NSC 66811 is a potent inhibitor of murine double minute 2 (Mdm2) interaction with p53 by binding Mdm2 (Ki = 120 nM), in this way activating p53. NSC 66811 induces the accumulation of p21, p53, and Mdm2 in human colon cancer cells in vitro. Inhibitors of the Mdm2-p53 interaction, including NSC 66811, induce p53- and p21-dependent cell cycle arrest and p53-dependent cell death in tumor cell lines.
