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-115990
    Topoisomerase IV inhibitor 1
    		Inhibitor
    Topoisomerase IV inhibitor 2 (compound 7d) is a potent DNA topoisomerase IV (TOPO IV) inhibitor with IC50s of 0.23 μM and 0.43 μM for TOPO IV and DNA gyrase, respectively. Topoisomerase IV inhibitor 2 has anti-bacterial activity, with MICs of 0.972 μM and 0.608 μM in Staphylococcus aureus Newman and Escherichia coli ATCC8739, respectively.
    Topoisomerase IV inhibitor 1
  • HY-N8248A
    (-)-Eleutherin
    (-)-Eleutherin is a pyranonaphthoquinone derivative that exhibits cytotoxic activity by inhibiting DNA topoisomerase II. (-)-Eleutherin has been shown to have promising potential as a medicinal compound due to its association with naphthoquinones. (-)-Eleutherin demonstrates significant DNA fragmentation rates, indicating its strong cytotoxic effects on cells. Additionally, (-)-Eleutherin possesses higher antioxidant potential compared to control samples, contributing to its therapeutic efficacy.
    (-)-Eleutherin
  • HY-153401
    Topoisomerase II inhibitor 13
    		Inhibitor 99.26%
    Topoisomerase II inhibitor 13 is a topoisomerase II (Topo II) inhibitor. Topoisomerase II inhibitor 13 shows antiproliferative activity against several cancer cells. Topoisomerase II inhibitor 13 induces cancer cells apoptosis.
    Topoisomerase II inhibitor 13
  • HY-158329
    Alloc-DOX
    		Inhibitor
    Alloc-DOX (N-Alloc doxorubicin) is a Doxorubicin (HY-15142A) prodrug. The combination of a catalyst (such as nano-palladium) and alloc-DOX leads to a decrease in cell viability and tumour growth.
    Alloc-DOX
  • HY-W046353R
    2-Methoxycinnamaldehyde (Standard)
    		Inhibitor
    2-Methoxycinnamaldehyde (Standard) is the analytical standard of 2-Methoxycinnamaldehyde. This product is intended for research and analytical applications. 2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound that can be isolated from Cinnamomum cassia. 2-Methoxycinnamaldehyde inhibits topoisomerase-I/II and NF-κB signaling pathway, causes mitochondrial dysfunction, induces lysosomal vesiculation, thereby leading to DNA damage and cell apoptosis. 2-Methoxycinnamaldehyde exhibits antitumor effects.
    2-Methoxycinnamaldehyde (Standard)
  • 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-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-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-171124
    Tilatamig samrotecan
    		Inhibitor
    Tilatamig samrotecan (AZD9592) is an antibody-drug conjugate (ADC) used to deliver topoisomerase I inhibitors (TOP1i), targeting the epidermal growth factor receptor (EGFR) and c-MET, with anti-tumor activity. Tilatamig samrotecan (AZD9592) can induce DNA double-strand breaks, increase the expression of pRAD50 and γH2AX, and inhibit the growth of non-small cell lung cancer.
    Tilatamig samrotecan
  • HY-164836
    Deruxtecan-Eribulin
    		Inhibitor
    Deruxtecan-Eribulin is a Drug-Linker Conjugates for ADC, which is composed of a linker and a toxic molecule Exatecan (HY-13631) (DNA topoisomerase I inhibitor) and Eribulin (HY-13442) (Microtubule inhibitor). Deruxtecan-Eribulin can be used for ADC synthesis.
    Deruxtecan-Eribulin
  • HY-109855
    CP-67015
    		Inhibitor
    CP-67015, a quinolone antibiotic, is a potent topoisomerase II inhibitor. CP-67015 is a positive direct-acting mutagen in mammalian cells with both gene and chromosomal level effects.
    CP-67015
  • HY-156670
    Camptothecin analog-1
    Camptothecin analog-1 (Comp 166) is a camptothecin analog.
    Camptothecin analog-1
  • HY-161628
    Tapcin
    		Inhibitor
    Tapcin is a dual inhibitor for topoisomerase I and topoisomerase II, with IC50 of 203 and 71 nM. Tapcin inhibits proliferations of cancer cells A-375, HeLa, Huh7.5, U2-OS, A549, Caco-2 and HT29, with IC50s of 441, 1.04, 40.5, 0.002, 0.006, 0.287 and 0.842 nM, respectively. Tapcin exhibits antitumor activity in HT29 xenograft model.
    Tapcin
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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