Description
Nutlin-3 can inhibit MDM2 with IC50 of 90 nM.
Storage
2 years at -20centigrade Powder
Molecular Formula
C30H30Cl2N4O4
Chemical Name
4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one
Solubility
DMSO 100 mg/mL, Water
In vitro
Nutlin-3 is a small molecule inhibitor of the p53/MDM2 interaction, is sufficient to kill B-CLL cells. In vitro treatment with nutlin-3 induced a significant cytotoxicity on primary CD19 (+) B-CLL cells, but not on normal CD19(+) B lymphocytes, peripheral-blood mononuclear cells, or bone marrow hematopoietic progenitors. Nutlin-3 efficiently induces apoptosis and diminishes long-term survival of human fibroblasts transformed in vitro by Hdm2 but not HdmX. Nutlin-3 antagonists of MDM2, activate p53 and induce apoptosis in cancer cells.
In vivo
The MDM2 antagonist nutlin-3 induces the accumulation of p53 protein in B-CLL cells as well as in primary normal cells. Nutlin-3 induces a dose-dependent cytotoxicity on B-CLL cells.
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