GSK-3 inhibitor 3 is a selective, orally active, brain-permeable GSK-3 inhibitor that inhibits GSK-3α and GSK-3β with IC50s of 0.35 nM and 0.25 nM, respectively.GSK-3 inhibitor 3 reduces the phosphorylation level of tau protein S396 with an IC50 of 10 nM in a triple transgenic mouse model of Alzheimer's disease. GSK-3 inhibitor 3 reduced the phosphorylation level of tau protein S396 in a triple transgenic mouse model of Alzheimer's disease, with an IC50 of 10 nM.GSK-3 inhibitor 3 can be used for the study of neurological diseases.

CDK2:0.22 μM, GSK-3α:0.35 nM, CDK5:1.3 μM, GSK-3β:0.25 nM

GSK-3 inhibitor 3 (Compound 34) (1 μM) is a highly selective inhibitor of CDK2 and CDK5 with IC50s of 0.22 μM and 1.3 μM for CDK2 and CDK5, respectively.[1]

GSK-3 inhibitor 3 (Compound 34) (2 mg/kg; i.v.;10 mg/kg orally; Alzheimer’s disease model using LaFerla 3xTg-C57BL6 mice) demonstrated a T1/2 of 2.5 hours (i.v.) in male C57BL6 mice and an oral bioavailability (F%) of approx. 100%.[1]
GSK-3 inhibitor 3 (10 mg/kg, single oral dose) reduces Tau 396 phosphorylation levels by 33% in a triple transgenic mouse model of Alzheimer's disease.[1]