Potent, selective O-GlcNAcase inhibitor (K i = 21 nM). Blocks tau phosphorylation. Increases O-GlcNAc-modified protein levels (EC 50 = 30 nM). Shows antitauopathic effects in vivo . Orally active. Blood-brain barrier permeable.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of O-GlcNAcase
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
Thiamet G is a potent and selective inhibitor of O-GlcNAcase (OGA), which acts to remove O-GlcNAc from modified proteins, with Ki of 20 nM for human OGA.
Application：
Thiamet G has been used as an O-GlcNAcase inhibitor:
to treat human embryonic kidney 293 cells in order to study its effect on Wnt/beta-catenin signalling
to treat lytically-replicating producer
to incubate mice (C57BL/6) aortic segments to increase global O-GlcNAc levels
1.Yuzwa SA, Macauley MS, Heinonen JE, Shan X, Dennis RJ, He Y, Whitworth GE, Stubbs KA, McEachern EJ, Davies GJ et al.. (2008) A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo.. Nat Chem Biol, 4 (8):(483-90). [PMID:18587388]
2.Selnick HG, Hess JF, Tang C, Liu K, Schachter JB, Ballard JE, Marcus J, Klein DJ, Wang X, Pearson M et al.. (2019) Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies.. J Med Chem, 62 (22):(10062-10097). [PMID:31487175]
3.Weng Y et al.. (2021) O-GlcNAcylation drives calcium signaling toward osteoblast differentiation: A bioinformatics-oriented study.. Biofactors, 47 (6):(992-1015). [PMID:34418170]
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