Small-molecule inhibitor: A-705253

Name

Common name: A-705253
Other names: N-(1-benzyl-2-carbamoyl-2-oxoethyl)-2-[E-2-(4-diethylaminomethylphenyl)ethen-1-yl]benzamide

History: A-705253 is a benzoylalanine-derived ketoamide that was described by Lubisch et al. (2003) as a nanomolar inhibitor of calpain 1 with oral bioavailability in rat.
Peptidases inhibited: calpain 1, calpain 2
Pharmaceutical relevance: It is reported that A-705253 prevents stress-induced tau hyperphosphorylation (Nikkel et al., 2012) and mitigates Alzheimer"s disease-like pathology and cognitive decline in aged 3xTgAD mice (Medeiros et al., 2012).