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 μM for both enzymes. It also potently inhibits glycogen synthase kinase 3 beta (GSK3β) with an IC50 of 0.21 μM. Furthermore, it effectively inhibits tau protein and Aβ1-42 peptide self-aggregation, and can bind the peripheral anionic site (PAS) to prevent amyloid-beta (Aβ)-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].

AChE/BChE-IN-5 (BMC-16) is a dual inhibitor of AChE and BChE that can cross the BBB, with IC50 values of 266 nM for human AChE (hAChE) and 10.6 nM for human BChE (hBChE) [1].

BChE-IN-5 is a potent and selective inhibitor of BChE (IC50: 2.8 nM) with a higher inhibitory effect on hBChE than hAChE and potential applications in Alzheimer's disease research.