GFAP/NF-κB/APOE/NLRP3-IN-1

GFAP/NF-κB/APOE/NLRP3-IN-1 (Compound 11a) potently inhibits human acetylcholinesterase with an IC₅₀ of 3.50 nM, acting as a hybrid inhibitor targeting both the catalytic and peripheral anionic sites of the enzyme^[1].
GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits butyrylcholinesterase with an IC₅₀ of 4.30 μM, showing greater potency than donepezil^[1].
GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits BACE-1 with an IC₅₀ of 14.61 nM, demonstrating greater potency and higher selectivity over BACE-2 than the reference drug ly2886721^[1].
GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits Aβ_1-42 aggregation with an IC₅₀ of 8.63 μM, showing significantly greater potency than donepezil^[1].
GFAP/NF-κB/APOE/NLRP3-IN-1 has a comparable safety profile to donepezil in SH-SY5Y neuroblastoma cells, with an IC₅₀ of 80.3 μg/mL, and does not cause significant cytotoxicity at concentrations used for Aβ aggregation inhibition^[1].
GFAP/NF-κB/APOE/NLRP3-IN-1 exhibits high blood-brain barrier permeability with an effective permeability coefficient of 21.08 × 10^-6 cm/s, classifying it as CNS-permeable and showing greater permeability than donepezil^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.