A nutlin-3 analog with p53 modulating activity 1 mg

Description

The protein p53, often called the ‘guardian of the genome,’ is a transcription factor that is activated in response to cellular stress (low oxygen levels, heat shock, DNA damage, etc.) and acts to prevent further proliferation of the stressed cell by promoting cell cycle arrest or apoptosis.1,2 Its role as a tumor suppressor is evident by the observation that approximately 50% of human tumors have mutated or non-functional p53. Mdm2, a key negative regulator of p53 which is over-expressed in many human tumors, functions by binding to and targeting p53 for proteasomal degradation. Nutlin-3 inhibits p53-Mdm2 interaction with a IC50 of 0.09 µM.3 It induces the expression of p53-regulated genes and exhibits potent antiproliferative activity in cells with functional p53, but not in cells with mutated p53. Nutlin-3 also inhibits the growth of human tumor xenografts in nude mice by 90% at a dose of 200 mg/kg.3WARNING This product is not for human or veterinary use.