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Description: Nutlin-3, a tetra-substituted imidazoline, is a novel potent and selective small-molecule antagonist/inhibitor of murine double minute 2 (MDM2) with potential antitumor activities. Nutlin-3 is essentially a PPI (protein protein interaction) inhibitor, it acts by occupying the binding site of p53 in MDM2 and consequently preventing MDM2 binding to p53, which leads to the disruption of the autoregulator feedback loop and the fostering of the p53 tumor suppressor network. It also binds to murine double minute 4 (MDM4), which is another component of the p35 tumor surveillance pathway. Nutlin-3 binds MDM2 in the TP53-binding pocket, thereby interfering with MDM2-directed TP53 degradation. isrupts its interaction with p53, leading to the stabilization and activation of p53.
References: Science. 2004 Feb 6; 303(5659):844-8; Nature. 2006 Nov 2; 444(7115):61-6.
Related CAS:548472-68-0 (Nutlin-3); 675576-98-4 (Nutlin-3a); 675576-97-3 (Nutlin-3b)
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