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Beschreibung

A cell-permeable hydroxyethylene dipeptide isostere that acts as a highly specific and a potent inhibitor of gamma-secretase (Abetatotal IC50 = 17 nM, Abeta40 IC50 = 48 nM, and Abeta42 IC50 = 67 nM in SHSY5Y cells overexpressing spbetaA4CTF). Binds to presenilin and blocks Notch intracellular domain production. Functions as a transition state analog mimic at the catalytic site of an aspartyl protease, however, it exhibits over 100-fold greater selectivity for gamma-secretase than for cathepsin D., A cell-permeable hydroxyethylene dipeptide isostere that acts as a potent and highly specific inhibitor of gamma-secretase (Abeta total IC50 = 17 nM, Abeta40 IC50 = 48 nM, and Abeta42 IC50 = 67 nM in SH-SY5Y cells overexpressing spbetaA4CTF). Binds to presenilin and blocks Notch intracellular domain production. Also reported to block the formation of epsilonCTF, resulting in the accumulation of alpha- and betaCTF. Functions as a transition state analog mimic at the catalytic site of an aspartyl protease, however, it exhibits over 100-fold greater selectivity for gamma-secretase than for cathepsin D.