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γ-Secretase Inhibitor XXI, Compound E
(S,S)- 2-[2-(3,5-Difluorophenyl)-acetylamino]-N-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-propionamide, 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(M1727V); 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 (200-400 µM).
产品信息
Form White solid
Primary Target γ-secretase and Notch processing Ab40 in CHO cells overexpressing wild type bAPP
Primary Target IC50 300 pM
Secondary target 240 pM for Aβ40, 370 pM for Aβ42, and 320 pM for NICD, respectively, in HEK293 cells stably transfected with bAPP695 and mNotchDE(M1727V); 100 pM for both Aβ40 and Aβ42 in SH-SY5Y cells stably transfected with SPA4CT
Molar mass 490.5
Protect from Light 是的
Packaged under inert gas 是的
Cell permeable 是的
Purity ≥95% by HPLC
Solubility DMSO
Chemical formula C27H24F2N4O3
CAS number 209986-17-4
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling |