209986-17-4

A cell-permeable, potent, selective, peptidomimetic, non-transition-state analog inhibitor of -secretase and Notch processing

ChEBI: Compound E is an L-alanine derivative that is the amide obtained by formal condensation of the carboxy group of N-[(3,5-difluorophenyl)acetyl]-L-alanine with the amino group of (3S)-3-amino-1-methyl-5-phenyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one. An inhibitor of memapsin 2 (gamma-secretase). It has a role as an EC 3.4.23.46 (memapsin 2) inhibitor. It is a 1,4-benzodiazepinone, a L-alanine derivative and a difluorobenzene.

Cell permeable: yes''Primary Target
γ-secretase and Notch processing Ab40 in CHO cells overexpressing wild type bAPP''Product does not compete with ATP.''Reversible: no''Target IC50: 300 pM for Aβ40 in CHO cells overexpressing wild typeβAPP; 240 pM for Aβ40370 pM for Aβ42and 320 pM for NICDrespectivelyin HEK293 cells stably transfected with βAPP695 and mNotchΔE(M1727V); 100 pM for both Aβ40

+4°C