hAChE/hBACE-1-IN-2 is a potent, orally active, blood-brain barrier transboundary triple inhibitor of hAChE , hBChE , and HACE-1 with IC 50 s of 0.113 μM, 1.48 μM and 0.38 μM, respectively. hAChE/hBACE-1-IN-2 has antioxidant activity. hAChE/hBACE-1-IN-2 also inhibits Aβ1 1-42 aggregation. hAChE/hBACE-1-IN-2 can be used to study Alzheimer's disease.