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Thiamet G

Thiamet G
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Purity:99.76%
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Thiamet G

Catalog No. T6056Cas No. 1009816-48-1
Thiamet G is a potent, selective O-GlcNAcase inhibitor with Kiof 21 nM, while exhibiting 37, 000-fold selectivity over human lysosomal –hexosaminidase.
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Pack SizePriceAvailabilityQuantity
2 mg$37In Stock
5 mg$57In Stock
10 mg$94In Stock
25 mg$198In Stock
50 mg$361In Stock
100 mg$537In Stock
500 mg$1,190In Stock
1 mL x 10 mM (in DMSO)$57In Stock
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Product Introduction

Bioactivity
Description
Thiamet G is a potent, selective O-GlcNAcase inhibitor with Kiof 21 nM, while exhibiting 37, 000-fold selectivity over human lysosomal –hexosaminidase.
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. [1] Thiamet G (12.5 nM and 25 nM) significantly enhances p38 phosphorylation by increasing O-GlcNAcylation in mesangial cells. [2] In O-GlcNAc transferase or O-GlcNAcase gain of function cells, thiamet-G restores the assembly of the spindle and partially rescues histone phosphorylation. [3]
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. [1] 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. [4]
Kinase Assay
All enzymatic assays are performed in triplicate at 37°C using 4-methylumbelliferyl N-acetyl-β-d-glucosaminide dehydrate as substrate. 1 nM of purified OGA is incubated with the compounds for 5 min, and then 0.2 mM of the substrate is added. The liberation of 4-methylumbellifery is monitored by kinetic reading at excitation/emission 355/460 nm using a Tecan M200 plate in a mode of 60 s/cycle and 15 cycles in total.
Cell Research
Jurkat cells are seeded at 6000 cells/well in a 96-well plate, and 12 h later, cells are treated with compounds for the indicated time. Cell viability is determined by XTT assay.
AliasTMG
Chemical Properties
Molecular Weight248.3
FormulaC9H16N2O4S
Cas No.1009816-48-1
Storage & Solubility Information
Storage|Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
H2O: 50 mg/mL (201.37 mM), Sonication is recommended.
DMSO: 100 mg/mL (402.74 mM), Sonication is recommended.
Solution Preparation Table
DMSO/H2O
1mg5mg10mg50mg
1 mM4.0274 mL20.1369 mL40.2739 mL201.3693 mL
5 mM0.8055 mL4.0274 mL8.0548 mL40.2739 mL
10 mM0.4027 mL2.0137 mL4.0274 mL20.1369 mL
20 mM0.2014 mL1.0068 mL2.0137 mL10.0685 mL
50 mM0.0805 mL0.4027 mL0.8055 mL4.0274 mL
100 mM0.0403 mL0.2014 mL0.4027 mL2.0137 mL

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