Compound E

gamma-Secretase is a multimeric aspartyl protease that regulates signaling pathways by proteolytically cleaving substrates, abrogating or releasing signaling molecules. Two well-known substrates are the carboxyl-terminal fragments (CTFs) of the receptor Notch, which has key roles in development, and that of amyloid precursor protein (APP), which is important in Alzheimer's disease. Compound E is a potent, cell-permeable, and selective inhibitor of gamma-secretase, blocking the cleavage of both APP and Notch CTFs with IC50 values of ~0.3 nM. Compound E induces neuronal differentiation, impairs ovarian folliculogenesis, and suppresses thymocyte development by preventing Notch activation by gamma-secretase.Formal Name: N-[(1S)-2-[[(3S)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-benzeneacetamide. CAS Number: 209986-17-4. Synonyms: gamma-Secretase Inhibitor XXI. Molecular Formula: C27H24F2N4O3. Formula Weight: 490.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS (pH7.2) (1:30): 0.03 mg/ml, DMSO: 20 mg/ml, Ethanol: 2 mg/ml. lambdamax: 228 nm. SMILES: O=C1[C@@H](NC([C@H](C)NC(CC2=CC(F)=CC(F)=C2)=O)=O)N=C(C3=CC=CC=C3)C4=C(C=CC=C4)N1C. InChi Code: InChI=1S/C27H24F2N4O3/c1-16(30-23(34)14-17-12-19(28)15-20(29)13-17)26(35)32-25-27(36)33(2)22-11-7-6-10-21(22)24(31-25)18-8-4-3-5-9-18/h3-13,15-16,25H,14H2,1-2H3,(H,30,34)(H,32,35)/t16-,25+/m0/s1. InChi Key: JNGZXGGOCLZBFB-IVCQMTBJSA-N.