BNS-22

BNS-22 is a DNA topoisomerase II (TOP2) catalytic inhibitor with the IC50 values of 2.8 μM and 0.42 μM for human TOP2α and TOP2β, respectively. BNS-22 induces abnormal division and has anti-proliferative activity[1].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase

topoisomerase II alpha:2.8 μM (IC50, in human)

topoisomerase II beta:0.42 μM (IC50, in human)

BNS-22 (0-30 μM, 24-48 h) can inhibit cell growth and influence on cell cycle progression of the human cervical epidermoid carcinoma cell line HeLa in a dose-dependent manner[1]. BNS-22 (0-30 μM, 0-6 h) does not induce DNA damage and has an antagonistic effect on TOP2 toxin-mediated DNA damage[1]. Cell Proliferation Assay[1] Cell Line: HeLa cell lines Concentration: 0-30 μM Incubation Time: 24 h, 48 h Result: Inhibited cell growth with the IC50 value of 4.9 μM after 24 hours and 1.0 μM after 48 hours. Cell Cycle Analysis[1] Cell Line: HeLa cell lines Concentration: 0-30 μM Incubation Time: 24 h Result: Increased number of cells in G2/M phase. Disrupted mitotic spindle formation and induced polyploid cell formation at 3 μM. Western Blot Analysis[1] Cell Line: HeLa cell lines Concentration: 0-30 μM Incubation Time: 0, 30 min, 1 h, 2 h, 4 h, 6 h Result: Decreased etoposide-induced γ-H2AX expression and decreased total cellular TOP2β levels, but not TOP2α levels.

[1]. Makoto Kawatani, et al. Identification of a small-molecule inhibitor of DNA topoisomerase II by proteomic profiling. Chem Biol. 2011 Jun 24;18(6):743-51.