Thiamet G

Thiamet G is a potent and selective inhibitor of O-GlcNAcase with a Ki value of 21 nM. It increases cellular O-GlcNAc-modified protein levels with an EC₅₀ of 30 nM and blocks phosphorylation of tau protein both in cultured PC-12 cells and in rats (200 mg/kg/day). It is the first highly potent O-GlcNAcase inhibitor known to be orally bioavailable and can effectively cross the blood brain barrier. It may potentially block pathological hyperphosphorylation of tau in Alzheimer's disease.