A cell-permeable phenyl-pyraz-olylidene compound that competes with p53-derived peptide (aa 15-29) binding to MDMX in cell-free binding assays (EC₅₀ = 2.3 µM) in a reversible manner and effectively disrupts cellular p53-MDMX interaction (IC₅₀<20 µM in C33A, HER, and Weri1 cultures), while exhibiting much weaker affinity toward MDM2 (EC₅₀ = 26 µM in p53 peptide competition assays). MDMX inhibition by 20 µM SJ-172550 and MDM2 inhibition by 5 µM Nutlin-3a (Cat. Nos. 444143 & 444151) are both shown to result in reduced proliferation and increased cellular caspase-3 in cultured cells, however, only MDM2, but not MDMX, inhibition results in a significant p53 protein level upregulation.

A cell-permeable phenyl-pyrazolylidene compound that competes with p53-derived peptide (aa 15-29) binding to MDMX in cell-free binding assays (EC₅₀ = 2.3 M) in a reversible manner and effectively disrupts cellular p53-MDMX interaction (IC₅₀<20 M in C33A, HER, and Weri1 cultures), while exhibiting much weaker affinity toward MDM2 (EC₅₀ = 26 M in p53 peptide competition assays). MDMX inhibition by 20 M SJ-172550 and MDM2 inhibition by 5 M Nutlin-3a are both shown to result in reduced proliferation and increased cellular caspase-3 in cultured cells, however, only MDM2, but not MDMX, inhibition results in a significant p53 protein level upregulation.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C. Stock solutions are stable for up to 6 months at -20°C.

Reed, D., et al. 2010. J. Biol. Chem.285, 10786.

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

Toxicity: Standard Handling (A)