MRK-003

MRK-003 is a potent and selective small molecule γ-secretase inhibitor developed by Merck. It acts by inhibiting the γ-secretase complex responsible for the proteolytic cleavage of several substrates including amyloid precursor protein (APP) and Notch receptor proteins. By blocking γ-secretase activity, MRK-003 reduces production of amyloid-beta peptides implicated in Alzheimer's disease pathology and inhibits Notch signaling relevant to cancer biology. Preclinical studies have shown that MRK-003 induces caspase-dependent apoptosis and inhibits proliferation in multiple myeloma and non-Hodgkin's lymphoma cell lines as well as reducing brain Aβ production in vivo[1][6]. It is considered an experimental compound with no reported clinical development beyond preclinical stages for Alzheimer's disease or cancer[5].

Other names

(1'R,4R)-2-(2,2,2-trifluoroethyl)-5'-[(E)-3-[4-(trifluoromethyl)piperidin-1-yl]prop-1-enyl]spiro[1,2,5-thiadiazolidine-4,13'-tricyclo[8.2.1.03,8]trideca-3(8),4,6-triene] 1,1-dioxideMRK003MRK-003MRK 003DJ2AZE88DEDJ-2AZE88DEDJ 2AZE88DE623165-93-5