Small-molecule inhibitor: DAPT

Summary Literature

Name

Common name: DAPT
Other names: gamma-secretase inhibitor IX; GSI-IX; N-[N-(3,5-difluorophenylacetyl)-L-alanyl]-S-phenylglycine tbutyl ester

Inhibition

History: An early published account of DAPT was that of Dovey et al. (2001).
Peptidases inhibited: Considered to be a specific inhibitor of the gamma-secretase activity of the complexes of presenilin.
Mechanism: inhibition is reversible.
Pharmaceutical relevance: DAPT, given orally to mice, significantly lowered amyloidogenic peptide levels in brain (El Mouedden et al., 2006).

Chemistry

CID at PubChem: 2956
Structure
Chemical/biochemical name: N-[N-(3,5-difluorophenacetyl)-l-alanyl]-S-phenylglycine t-butyl ester
Formula weight: 432