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Thiamet G CAS: 1009816-48-1

Category: Inhibitors
Product Name: Thiamet G
Cat No: I000110
CAS No: 1009816-48-1
Synonyms: 2-(ethylamino)-3aR,6S,7R,7aR-tetrahydro-5R-(hydroxymethyl)-5H-pyrano[3,2-d]thiazole-6,7-diol
Molecular Formula: C9H16N2O4S
Molecular Weight: 248.3
SMILES: [H][C@@]12[C@@](N=C(N(CC)[H])S2)([H])[C@@H](O)[C@H](O)[C@@H](CO)O1
Solubility: DMSO: ≥ 45 mg/mL
Target: O-GlcNAcase inhibitor
IC50: 21 nM [1]
Storage: -20°C
CAS 1009816-48-1,Thiamet G
  • Description

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.

  • Spec

Appearance:A crystalline solid

  • References

[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.

price inquiry for CAS:1009816-48-1, Product:Thiamet G