A cell-permeable and reversible inhibitor of Hdm2 E3 ligase that selectively blocks Hdm2 E3-mediated ubiquitination. Has been shown to inhibit ubiquitination of p53 in vitro (IC₅₀ = 12.7 µM using Ub-Ubc as the donor substrate). Exhibits little effect towards other ubiquitin-using enzymes (IC₅₀ >100 µM for E1, Nedd-4, and SCF) or the auto-ubiquitination activity of Hdm2. The inhibition is non-competitive with respect to either the donor or acceptor substrate.

Cell permeable: yes

Primary Target
ubiquitination of p53 in vitro

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 12.7 µM inhibiting ubiquitination of p53 in vitro using Ub-Ubc as the donor substrate

Packaged under inert gas

Lai, Z., et al. 2002. Proc. Natl. Acad. Sci. USA99, 14734.

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

Toxicity: Standard Handling (A)