A stabilizer of mutant p53, increases the thermal stability and inhibits aggregation of the mutant p53Y220C DNA-binding domain (Kd = 4 µM), selectively inhibits growth of NUGC-3 cells expressing p53Y220C over WI38 cells that do not express the p53Y220C mutant (IC50s = 90 and >120 µM, respectively), selectively...

Description: MB710, an aminobenzothiazole derivative, stabilizes the oncogenic p53 mutation Y220C by binding tightly to the Y220C pocket, enhancing the stability of p53-Y220C with a dissociation constant (Kd) of 4.1 µM. This compound exhibits anticancer activity in cell lines harboring the p53-Y220C mutation [1]....