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Thiamet G is a potent and selective inhibitor of O-GlcNAcase with Ki value of 21 nM [1].

O-GlcNAcase is an enzyme that removes GlcNAc from proteins. O-GlcNAcylation refers to the posttranslational modification of O-linkage of N-acetyl-glucosamine moieties to threonine and serine residues on proteins [2].

Thiamet G is a potent and selective O-GlcNAcase inhibitor. In kinetic assays, thiamet G competitively inhibited human O-GlcNAcase with Ki value of 21 nM. Thiamet G was extremely stable in aqueous solution. In nerve growth factor (NGF)-differentiated PC-12 cells, thiamet G significantly increased cellular O-GlcNAc levels with EC50 value of 30 nM in a dose dependent way. Thiamet G significantly reduced phosphorylation levels at Ser396 and Thr231 of Tau by 2.1-fold and 2.7-fold, respectively. Also, thiamet G decreased the phosphorylation levels at Ser422 and Ser262 [1]. Thiamet G significantly sensitized human leukemia cell lines to paclitaxel, a microtubule-stabilizing agent [2].

In rats, thiamet G could readily cross the blood brain barrier and dose-dependently increased brain O-GlcNAc levels. Thiamet G reduced tau phosphorylation at Ser396, Thr231 and Ser422 by 2.7, 3.1 and 1.8-fold, respectively [1].

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