β-Secretase Inhibitor IV is a potent, cell-active inhibitor of BACE-1(IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively).

Cathepsin D:7620±210 nM , BACE1:15.3±0.6 nM , BACE2:230±26 nM

β-Secretase Inhibitor IV (Compound 2) inhibits the production of Aβ peptides with an EC50 of 43 nM in the cell culture assay. β-Secretase Inhibitor IV potently suppresses the secretion of sAPP_NF and EV40 from HEK293T cells(IC50 : 30 nM).