Packaged under inert gas.
565790-500
565790-1MG
565790-500EA
446
EUR
InStock
565790-500
565790-1MG
Compound E ≥95% (par HPLC) Calbiochem®, Sigma-Aldrich®
Compound E
A cell-permeable, potent, selective, peptidomimetic, non-transition-state analog inhibitor of γ-secretase and Notch processing (IC₅₀=300 pM for Aβ₄₀ in CHO cells overexpressing wild type βAPP; 240 pM for Aβ₄₀, 370 pM for Aβ₄₂, and 320 pM for NICD, respectively, in HEK293 cells stably transfected with βAPP₆₉₅
and mNotchδE; 100 pM for both Aβ₄₀ and Aβ₄₂ in SH-SY5Y cells stably transfected with SPA4CT).
Lowers Aβ 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 to 400 µM).