RO-5963

RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively[1].

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> MDM-2/p53

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 Concentration: 10, 20 μM Incubation Time: 48 hours Result: Potently showed apoptotic activity. Western Blot Analysis[1] Cell Line: LNCap, U2OS, RKO, A489, 22Rv1, HCT116, H460, LOX, MCF7, A549, G401 cells Concentration: 10 μM Incubation Time: 24 hour Result: Effectively activated p53 and elevated p21 and MDM2 levels.

[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.