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-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-E70899D
    Topoisomerase IV, Acinetobacter baumannii
    Topoisomerase IV, Acinetobacter baumannii (EC 5.99.1.) is prepared by overexpressing the subunits in E. coli. Topoisomerase IV is supplied as a heterotetramer complex in Dilution buffer.
    Topoisomerase IV, Acinetobacter baumannii
  • HY-118823
    Amonafide L-malate
    		Inhibitor
    Amonafide L-malate is a topoisomerase II inhibitor and DNA intercalator that induces Apoptotic signaling by blocking the binding of Topo II to DNA.
    Amonafide L-malate
  • HY-E70899A
    Topoisomerase IV, Staphylococcus aureus
    Topoisomerase IV, Staphylococcus aureus (EC 5.99.1.) is prepared by overexpressing the subunits in E.coli.
    Topoisomerase IV, Staphylococcus aureus
  • 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-185397
    2-MSP(4-OMe)-5-HA-PEG8-VA-Exatecan
    		Inhibitor
    2-MSP(4-OMe)-5-HA-PEG8-VA-Exatecan is a Drug-linker conjugates for ADC consisting of the ADC Cytotoxin Exatecan (HY-13631) and a linker. 2-MSP(4-OMe)-5-HA-PEG8-VA-Exatecan can be used for synthesis of ADCs.
    2-MSP(4-OMe)-5-HA-PEG8-VA-Exatecan
  • HY-177682
    N-(NHS-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan)
    N-(NHS-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(NHS-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
    N-(NHS-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan)
  • HY-180509
    Topoisomerase I/IIα-IN-1
    		Inhibitor
    Topoisomerase I/IIα-IN-1 (Compound 20i) is a Topoisomerase I/IIα inhibitor. MDM2-IN-27 can effectively block the inhibitory effect of MDM2 on p53, thereby activating the p53 pathway. MDM2-IN-27 has relatively poor anti-proliferative activity against breast cancer, colon cancer, and cutaneous squamous cell carcinoma.
    Topoisomerase I/IIα-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-16560R
    Camptothecin (Standard)
    		Inhibitor
    Camptothecin (Standard) (Campathecin (Standard)) is the analytical standard of Camptothecin (HY-16560). This product is intended for research and analytical applications. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells.
    Camptothecin (Standard)
  • 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 (Compound 11) is a bioactive compound-linker conjugate for ADC. Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan can conjugate with antibodies to form ADC (C-11) with anti-tumor activity. Exatecan is a DNA Topoisomerase I inhibitor. Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan can be used in the research of squamous cell carcinoma, pancreatic adenocarcinoma and colorectal cancer.
    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
  • HY-17028A
    (Rac)-Besifloxacin hydrochloride
    		Inhibitor
    (Rac)-Besifloxacin Hydrochloride is a fourth generation fluoroquinolone antibiotic. (Rac)-Besifloxacin Hydrochloride is a DNA gyrase and topoisomerase IV inhibitor. (Rac)-Besifloxacin Hydrochloride has broad-spectrum antibacterial activity, it is effective against Gram-negative and Gram-positive aerobic and anaerobic strains and reduces the incidence of drug resistance. (Rac)-Besifloxacin Hydrochloride has anti-inflammatory activity. Besifloxacin Hydrochloride can be used in bacterial conjunctivitis research.
    (Rac)-Besifloxacin hydrochloride
  • HY-145851
    Top/HDAC-IN-1
    		Inhibitor
    Top/HDAC-IN-1 (Compound 29b) is a topoisomerase/HDAC dual inhibitor with IC50s of 18, 230, 790, 87, and 5250 nM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, respectively. Top/HDAC-IN-1 exhibits potent antitumor activities against the HCT116 cell line with the IC50 of 180 nM. Top/HDAC-IN-1 efficiently induces apoptosis with G2 cell cycle arrest in HCT116 cells.
    Top/HDAC-IN-1
  • HY-13630R
    Etoposide phosphate (Standard)
    		Inhibitor
    Etoposide phosphate (Standard) is the analytical standard of Etoposide phosphate. This product is intended for research and analytical applications. Etoposide phosphate (BMY-40481) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate is the phosphate ester proagent of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate induces cell cycle arrest, apoptosis, and autophagy.
    Etoposide phosphate (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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