AChE/BChE-IN-12 (compound 10b), a 3,5-dimethoxy analogue, is a potent AChE , BChE , and β-secretase-1 (BACE-1) inhibitor, with IC 50 values of 2.57, 3.26, and 10.65 μM, respectively. AChE/BChE-IN-12 crosses the blood-brain barrier via passive diffusion and inhibits the self-aggregation of amyloid-β monomers. AChE/BChE-IN-12 can be used for Alzheimer’s disease (AD) research.