Thiamet G

CAS No. : 1009816-48-1

Thiamet G,1009816-48-1
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000110
Molecular Formula:C9H16N2O4S
Molecular Weight:248.3
Target:O-GlcNAcase inhibitor
IC50:21 nM [1]
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Appearance:A crystalline solid
Cat No:I000110
Cas No:1009816-48-1
Product-Name:Thiamet G

Thiamet G is a potent and selective inhibitor of O-GlcNAcase that demonstrates a Ki value of 21 nM.
IC50 value: 21 nM [1]
Target: O-GlcNAcase inhibitor
Thiamet G increases cellular O-GlcNAc-modified protein levels (EC50 = 30 nM) and blocks phosphorylation of tau protein both in cultured PC-12 cells and in rats (200 mg/kg/day). Thiamet G is the first highly potent O-GlcNAcase inhibitor known to be orally bioavailable and effectively cross the blood brain barrier.

[1]. Yuzwa SA, et al. Increasing O-GlcNAc slows neurodegeneration and stabilizes tau against aggregation. Nat Chem Biol. 2012 Feb 26;8(4):393-9.
[2]. Andrés-Bergós J, et al. The increase in O-linked N-acetylglucosamine protein modification stimulates chondrogenic differentiation both in vitro and in vivo. J Biol Chem. 2012 Sep 28;287(40):33615-28.
[3]. Ding N, et al. Thiamet-G-mediated inhibition of O-GlcNAcase sensitizes human leukemia cells to microtubule-stabilizing agent paclitaxel. Biochem Biophys Res Commun. 2014 Oct 24;453(3):392-7.

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