A cell-permeable and highly potent active enantiomer of Nutlin-3 (Cat. No. 444143) that binds to the p53-binding pocket and blocks the interaction of p53 and MDM2 (IC₅₀ = 90 nM). 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.

Packaged under inert gas

Toxicity: Standard Handling (A)

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

Ohnstad, H.O., et al. 2011. BMC Cancer11, 211.
Shen, H. and Maki, C.G., 2010. J. Biol. Chem.285, 23105.
Kawamura, T., et al. 2009. Nature460, 1140.
Kojima, K., et al. 2006. Blood108, 993.
Laurie, N.A., et al. 2006. Nature444, 61.
Tovar, C., et al. 2006. Proc. Natl. Acad. Sci. USA103, 1888.
Vassilev, L.T. 2006. Trends Mol Med.13, 23.
Thompson, T., et al. 2004. J. Biol. Chem.279, 53015.
Vassilev, L.T., et al. 2004. Science303, 844.

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