Drug intelligence / Profile preview

tert-butyl (2S)-2-[[(2S)-2-[[2-(3,5-difluorophenyl)acetyl]amino]propanoyl]amino]-2-phenylacetate

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

DAPT (N-[N-(3,5-difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl ester) is a potent and orally active small molecule that functions as a gamma-secretase inhibitor. By inhibiting gamma-secretase, DAPT indirectly modulates the Notch signaling pathway, as Notch is a key substrate for gamma-secretase. This mechanism leads to a reduction in the production of amyloid-beta (Aβ) and Aβ42, and can induce cell differentiation, autophagy, and apoptosis. DAPT exhibits neuroprotective activity and is primarily used in research settings to study neurodegenerative conditions like Alzheimer's disease, as well as autoimmune and lymphoproliferative diseases, and various cancers. It is also employed to modulate Notch activity in embryonic stem cell differentiation.

Other names
N-[N-(3,5-difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl esterN-[(3,5-Difluorophenyl)acetyl]-L-alanyl-2-phenyl]glycine-1,1-dimethylethyl ester
02

Targets

GSEC (Gamma-Secretase Complex)BACE1 (Beta-site APP-cleaving enzyme 1)

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