GSK3β-IN-3 is an ATP-competitive GSK-3β inhibitor (IC50= 0.90 μM) that demonstrates good blood-brain barrier permeability (Pe= 10.7 x 10^-6 cm/s). It effectively reduces tau protein phosphorylation in the BR5706 strain and decreases Aβ aggregate deposition in the CL2006 strain, indicating its potential as a candidate for Alzheimer's disease (AD) research.

GSK-3β:0.90 μM

GSK3β-IN-3 (compound 66) effectively inhibits GSK-3β with an IC50 of 0.90 μM at concentrations ranging from 0.01 to 100 μM. Additionally, GSK3β-IN-3 exhibits ATP-competitive inhibition of the GSK-3β enzyme at concentrations of 0-50 μM.

GSK3β-IN-3 (compound 66), at a concentration of 10 μM, reduces p-Tau (Ser396) levels in the Caenorhabditis elegans BR5706 strain. It also increases the number of flagella and reduces Aβ deposition in the C. elegans CL2006 strain. Furthermore, GSK3β-IN-3 demonstrates good stability in human microsomes and shows potential for crossing the blood-brain barrier in PAMPA-BBB assays. It has a high plasma protein binding rate of 96.4%.