MDM2 Antagonist IV, Nutlin-3a ((-)-4-(4,5-bis-(4-Chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazole-1-carbonyl)piperazine-2-one)

Blue Ice

581, 5

Supplied as a white powder.

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.

Synonyms: (-)-4-(4, 5-bis-(4-Chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4, 5-dihydroimidazole-1-carbonyl)piperazine-2-one

CAS Number:
675576-98-4

Molecular Formula:
C₃₀H₃₀Cl₂N₄O₄

Solubility:
DMSO

Molecular Weight:
581.5

Storage and Stability:
Store at -20°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.