM, respectively. Topoisomerase IIα-IN-6 has stable metabolism.
    Topoisomerase IIα-IN-6
  • HY-144774
    Topoisomerase I inhibitor 5
    		Inhibitor
    Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin.
    Topoisomerase I inhibitor 5
  • HY-RS14890
    TOP1 Human Pre-designed siRNA Set A
    		Inhibitor

    TOP1 Human Pre-designed siRNA Set A contains three designed siRNAs for TOP1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    TOP1 Human Pre-designed siRNA Set A
  • HY-146021
    Topoisomerase IIα-IN-2
    		Inhibitor
    Topoisomerase IIα-IN-2 (compound 5) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-2 exhibits high antiproliferative activity against human cancer cell lines. Topoisomerase IIα-IN-2 significantly induces DNA damage and arrests cancer cells at G2/M phase.
    Topoisomerase IIα-IN-2
  • HY-151453
    Topoisomerase IIα-IN-4
    		Inhibitor
    Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC50 value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer.
    Topoisomerase IIα-IN-4
  • HY-160756
    Val-Cit-Exatecan
    		Inhibitor
    Val-Cit-Exatecan is a peptide-linked anti-tumor payload that can be used for the synthesis of antibody-drug conjugates (ADC). Val-Cit-Exatecan consists of DNA TopI inhibitor Exatecan (HY-13631) and a cathepsin-cleavable ADC linker (valine-citrulline). Val-Cit-Exatecan can be used in the research of colorectal cancer, gastric cancer, breast cancer, non-small cell lung cancer, ovarian cancer, head and neck cancer, pancreatic cancer, cervical cancer, and melanoma.
    Val-Cit-Exatecan
  • HY-174404
    Topoisomerase II inhibitor 23
    		Inhibitor
    Topoisomerase II inhibitor 23 is a potent topoisomerase II inhibitor (IC50 = 0.94 μM). Topoisomerase II inhibitor 23 shows high selectivity and exceptional cytotoxic activity in MCF-7, HepG2, and HCT116 cells. Topoisomerase II inhibitor 23 induces cell cycle arrest at the G1 phase, leading to inhibition of cell proliferation. Topoisomerase II inhibitor 2 induces apoptosis by up-regulating the pro-apoptotic Bax level and down-regulating the anti-apoptotic Bcl-2 level.
    Topoisomerase II inhibitor 23
  • HY-N0716BR
    Berberine sulfate (Standard)
    		Inhibitor
    Berberine (sulfate) (Standard) is the analytical standard of Berberine (sulfate). This product is intended for research and analytical applications. Berberine sulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine sulfate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine sulfate has antineoplastic properties. The sulfate form improves bioavailability[1][2].
    Berberine sulfate (Standard)
  • HY-153685
    NISC-6
    		Inhibitor
    NISC-6 is a novel dual Topo-IIα/Akt inhibitor. NISC-6 has inhibitory activity against various cells, such as UACC903 (IC50 = 2.5 µM) and CHL-1 (IC50 = 0.8 µM) cells. NISC-6 dose dependently induces early and late apoptosis. NISC-6 can be used for research on melanoma.
    NISC-6
  • HY-178738
    GC-072
    		Inhibitor
    GC-072 is an orally active, 4-oxoquinolizine antibiotic that selectively inhibits bacterial DNA gyrase and Topo IV enzymes. GC-072 does not inhibit human topoisomerases I and II. GC-072 demonstrates strong antimicrobial activity against various bacterial strains, including Gram-positive, Gram-negative, and resistant bacteria. GC-072 also exhibits bactericidal activity against Burkholderia pseudomallei both extracellularly and intracellularly, leading to dose-dependent survival in mice exposed to lethal inhalational models of B. pseudomallei infection. GC-072 can be used for the research of melioidosis.
    GC-072
  • HY-162587
    Fagopyrine
    		Inhibitor
    Fagopyrine is a DNA topoisomerase I (Topo I) inhibitor. Fagopyrine is a photosensitizer that can be used in the study of tumors.
    Fagopyrine
  • HY-180823
    Topoisomerase II/EGFR-IN-2
    		Inhibitor
    Topoisomerase II/EGFR-IN-2 (Compound 3) is an inhibitor of Topoisomerase IIα (IC50 = 0.122 μM) and EGFR-TKWT (IC50 = 16.8 μM). Topoisomerase II/EGFR-IN-2 inhibits the proliferation of HeLa and HepG2 cells, inducing cell cycle arrest and apoptosis. Topoisomerase II/EGFR-IN-2 upregulates caspase-3 and Bax, and downregulates Bcl-2. Topoisomerase II/EGFR-IN-2 can be used to study liver cancer and cervical cancer.
    Topoisomerase II/EGFR-IN-2
  • HY-147698
    ZLHQ-5f
    		Inhibitor
    ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC50 of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile.
    ZLHQ-5f
  • HY-181694
    SeSA-HCPT
    		Inhibitor
    SeSA-HCPT is an orally active dual-target inhibitor integrating Topo I and HDAC inhibition. SeSA-HCPT induces potent DNA damage, apoptosis, S-phase arrest in prostate cancer cells. SeSA-HCPT inhibits cancer cells proliferation and migration. SeSA-HCPT impairs homologous recombination by suppressing KIF4A-RAD51 signaling. SeSA-HCPT markedly inhibits CRPC tumor growth with minimal systemic toxicity.
    SeSA-HCPT
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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