85-2074-38 MDM2 Antagonist IV, Nutlin-3a ((-)-4-(4,5-bis-(4-Chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazole-1-carbonyl)piperazine-2-one) 5mg CAS No:675576-98-4 217535
A cell-permeable and highly potent active enantiomer of Nutlin-3 that binds to the p53-binding pocket and blocks the interaction of p53 and MDM2 (IC50=90nM). Exhibits over 150-fold greater affinity for MDM2 than its less active enantiomer, Nutlin-3b. Induces p53 mediated apoptosis by both transcription-dependent and independent mechanisms. Shown to greatly potentiate the cytotoxic effects of chemotherapeutic agents and reduce tumor burden in vivo. Also shown to overcome ATM-mediated resistance to fludarabine in chronic lymphocyte leukemia. Cells treated with Nutlin-3a permanently lose their ability to proliferate and enter into a pattern of permanent senescence. Mouse embryonic fibroblasts with p53+/+ MEFs show significantly reduced reprogramming capabilities following Nutlin-3a treatment.