product name Thiamet G
Description: Thiamet G is a potent, selective O-GlcNAcase inhibitor with Ki of 21 nM, it displayed 37,000-fold selectivity over human lysosomal–hexosaminidase. 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.
References: Nat Chem Biol. 2008 Aug;4(8):483-90; Am J Physiol Endocrinol Metab. 2011 Oct;301(4):E713-26.
248.3
Formula
C9H16N2O4S
CAS No.
1009816-48-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 50 mg/mL (201.4 mM)
Water: 50 mg/mL (201.4 mM)
Ethanol: 12 mg/mL (48.3 mM)
Solubility (In vivo)
Saline: 30 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: In NGF-differentiated PC-12 cells, inhibition of O-GlcNAcase by Thiamet G increases the cellular levels of O-GlcNAc with EC50 of approximately 30 nM. Thiamet G (100 mM) reduces tau phosphorylation by approximately 2.1-fold, 2.7-fold, 1.2-fold and 1.3-fold for Ser396, Thr231, Ser422 and Ser262, respectively. Thiamet G (12.5 nM and 25 nM) significantly enhances p38 phosphorylation by increasing O-GlcNAcylation in mesangial cells. In O-GlcNAc transferase or O-GlcNAcase gain of function cells, thiamet-G restores the assembly of the spindle and partially rescues histone phosphorylation. Kinase Assay: Cell Assay: 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. |
|---|---|
| In Vivo | In rats, thiamet G (50 mg/kg) administrated by i.v. crosses the blood brain barrier and then results in increase in brain O-GlcNAc levels in a dose- and time-dependent manner, and reduction of tau phosphorylation in rat brain. Thiamet G is also orally bioavailable. O-GlcNAc accumulation induced by thiamet G stimulates chondrogenic differentiation in C57/bl mice by increasing the gene expression of differentiation markers, as well as the activity of MMP-2 and -9. |
| Animal model | Healthy Sprague-Dawley rats. |
| Formulation & Dosage | Dissolved in water; Healthy Sprague-Dawley rats.; p.o. or i.v. |
| References | Nat Chem Biol. 2008 Aug;4(8):483-90; Am J Physiol Endocrinol Metab. 2011 Oct;301(4):E713-26; J Biol Chem. 2012 Sep 28;287(40):33615-28. |
