Nutlin-3

Nutlin-3 is a small molecule inhibitor of the MDM2/p53 interaction, which leads to the non-genotoxic p53 stabilization, activation of cell cycle arrest and apoptosis pathways. Nutlin-3 inhibits the MDM2-p53 interaction with IC50 of 0.09 μM and synergistically activates p53 to suppress tumor growth. Nutlin-3 induces apoptosis in cancer cells. Nutlin-3 treatment induces the expression of MDM2 and p21, and displays potent antiproliferative activity with IC50 of ~1.5 μM in cells with wild-type p53 such as HCT116, RKO and SJSA-1. Nutlin-3 is currently in phase I clinical trial for the treatment of retinoblastoma.