Verubecestat (MK-8931)

Description: MK-8931 (also known as Verubecestat or SCH 900931) is a beta-secretase 1 and BACE1 inhibitor that is in Phase 3 clinical trial for treatment of Alzheimer's disease. Amyloidogenic pathway in Alzheimer's disease (AD) involves breakdown of APP by beta-secretase followed by gamma-secretase and results in formation of amyloid beta plaque. beta-secretase has been a promising target for developing novel anti-Alzheimer drugs.MK-8931 binds significantly to beta-secretase. target: BACE1. In vitro:MK-8931 can effectively reduce Abeta40 in cells with a Ki of 7.8 nM and an IC50 of 13 nM. Docking revealed that, with respect to their free binding energy, acylguanidine 7a has the lowest binding energy followed by MK-8931 and pioglitazone and binds significantly to beta-secretase.

References: Transl Neurodegener. 2016 Jul 14; 5:13; Adv Bioinformatics. 2016; 2016:9258578.

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