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Thiamet G

Catalog No. T6056   CAS 1009816-48-1
Synonyms: TMG

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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Thiamet G Chemical Structure
Thiamet G, CAS 1009816-48-1
Pack Size Availability Price/USD Quantity
2 mg In stock $ 37.00
5 mg In stock $ 57.00
10 mg In stock $ 94.00
25 mg In stock $ 198.00
50 mg In stock $ 361.00
100 mg In stock $ 537.00
500 mg In stock $ 1,190.00
1 mL * 10 mM (in DMSO) In stock $ 57.00
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Purity: 99.76%
Purity: 99.74%
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Biological Description
Chemical Properties
Storage & Solubility Information
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&IC50 O-GlcNAcase: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. [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.
Synonyms TMG
Molecular Weight 248.3
Formula C9H16N2O4S
CAS No. 1009816-48-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 12.4 mg/mL (50 mM)

TargetMolReferences and Literature

1. Yuzwa SA, et al. Nat Chem Biol. 2008, 4(8), 483-490. 2. Goldberg H, et al. Am J Physiol Endocrinol Metab. 2011, 301(4), E713-726. 3. Tan EP, et al. J Biol Chem. 2013, 288(38), 27085-27099. 4. Andrés-Bergós J, et al. J Biol Chem. 2012 Sep 28;287(40):33615-28.

TargetMolCitations

1. Liu R, Liu Y, Zhang W, et al.PCK1 attenuates tumor stemness via activating the Hippo signaling pathway in hepatocellular carcinoma.Genes & Diseases.2023: 101114.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Bioactive Compound Library Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library Bioactive Lipid Compound Library Anti-Aging Compound Library Autophagy Compound Library

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Keywords

Thiamet G 1009816-48-1 Autophagy Others Inhibitor TMG inhibit inhibitor

 

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