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Thiamet G

Thiamet G is a potent, selective O-GlcNAcase inhibitor with Kiof 21 nM, while exhibiting 37,000-fold selectivity over human lysosomal –hexosaminidase.

Thiamet G Chemical Structure

Thiamet G Chemical Structure

CAS: 1009816-48-1

Selleck's Thiamet G has been cited by 12 Publications

2 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Biological Activity

Description Thiamet G is a potent, selective O-GlcNAcase inhibitor with Kiof 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 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]
Experimental Result Images Methods Biomarkers Images PMID
Immunofluorescence Iba-1 / CD16/32 CD206 27864466
In Vivo
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]
Animal Research Animal Models Healthy Sprague-Dawley rats.
Dosages 200 mg/kg (p.o.), ~50 mg/kg (i.v.)
Administration Administrated by p.o. or i.v.

Chemical Information & Solubility

Molecular Weight 248.3 Formula

C9H16N2O4S
CAS No. 1009816-48-1 SDF Download Thiamet G SDF
Smiles CCN=C1NC2C(C(C(OC2S1)CO)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 50 mg/mL ( (201.36 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 50 mg/mL

Ethanol : 6 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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