semagacestat-ly450139

Description: Semagacestat (also known as LY450139; LY4501) is a novel and potent gamma-secretase inhibitor/blocker for Abeta42, Abeta40 and Abeta38 with the potential for treating Alzheimer's disease. It inhibits Abeta42, Abeta40 and Abeta38 with IC50 calues of 10.9 nM, 12.1 nM and 12.0 nM, it also inhibits Notch signaling with IC50 of 14.1 nM in H4 human glioma cell. Semagacestat was in Phase III trials, but was terminated in August 2010, due to a disppointing performance.

References: J Neurosci. 2012 Feb 8; 32(6):2037-50; J Neurochem. 2009 Sep; 110(5):1377-87.

Chemical Name: (S)-2-hydroxy-3-methyl-N-((S)-1-(((S)-3-methyl-2-oxo-2, 3, 4, 5-tetrahydro-1H-benzo[d]azepin-1-yl)amino)-1-oxopropan-2-yl)butanamide

SMILES Code: CC(C)[CH](O)C(N[CH](C)C(N[CH]1C(N(C)CCC2=CC=CC=C12)=O)=O)=O