Comments: gamma-secretase modulator (GSM) that blocks gamma-secretase cleavage of amyloid-beta protein precursor (AbetaPP Bioactivity comments: Mechanism of action thought to be gammasecretase modulation but no quantitiative data reported.
Comments: gamma-secretase and Notch pathway inhibitor that was originally intended for the treatment of Alzheimer Bioactivity comments: gamma-secretase-mediated Notch receptor cleavage in vitro . Since gamma-secretase is a protein complex
Comments: gamma-secretase inhibitor (GSI) for Alzheimer's Disease that selectively inhibits cleavage of APP over Bioactivity comments: gamma-secretase function, and displaces a tritiated analog of GSI-953 from enriched gamma-secretase
Comments: gamma-secretase inhibitor. It is a reversible, non-competitive, and orally bioactive agent. It was proposed Clinical use: gamma-secretase inhibitor to reach the clinic and was the first approved treatment for desmoid Bioactivity comments: gamma-secretase activity with an IC50 of 1.2nM , measured as a reduction of Abeta
Synonyms: gamma-Secretase Inhibitor IX Comments: gamma-secretase inhibitor that is used experimentally to inhibit NOTCH pathway signalling. Chemically it is a modified Bioactivity comments: gamma-secretase inhibitor IN973 from the enzyme complex in human THP-1 cells in vitro
Comments: gamma-secretase/NOTCH pathway inhibitor that was developed for anti-tumour potential . Structurally, it is a modified Bioactivity comments: gamma-secretase-madiated cleavage of NOTCH1 in MDA-MB-231 cancer cells with an IC50
Comments: gamma-secretase inhibitor that was developed by Eli Lilly as a potential treatment for Alzheimer Bioactivity comments: Shows potent Inhibition of gammasecretase-mediated amyloid beta (1 to 40) production in vitro
Comments: gamma-secretase modulator (GSM). These are small molecules (<600 Da) causing a product shift from Bioactivity comments: Note as a GSM the potency of gammasecretase inhibition is low