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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
MDM2
Product does not compete with ATP.
Reversible: no
Target IC50: 90 nM for Nutlin-3a and 13.6 µM for Nutlin-3b
Packaging
Packaged under inert gas
Warning
Toxicity: Harmful (C)
Reconstitution
Following reconstitution, aliquot, purge with inert gas, and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Thompson, T., et al. 2004. J. Biol. Chem.279, 53015.
Vassilev, L.T., et al. 2004. Science303, 844.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 444143-1MG
