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Nutlin-3MDM2 antagonist,inhibits MDM2-p53 interaction

Nutlin-3

Catalog No. A4228
Size Price Stock Qty
Evaluation Sample $28.00 In stock
5mg $80.00 In stock
10mg $120.00 In stock
25mg $260.00 In stock
100mg $590.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Nutlin-3

Related Biological Data

Nutlin-3

Related Biological Data

Nutlin-3

Related Biological Data

Nutlin-3

Biological Activity

Description Nutlin-3 is a potent and selective antagonist of Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) with IC50 of 90 nM.
Targets Mdm2          
IC50 90 nM          

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Chemical Properties

Cas No. 890090-75-2 SDF Download SDF
Synonyms Nutlin 3,MDM2 Antagonist
Chemical Name 4-[4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazin-2-one
Canonical SMILES CC(C)OC1=C(C=CC(=C1)OC)C2=NC(C(N2C(=O)N3CCNC(=O)C3)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl
Formula C30H30Cl2N4O4 M.Wt 581.5
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Nutlin-3, a tetra-substituted imidazoline, is a potent and selective small-molecule antagonist of murine double minute 2 (MDM2), which occupies the binding site of p53 in MDM2 and consequently prevent MDM2 binding to p53 leading 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 is being investigated as an antitumor agent for its antiangiogenic activity in cells through inhibiting endothelial cell migration, inducing cell cycle arrest, and increasing apoptotic tendency in endothelial cells. 

Reference

Bernd R. Binder. A novel application for murine double minute 2 antagonists: the p53 tumor suppressor network also controls angiogenesis. Circ Res. 2007; 100: 13-14