Small-molecule inhibitor: semagacestat

Summary Literature

Name

Common name: semagacestat
Other names: LY450139

Inhibition

History: The development of semagacestat has been reviewed by Henley et al. (2009).
Peptidases inhibited: Inhibits the gamma-secretase activity of the complex in which the active peptidase is presenilin 1 and/or presenilin 2 (Imbimbo, 2008).
Pharmaceutical relevance: Semagacestat has been submitted to clinical trials related to the treatment of Alzheimer"s disease (Henley et al., 2009).

Chemistry

CID at PubChem: 9843750
Structure
Chemical/biochemical name: (2S)-2-hydroxy-3-methyl-N-[(2S)-1-[[(1S)-3-methyl-2-oxo- 4,5-dihydro-1H-3-benzazepin-1-yl]amino]-1-oxopropan-2- yl]butanamide; hydroxylvaleryl monobenzocaprolactam
Formula weight: 361