HAChE-IN-5

HAChE-IN-5 (compound 49) is a dual inhibitor of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBuChE), showing IC50 values of 0.17 ?M for both enzymes. It also potently inhibits glycogen synthase kinase 3 beta (GSK3?) with an IC50 of 0.21 ?M. Furthermore, it effectively inhibits tau protein and A?1-42 peptide self-aggregation, and can bind the peripheral anionic site (PAS) to prevent amyloid-beta (A?) -induced neurotoxicity. hAChE-IN-5's ability to cross the blood-brain barrier (BBB) supports its potential in developing multitargeted anti-Alzheimer's agents [1].