Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Primary TargetMDM2

Cell permeable: yes

Target IC₅₀: 90 nM for Nutlin-3a and 13.6 µM for Nutlin-3b

General description

A cell-permeable cis-imidazoline compound that acts as a potent and selective MDM2 antagonist (IC₅₀ = 90 nM for Nutlin-3a and 13.6 µM for Nutlin-3b) and displays antitumor properties. Activates p53 pathway by binding MDM2 in the p53-binding pocket and inhibits MDM2-p53 interaction. Shown to suppress tumor growth by induction of apoptosis in several cancer cells with wild-type p53 and in xenografted tumor mice. A 10 mM (1 mg/172 µl) solution of MDM2 Antagonist, Nutlin-3, Racemic (Cat. No. 444151) in DMSO is also available.

A cell-permeable, potent, and selective MDM2 antagonist (IC₅₀ = 90 nM for Nutlin-3a and 13.6 µM for Nutlin-3b) that displays antitumor properties. Activates the p53 pathway by binding MDM2 in the p53-binding pocket and inhibiting the MDM2-p53 interaction. Shown to induce apoptosis in several cancer cell lines with wild-type p53 and in xenografted tumor mice.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Thompson, T., et al. 2004. J. Biol. Chem.279, 53015.Vassilev, L.T., et al. 2004. Science303, 844.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot, purge with inert gas, and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Harmful (C)