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-131540
    (±)-E-Homocamptothecin
    Inhibitor
    (±)-E-Homocamptothecin (BN 80245) is a topoisomerase I inhibitor. (±)-E-Homocamptothecin can be used for the research of cancer.
    (±)-E-Homocamptothecin
  • HY-177679
    N-(Amino-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan)
    N-(Amino-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-(Amino-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-(Amino-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan)
  • HY-182074
    DNA Gyrase-IN-18
    Inhibitor
    DNA Gyrase-IN-18 (Compound 6B) is a DNA Gyrase inhibitor and Antibacterial agent. DNA Gyrase-IN-18 significantly inhibits the supercoiling activity of DNA Gyrase. DNA Gyrase-IN-18 inhibits biofilm formation by *Staphylococcus aureus*. DNA Gyrase-IN-18 exhibits excellent antibacterial activity, with a MIC of 0.125 μg/mL against Staphylococcus aureus and a MIC of 0.5 μg/mL against Mycobacterium tuberculosis.
    DNA Gyrase-IN-18
  • HY-E70898C
    Topoisomerase IV, E. coli
    Topoisomerase IV, E. coli (EC 5.99.1.) is prepared by overexpressing the parC and parE subunits in E. coli. Topoisomerase IV is supplied as a heterotetramer complex in Dilution buffer.
    Topoisomerase IV, E. coli
  • HY-E70899B
    Topoisomerase IV, Pseudomonas aeruginosa
    Topoisomerase IV, Pseudomonas aeruginosa (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, Pseudomonas aeruginosa
  • HY-W040298
    Ciprofloxacin lactate
    Inhibitor
    Ciprofloxacin (Bay-09867) lactate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin lactate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin lactate has anti-proliferative activity and induces apoptosis. Ciprofloxacin lactate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
    Ciprofloxacin lactate
  • HY-160598
    Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol
    Inhibitor
    Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol (compound 45) is a camptothecin compound that can inhibit cell proliferation, with an IC50 of 2.92 ng/mL for MDA‑MB‑468 cells. Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol can be used for the research of cancer.
    Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol
  • HY-158390
    Anticancer agent 217
    Inhibitor
    Anticancer agent 217 (35B) is a Camptothecin compound, with IC50 values of 6.2 nM and 7.1 nM in MCF-7 cells and MDA-MB-231 cells, respectively.
    Anticancer agent 217
  • HY-158392
    Anticancer agent 219
    Inhibitor
    Anticancer agent 219 (P139) is a Camptothecin compound, with anticancer activity.
    Anticancer agent 219
  • HY-146138
    EGFR-IN-57
    Inhibitor
    EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis.
    EGFR-IN-57
  • HY-160597
    Exatecan-amide-bicyclo[1.1.1]pentan-1-ol
    Inhibitor
    Exatecan-amide-bicyclo[1.1.1]pentan-1-ol (Compound 79) is an exatecan (HY-13631) derivative that can be used as a payload in drug conjugates. Exatecan-amide-bicyclo[1.1.1]pentan-1-ol has significant inhibitory activity against a variety of tumor cell lines.
    Exatecan-amide-bicyclo[1.1.1]pentan-1-ol
  • HY-146020
    Topoisomerase IIα-IN-1
    Inhibitor
    Topoisomerase IIα-IN-1 (compound 2) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-1 exhibits high antiproliferative activity against human cancer cell lines.
    Topoisomerase IIα-IN-1
  • HY-N10115
    Huanglongmycin N
    Inhibitor
    Huanglongmycin N is a DNA topoisomerase I inhibitor (EC50 = 14 μM).
    Huanglongmycin N
  • HY-13631G
    Exatecan analog 13
    Inhibitor
    Exatecan analog 13 is a analog of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50 = 2.2 μM).
    Exatecan analog 13
  • HY-16562S2
    Irinotecan-13C6
    Inhibitor
    Irinotecan-13C6 ((+)-Irinotecan-13C6) is the 13C-labeled Irinotecan (HY-16562). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.
    Irinotecan-<sup>13</sup>C<sub>6</sub>
  • HY-N0716AR
    Berberine hemisulfate (Standard)
    Inhibitor
    Berberine (hemisulfate) (Standard) is the analytical standard of Berberine (hemisulfate). This product is intended for research and analytical applications. Berberine hemisulfate is the hemisulfate form of Berberine (HY-N0716). Berberine hemisulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian. Berberine hemisulfate exhibits anti-inflammatory, antibiobic, antitumor, cardiovascular protective and neuroprotective activity.
    Berberine hemisulfate (Standard)
  • HY-13631N
    (9R)-Exatecan
    Inhibitor
    (9R)-Exatecan (DX8951f) is the (1R,9S) stereoisomer of Exatecan (HY-13631). Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
    (9R)-Exatecan
  • HY-W031307
    Topoisomerase IIα-IN-8
    Inhibitor
    Topoisomerase IIα-IN-8 (compound 15) is a weak human DNA topoisomerase IIa (htIIa) inhibitor, with an IC50 of 462 ± 38.0 μM.
    Topoisomerase IIα-IN-8
  • HY-W353258R
    Moxifloxacin hydrochloride monohydrate (Standard)
    Inhibitor
    Moxifloxacin hydrochloride (BAY 12-8039) monohydrate (Standard) is the analytical standard of Moxifloxacin hydrochloride monohydrate. This product is intended for research and analytical applications. Moxifloxacin hydrochloride monohydrate is a blood-brain barrier-permeable, orally active topoisomerase II/IV inhibitor and a fluoroquinolone antibiotic. Moxifloxacin hydrochloride monohydrate disrupts bacterial DNA replication, transcription, repair and chromosome segregation processes. Moxifloxacin hydrochloride monohydrate exhibits activity against Gram-positive bacteria, Gram-negative bacteria, anaerobes, atypical pathogens, drug-resistant respiratory pathogens, Mycobacterium tuberculosis, mycoplasmas and Ureaplasma urealyticum.
    Moxifloxacin hydrochloride monohydrate (Standard)
  • HY-177585
    BCPT02
    Inhibitor
    BCPT02 (BLD1102) is a Topoisomerase-I inhibitor and ADC payload (ADC Payload). BCPT02 can form the ADC BCG041. BCPT02 is applicable to cancer-related research.
    BCPT02
Cat. No. Product Name / Synonyms Species Source
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