AChE-IN-12

AChE-IN-12 is a potent and blood-brain barrier (BBB) penetrant acetylcholinesterase (AChE) with IC50s of 0.41 μM and 1.88 μM for rat AChE and electric eel AChE. AChE-IN-12 is also a good antioxidant (ORAC = 3.3 eq), selective metal chelator and huMAO-B inhibitor (IC50 = 8.8 µM). AChE-IN-12 has remarkable inhibition of self- and Cu2+-induced Aβ1-42 aggregation, as well as exhibits a good neuroprotective effect. AChE-IN-12 can be used for researching Alzheimer’s disease[1].

Signaling Pathways >> Neuronal Signaling >> Monoamine Oxidase

Research Areas >> Neurological Disease

Signaling Pathways >> Neuronal Signaling >> AChE

IC50: 0.41 μM (rat AChE), 1.88 μM (electric eel AChE), 8.8 µM (huMAO-B)[1]

AChE-IN-12 (compound 17f）(10-100 μM) exhibits no obvious cytotoxicity until the concentration increased up to 50 µM[1]. AChE-IN-12 (10 and 50 μM) adds up the cell viability of H2O2-induced PC12 cells[1]. Cell Cytotoxicity Assay Cell Line: PC12 cells[1] Concentration: 10, 50 and 100 μM Incubation Time: Result: Did not show obvious cytotoxicity until the concentration increased up to 50 µM. Cell Viability Assay Cell Line: PC12 cells (exposed to 100 µM H2O2 for 1 hour to establish the oxidative damage model)[1] Concentration: 10 and 50 μM Incubation Time: Result: Added up the cell viability to 65.7% (p < 0.05) and 73.4% (p < 0.05) at 10 and 50 μM, respectively.

[1]. Sang Z, Song Q, Cao Z, Deng Y, Zhang L. Design, synthesis, and evaluation of chalcone-Vitamin E-donepezil hybrids as multi-target-directed ligands for the treatment of Alzheimer's disease. J Enzyme Inhib Med Chem. 2022;37(1):69-85.