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-B0356R
    Ciprofloxacin (Standard)
    		Inhibitor
    Ciprofloxacin (Standard) is the analytical standard of Ciprofloxacin. This product is intended for research and analytical applications. Ciprofloxacin (Bay-09867) is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin has anti-proliferative activity and induces apoptosis. Ciprofloxacin is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
    Ciprofloxacin (Standard)
  • HY-16568R
    Irinotecan hydrochloride trihydrate (Standard)
    		Inhibitor
    Irinotecan (hydrochloride trihydrate) (Standard) is the analytical standard of Irinotecan (hydrochloride trihydrate). This product is intended for research and analytical applications. Irinotecan hydrochloride trihydrate ((+)-Irinotecan hydrochloride trihydrate) is a topoisomerase I inhibitor with antitumor activity.
    Irinotecan hydrochloride trihydrate (Standard)
  • HY-13768D
    Topotecan acetate
    		Inhibitor
    Topotecan acetate is a topoisomerase inhibitor.
    Topotecan acetate
  • HY-152473
    Topoisomerase IIα-IN-6
    		Inhibitor
    Topoisomerase IIα-IN-6 (Compound 47d) is an inhibitor of DNA topoisomerase IIα/β. Topoisomerase IIα-IN-6 inhibits human topoisomerase IIα and human topoisomerase IIβ with IC50 values of 0.67 µM and 0.55 µM, respectively. Topoisomerase IIα-IN-6 has stable metabolism.
    Topoisomerase IIα-IN-6
  • HY-144774
    Topoisomerase I inhibitor 5
    		Inhibitor
    Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin.
    Topoisomerase I inhibitor 5
  • HY-RS14890
    TOP1 Human Pre-designed siRNA Set A
    		Inhibitor

    TOP1 Human Pre-designed siRNA Set A contains three designed siRNAs for TOP1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    TOP1 Human Pre-designed siRNA Set A
    TOP1 Human Pre-designed siRNA Set A
  • HY-146021
    Topoisomerase IIα-IN-2
    		Inhibitor
    Topoisomerase IIα-IN-2 (compound 5) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-2 exhibits high antiproliferative activity against human cancer cell lines. Topoisomerase IIα-IN-2 significantly induces DNA damage and arrests cancer cells at G2/M phase.
    Topoisomerase IIα-IN-2
  • HY-151453
    Topoisomerase IIα-IN-4
    		Inhibitor
    Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC50 value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer.
    Topoisomerase IIα-IN-4
  • HY-N0716BR
    Berberine sulfate (Standard)
    		Inhibitor
    Berberine (sulfate) (Standard) is the analytical standard of Berberine (sulfate). This product is intended for research and analytical applications. Berberine sulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine sulfate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine sulfate has antineoplastic properties. The sulfate form improves bioavailability[1][2].
    Berberine sulfate (Standard)
  • HY-162587
    Fagopyrine
    		Inhibitor
    Fagopyrine is a DNA topoisomerase I (Topo I) inhibitor. Fagopyrine is a photosensitizer that can be used in the study of tumors.
    Fagopyrine
  • HY-147698
    ZLHQ-5f
    		Inhibitor
    ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC50 of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile.
    ZLHQ-5f
  • HY-162342
    Topoisomerase I inhibitor 14
    		Inhibitor
    Topoisomerase I inhibitor 14 (Compound 4h) is an inhibitor for Topoisomerase I. Topoisomerase I inhibitor 14 inhibits proliferation of A549 and C6 with IC50s of 4.56 μM and 13.17 μM, without significant toxicity in healthy cells NIH3T3 (IC50 is 74.44 μM), which exhibits anticancer potency.
    Topoisomerase I inhibitor 14
  • HY-161501
    3-Fluoro-evodiamine glucose
    		Inhibitor
    3-Fluoro-evodiamine glucose (Compound 8) is an evodiamine-glucose conjugate. 3-Fluoro-evodiamine glucose activates the expression of glucose transporter 1 (GLUT1), and inhibits topoisomerase I/II. 3-Fluoro-evodiamine glucose induces apoptosis and arrests the cell cycle at G2/M phase. 3-Fluoro-evodiamine glucose exhibits antitumor efficacy in vivo and in vitro, without significant toxicity.
    3-Fluoro-evodiamine glucose
  • HY-N11536
    erythro-Austrobailignan-6
    		Inhibitor
    erythro-Austrobailignan-6 is an orally active anti-cancer agent. erythro-Austrobailignan-6 inhibits DNA topoisomerase I and II activity. erythro-Austrobailignan-6 induces cell apoptosis and increases phosphorylation of p38 and JNK.
    erythro-Austrobailignan-6
  • HY-145859
    Topo I-IN-1
    		Inhibitor
    Topo I-IN-1 (Compound 14d) is a potent Topo I inhibitor with antitumor activity and DNA intercalative capability. Topo I-IN-1 induces cell apoptosis.
    Topo I-IN-1
  • HY-13629S1
    Etoposide-13C,d3
    		Inhibitor
    Etoposide-13C,d3 is the 13C- and deuterium labeled Etoposide. Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy[1].
    Etoposide-<sup>13</sup>C,d<sub>3</sub>
  • HY-17460R
    Garenoxacin (Standard)
    		Inhibitor
    Garenoxacin (Standard) is the analytical standard of Garenoxacin. This product is intended for research and analytical applications. Garenoxacin (BMS284756) is an orally active quinolone antibiotic and has a broad spectrum of activity against a wide array of gram-positive and gram-negative bacteria, anaerobes, and fastidious organisms.
    Garenoxacin (Standard)
  • HY-168632
    Topoisomerase I/II inhibitor 6
    		Inhibitor
    Topoisomerase I/II inhibitor 6 (compound 3i) is a potent inhibitor of topoisomerase I and II with IC50s of 4.77 and 15 µM, respectively. Topoisomerase I/II inhibitor 6 shows antiproliferative activities against human melanoma LOX IMVI cancer cell line with IC50 values of 26.7 and 25.4 µM, respectively. Topoisomerase I/II inhibitor 6 provokes substantial levels of early, late apoptosis and increases the expression level of active caspase-3.
    Topoisomerase I/II inhibitor 6
  • HY-118168
    A 9387
    		Inhibitor
    A9387 is an inhibitor of the Tn3 Resolvase, which promotes site-specific recombination reactions between two directly repeated recombination sites. Several inhibitors have been isolated that inhibit this event. A9387 inhibits the binding of resolvase to the res site.
    A 9387
  • HY-163723
    EGFR-IN-116
    		Inhibitor
    EGFR-IN-116 (compound 14D) is an anticancer agent. EGFR-IN-116 against EGFR has the IC50 values​of EGFR, VEGFR-2 and Topo II are 0.103 μM, 0.069 μM and 19.74 μM, respectively.
    EGFR-IN-116
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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