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Thiamet G

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Catalog No. T6056Cas No. 1009816-48-1
Alias TMG

Thiamet G is a potent O-GlcNAcase inhibitor (Ki=20 nM) with selectivity. The role of O-GlcNAcase is to remove O-GlcNAc from the modified protein.

Thiamet G

Thiamet G

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Purity: 99.98%
Catalog No. T6056Alias TMGCas No. 1009816-48-1
Thiamet G is a potent O-GlcNAcase inhibitor (Ki=20 nM) with selectivity. The role of O-GlcNAcase is to remove O-GlcNAc from the modified protein.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$37In StockIn Stock
5 mg$57In StockIn Stock
10 mg$94In StockIn Stock
25 mg$198In StockIn Stock
50 mg$361In StockIn Stock
100 mg$537In StockIn Stock
500 mg$1,190-In Stock
1 mL x 10 mM (in DMSO)$57In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.98%
Color:White
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Product Introduction

Bioactivity
Description
Thiamet G is a potent O-GlcNAcase inhibitor (Ki=20 nM) with selectivity. The role of O-GlcNAcase is to remove O-GlcNAc from the modified protein.
Targets&IC50
O-GlcNAcase (OGA):21 nM (Ki), O-GlcNAcase (OGA):30 nM (EC50), O-GlcNAcase (OGA, human):20 nM (Ki)
In vitro
METHODS: PC-12 cells were treated with Thiamet G (1 nM-250 μM), and the level of O-GlcNAcase was detected by Western Blot. After PC-12 cells were treated with Thiamet G (100 mM), the level of O-GlcNAcase was detected by Western Blot.
RESULTS: Thiamet G inhibited O-GlcNAcase in PC-12 cells in a dose - and time-dependent manner and reduced the phosphorylation level of tau protein. [1]
METHODS: Mesangial cells were treated with Thiamet G (12.5, 25 nM), and the O-GlcNAcylation level and p38 phosphorylation level were detected by Western Blot.
RESULTS: Thiamet G significantly enhances p38 phosphorylation in glomerular cell lines by increasing O-GlcNAcylation. [2]
In vivo
METHODS: To study the neuroprotective effect of Thiamet G, Thiamet G (20 mg/kg) was intraperitoneally injected into mice for 3 consecutive days.
RESULTS: Thiamet G exhibited neuroprotective effects by inhibiting O-GlcNAcase. [3]
METHODS: To study the antiepileptic effect of Thiamet G, Thiamet G (10 mg/kg) was intraperitoneally injected into an epileptic rat model once a day for three consecutive days.
RESULTS: Thiamet G significantly reduced the duration of epileptic seizures and the frequency of interictal spikes. [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.
SynonymsTMG
Chemical Properties
Molecular Weight248.3
FormulaC9H16N2O4S
Cas No.1009816-48-1
Smiles[H][C@]12O[C@H](CO)[C@@H](O)[C@H](O)[C@@]1([H])N=C(NCC)S2
Relative Density.1.74 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
H2O: 50 mg/mL (201.37 mM), Sonication is recommended.
DMSO: 100 mg/mL (402.74 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (16.11 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
H2O/DMSO
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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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