RO-5963 is a potent, dual MDM2/MDMX-p53 interaction inhibitor with IC50 of 17 and 24 nM, respectively.
RO-5963 stabilizes p53 and activates the p53 pathway in cancer cells, inhibits the binding of p53 to MDM2 and MDMX.
RO-5963 restores p53 transcriptional activity, elevates protein levels of its transcription targets, p21 and MDM2, and overcomes the apoptotic resistance of MDMX-overexpressing cell line, SJSA-X, to nutlin-3.
RO-5963 decreases cell viability and induces cell death.
