Thiamet-G
O-GlcNAcase α1 antagonist / Potent, selective inhibitor of O-GlcNAcase (Ki = 21 nM for human O-GlcNAcase). Increases levels of O-GlcNAc-modified proteins in cellular assays and in vivo. Suppresses phosphorylation of tau protein in rat cortex and hippocampus.1 Stabilizes tau against aggregation and slows neurodegeneration.2 Prevents cognitive decline and amyloid plaque formation in bigenic tau/APP mutant mice.3 Active in vivo and blood brain barrier permeable.
Biochemicals & reagents
1009816-48-1
Thiamet G
1) Yuzwa et al. (2008), A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo; Nat.Chem.Biol. 4 483 2) Yuzwa et al. (2012), Increasing O-GlcNAc slows neurodegeneration and stabilizes tau against aggregation; Nat.Chem.Biol. 8 393 3) Yuzwa et al. (2014), Pharmacological inhibition of O-GlcNAcase (OGA) prevents cognitive decline and amyloid plaque formation in bigenic tau/APP mutant mice; Mol.Neurodegener. 9 42
-20°C
TARGET: Glycosylation -- PATHWAY: GlcNAc -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Neurodegeneration