RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively[1]. IC50: ~17 nM (p53-MDM2), ~24 nM (p53-MDMX)[1]
RO-5963 (10-20 μM; 48 hours) shows much higher apoptotic activity than Nutlin in both MCF7 and ZR75-30 cell lines[1].RO-5963 (10 μM, 24 hours) effectively activats p53 and elevates p21 and MDM2 levels[1]. Apoptosis Analysis[1] Cell Line: ZR75-30, MCF7 cells
[1]. Graves B, et al. Activation of the p53 pathway by small-molecule-induced MDM2 and MDMX dimerization. Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11788-93.