CS-1

CS1 is a potent DNA Topo II α inhibitor. CS1 displays broad-spectrum in vitro antitumor effects, low toxicity in vivo and potential anti-multidrug resistance capabilities. CS1 leads to DNA damage, cell cycle arrest at G2/M phase and apoptosis[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

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

topoisomerase II alpha

CS1 shows cytotoxicity with IC50 values of 16.92 and 18.88 µM for MCF-7 and MCF7/ADR cells, respectively[1] . CS1 (10, 50, 100 µM) inhibits the activity of topoisomerase II α (Topo IIα)[1]. CS1 (0-20 µM) shows antiproliferation activity in cancer cells[1]. CS1 (2.5, 5, 10 µM) induces cell cycle arrest at the G2/M phase[1]. CS1 (2.5, 5, 10 µM) induces cell apoptosis[1]. CS1 (5, 10, 15 µM; 24 h) induces DNA breaks in MDA-MB-231 cells[1]. Cell Cycle Analysis[1] Cell Line: MDA-MB-231 cells Concentration: 2.5, 5, 10 µM Incubation Time: Result: Cells were arrest at the G2/M phase. Apoptosis Analysis[1] Cell Line: MDA-MB-231 cells Concentration: 2.5, 5, 10 µM Incubation Time: Result: Induced apoptosis

CS1 (20 mg/kg; i.v.; every other day for two weeks) shows antitumor effects[1]. Animal Model: Five-week-old female athymic nude mice (BALB/c-nu)[1] Dosage: 20 mg/kg Administration: i.v., every other day for two weeks Result: Showed antitumor effects.

[1]. Shen Y, et al. CS1 is a novel topoisomerase IIα inhibitor with favorable drug resistance profiles. Biochem Biophys Res Commun. 2014; 453(3):302-8.