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Description

A cell-permeable, potent, selective, peptidomimetic, non-transition-state analog inhibitor of gamma-secretase and Notch processing (IC50 = 300 pM for Abeta40 in CHO cells overexpressing wild type betaAPP, 240 pM for Abeta40, 370 pM for Abeta42, and 320 pM for NICD, respectively, in HEK293 cells stably transfected with betaAPP695 and mNotchDeltaE(M1727V), 100 pM for both Abeta40 and Abeta42 in SH-SY5Y cells stably transfected with SPA4CT). Lowers Abeta levels in several APP transgenic mouse models. Reported to bind to presenilins and suppress the proteolytic cleavage of transmembrane protein substrates, including APLP1 and APLP2, CD44, ErbB4, E-cadherin, low density lipoprotein receptor-related proteins, Notch ligands, and p75NTR. Only weakly affects presenilinase activity at much higher concentrations (200-400 µ,M).