[CAS NO. 1009816-48-1] Thiamet G
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PRODUCTS SPECIFICATIONS [1009816-48-1]
Catalog
SLK-S7213
Brand
Selleck
CAS
1009816-48-1
DESCRIPTION [1009816-48-1]
Overview
| MDL | MFCD15144964 |
|---|---|
| Molecular Weight | 248.3 |
| Molecular Formula | C9H16N2O4S |
| SMILES | O[C@H]1[C@H](O)[C@@]2([H])N=C(NCC)S[C@@]2([H])O[C@@H]1CO |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0274 mL | 20.1369 mL | 40.2739 mL |
| 5 mM | 0.8055 mL | 4.0274 mL | 8.0548 mL |
| 10 mM | 0.4027 mL | 2.0137 mL | 4.0274 mL |
| 50 mM | 0.0805 mL | 0.4027 mL | 0.8055 mL |
Description
Thiamet G is a potent, selective inhibitor with of 21 nM, while exhibiting 37,000-fold selectivity over human lysosomal –hexosaminidase.
Targets
| O-GlcNAcase [1] (cell-free assay) |
| 21 nM(Ki) |
In vitro
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.
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.
References
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