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-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 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
  • 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)
  • HY-162101
    Topoisomerase inhibitor 3
    		Inhibitor
    Topoisomerase inhibitor 3 (compound 9) is a potent Topoisomerase inhibitor. Topoisomerase inhibitor 3 shows antiproliferative and anti-tumor activity.
    Topoisomerase inhibitor 3
  • HY-161980
    Topoisomerases/ribosomes-IN-1
    		Inhibitor
    Topoisomerases/ribosomes-IN-1 (compound 30f) is an inhibitor of ribosomes and topoisomerases, and has inhibitory effects on constitutively macrolide-resistant bacteria. Topoisomerases/ribosomes-IN-1 can inhibit bacterial protein synthesis (IC50: 0.647 μM) and DNA replication (IC50: 0.218 μM).
    Topoisomerases/ribosomes-IN-1
  • HY-147182
    3,6-Diamino-9(10H)-acridone
    		Inhibitor
    3,6-Diamino-9(10H)-acridone is a topoisomerase inhibitor.
    3,6-Diamino-9(10H)-acridone
  • HY-162091
    Topoisomerase I inhibitor 13
    		Inhibitor
    Topoisomerase I inhibitor 13 (Compound G11) is a Topo I inhibitor that inhibits cancer cell proliferation. Topoisomerase I inhibitor 13 significantly inhibits tumor growth in vivo.
    Topoisomerase I inhibitor 13
  • HY-157795
    Exatecan analogue 1
    		Inhibitor
    Exatecan analogue 1 (Icp-3) is a Exatecan (HY-13631) analogue. Exatecan analogue 1 can be used in the synthesis of antibody-drug conjugates (ADCs)
    Exatecan analogue 1
  • HY-156686
    NH2-methylpropanamide-Exatecan TFA
    		Inhibitor 99.80%
    NH2-methylpropanamide-Exatecan TFA is a methylpropanamide-modified Exatecan (HY-13631), which is the common ADC Cytotoxin used in the synthesis of ADC. Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
    NH2-methylpropanamide-Exatecan TFA
  • HY-16742R
    Gepotidacin (Standard)
    		Inhibitor
    Gepotidacin (Standard) is the analytical standard of Gepotidacin. This product is intended for research and analytical applications. Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor.
    Gepotidacin (Standard)
  • HY-172395
    TopoII/tubulin-IN-1
    		Inhibitor
    TopoII/tubulin-IN-1 (Compound 1B8) is a TopoII/tubulin inhibitor. TopoII/tubulin-IN-1 can inhibit the proliferation and the level of ROS of tumor cells, induce apoptosis and cell cycle arrest of tumor cells, but has no significant cytotoxicity to normal cells. TopoII/tubulin-IN-1 has antitumor activity.
    TopoII/tubulin-IN-1
  • HY-170912
    Topo I/II-IN-2
    		Inhibitor
    Topo I/II-IN-2 (Compound 3g) is an inhibitor of Topo I and Topo II. Topo I/II-IN-2 inhibits NCI-H446 cells and NCI-H1048 cells with IC50s of 1.30 μM and 1.42 μM, respectively. Topo I/II-IN-2 induces mitochondrial Apoptosis, mitochondrial dysfunction and activity generation. Topo I/II-IN-2 inhibits the PI3K/Akt/mTOR pathway. Topo I/II-IN-2 prevents SCLC (small cell lung cancer) cell proliferation, invasion, and migration in vitro. .
    Topo I/II-IN-2
  • HY-145867
    EGFR-IN-45
    		Inhibitor
    EGFR-IN-45 is a potent epidermal growth factor receptor (EGFR) pan inhibitor, with IC50s of 0.4 µM and 1.6 µM for EGFR and CDK2, respectively. EGFR-IN-45 also inhibit Topo I and Topo II. EGFR-IN-45 arrests cancer cells in the pre-G1 phase and induces apoptosis.
    EGFR-IN-45
  • HY-RS14892
    Top1 Rat Pre-designed siRNA Set A
    		Inhibitor

    Top1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Top1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Top1 Rat Pre-designed siRNA Set A
    Top1 Rat Pre-designed siRNA Set A
  • HY-149925
    DNA Gyrase-IN-6
    		Inhibitor
    Antibacterial agent 138 is a benzothiazole inhibitor of bacterial DNA gyrase and topoisomerase IV. Antibacterial agent 138 exhibits favorable solubility and plasma protein binding. Antibacterial agent 138 has antibacterial activity against Gram-positive and Gram-negative strains. Antibacterial agent 138 is a dual GyrB and ParE inhibitor.
    DNA Gyrase-IN-6
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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