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-145291
    CPT-Se4
    		Inhibitor
    CPT-Se4, a selenoproagent of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT-Se4 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se4 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC50= 2.54-6.4 μM).
    CPT-Se4
  • HY-101959
    Tyrphostin AG213
    		Inhibitor
    Tyrphostin AG213 (AG213) is an inhibitor of epidermal growth factor receptor (EGFR) protein tyrosine kinase (IC50=0.85 μM). Tyrphostin AG213 inhibits tyrosine kinase activity IC50=2.4 μM) and topoisomerase II (IC100=50 μM). Tyrphostin AG213 can induce nonapoptotic cell programmed death in tumor cells.
    Tyrphostin AG213
  • HY-118036
    ACT-387042
    		Inhibitor
    ACT-387042 is a bacterial topoisomerase inhibitor with broad-spectrum activity against Gram-positive and Gram-negative bacteria, including methicillin-resistant Staphylococcus aureus and penicillin- and fluoroquinolone-resistant Streptococcus pneumoniae .
    ACT-387042
  • HY-17577R
    Berberine chloride hydrate (Standard)
    		Inhibitor
    Berberine (chloride hydrate) (Standard) is the analytical standard of Berberine (chloride hydrate). This product is intended for research and analytical applications. Berberine chloride hydrate (Natural Yellow 18 chloride hydrate) is an alkaloid that acts as an antibiotic. Berberine chloride hydrate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties[1].
    Berberine chloride hydrate (Standard)
  • HY-160806
    (5-Cl)-Exatecan
    		Inhibitor
    (5-Cl)-Exatecan (compound 1-5) is a potent DNA topoisomerase inhibitor used in cancer research. (5-Cl)-Exatecan is an ADC Cytotoxin.
    (5-Cl)-Exatecan
  • HY-161082
    Topoisomerase I inhibitor 12
    		Inhibitor
    Topoisomerase I inhibitor 12 (compound 12), a Camptothecin (HY-16560)-based derivative, is a potent Topoisomerase I inhibitor. Topoisomerase I inhibitor 12 shows anticancer activity.
    Topoisomerase I inhibitor 12
  • HY-173001
    AuL1
    		Inhibitor
    AuL1 is an inhibitor of topoisomerase IIα (Top II) with DNA-intercalating properties. AuL1 is cytotoxic to tumor cells and can be used in the research of anticancer agents.
    AuL1
  • HY-168849
    Topoisomerase inhibitor 5
    		Inhibitor
    Topoisomerase inhibitor 5 (compound 158) is a Bacterial Topoisomerase Inhibitor inhibitor with the lowest inhibitory concentration of 0.125 μg/mL. Topoisomerase inhibitor has antituberculous activity.
    Topoisomerase inhibitor 5
  • HY-18350A
    Indimitecan hydrochloride
    		Inhibitor
    Indimitecan hydrochloride is a topoisomerase I (Top1) inhibitor with anticancer activities.
    Indimitecan hydrochloride
  • HY-158387
    Anticancer agent 214
    		Inhibitor
    Anticancer agent 214 (2) is a Camptothecin compound, with IC50 values of 2.6 nM and 15.7 nM in MCF-7 cells and MDA-MB-231 cells, respectively.
    Anticancer agent 214
  • HY-163118
    Topoisomerase II inhibitor 17
    		Inhibitor
    Topoisomerase II inhibitor 17 (compound 4c) is an inhibitor of thiazolopyrimidine topoisomerase (Topoisomerase) Top II (IC50: 0.23 μM). Topoisomerase II inhibitor 17 can significantly cause cell cycle disruption and apoptosis.
    Topoisomerase II inhibitor 17
  • HY-170580
    Topo I/II-IN-1
    		Inhibitor
    Topo I/II-IN-1 (compound 7t) is a potent Topo I and Topo II dual inhibitor. Topo I/II-IN-1 exhibits significant cytotoxicity against MCF-7 breast cancer cell line with an IC50 of 7.45 μM.
    Topo I/II-IN-1
  • HY-146437
    Topoisomerase I inhibitor 6
    		Inhibitor
    Topoisomerase I inhibitor 6 (Compound 3) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 6 is able to trap DNA-Top1 cleavage complex and found to be less cytotoxic in non-cancerous cell line. Topoisomerase I inhibitor 6 has the potential for the research of cancer diseases.
    Topoisomerase I inhibitor 6
  • HY-168150
    Topoisomerase I/II inhibitor 5
    		Inhibitor
    Topoisomerase I/II inhibitor 5 (compund 1) simultaneously inhibits activities of TopoI and II by binding to and stabilizing the G4 structure.
    Topoisomerase I/II inhibitor 5
  • HY-154797
    N,N-Dimethyldoxorubicin
    		Control
    N,N-Dimethyldoxorubicin is a Doxorubicin (HY-15142A) analogue. N,N-Dimethyldoxorubicin shows cytotoxicity against a panel of tumor cell lines (IC50s < 0.3 μM).
    N,N-Dimethyldoxorubicin
  • HY-150571
    Anticancer agent 76
    		Inhibitor
    Anticancer agent 76 (Compound CT2-3) is an anticancer agent. Anticancer agent 76 significantly inhibits the proliferation of human NSCLC cells, induces cell cycle arrest, causes ROS generation and induces cell apoptosis.
    Anticancer agent 76
  • HY-156402
    AuM1Gly
    		Inhibitor
    AuM1Gly is a topoisomerase I inhibitor. AuM1Gly affects the growth of MDA-MB-231 breast cancer cells, with IC50?values in the low nanomolar range.
    AuM1Gly
  • HY-143402
    Topoisomerase I/II inhibitor 2
    		Inhibitor
    Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer.
    Topoisomerase I/II inhibitor 2
  • HY-153067
    Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan
    		Inhibitor
    Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan is a coupling compound that can be used for the synthesis of ADC. Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan synthesized ADC shows good antitumor activity in vitro and in vivo.
    Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan
  • HY-156642
    (1-OH)-Exatecan
    		Inhibitor
    (1-OH)-Exatecan is a quinoline ring compound. (1-OH)-Exatecan has substantial antiproliferative effects. (1-OH)-Exatecan can be used for cancer diseases research.
    (1-OH)-Exatecan
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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