N-((3,3,3-Trifluoro-2-trifluromethyl)propionyl)sulfanilamide Pale yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. 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. Purity: ≥90% by HPLC. Ref.: Lai, Z., et al. 2002. Proc. Natl. Acad. Sci. USA 99, 14734. |
