MB710, an aminobenzothiazole derivative, is a stabilizer of oncogenic p53 mutation Y220C. MB710 binds tightly to the Y220C pocket and stabilizes p53-Y220C, with a Kd of 4.1?μM. MB710 shows anticancer activity in p53-Y220C cell lines[1].
MB710 (0-200 μM; 72 hours) shows relatively low toxicity against all cell lines tested at concentrations up to 60?μM, while showing initial selective viability reduction at higher concentrations[1].MB710 (72 hours) treats cancer cell lines NUGC3, NUGC4, WI38 and SW1088, with IC50s of 90, 120, >120, >120 μM, respectively[1].MB710 (0-120 μM; 72 hours; HUH-7 cells) shows stronger cytotoxic effects in presence of p53-Y220C[1].
[1]. Baud MGJ, et al. Aminobenzothiazole derivatives stabilize the thermolabile p53 cancer mutant Y220C and show anticancer activity in p53-Y220C cell lines. Eur J Med Chem. 2018;152:101-114.