Thiamet G

Catalog No.S7213 Batch:S721301

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Technical Data

Formula

C9H16N2O4S
Molecular Weight 248.3 CAS No. 1009816-48-1
Solubility (25°C)* In vitro DMSO 50 mg/mL (201.36 mM)
Water 50 mg/mL (201.36 mM)
Ethanol 12 mg/mL (48.32 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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]

Protocol (from reference)

Animal Study:[1]
  • 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.

Customer Product Validation

Data from [Data independently produced by Biochem Biophys Res Commun, 2014, 453(3), 392-7]

Data from [Data independently produced by , , Biomedicine & Pharmacotherapy, 2017, (91):731-738]

Selleck's Thiamet G has been cited by 14 publications

Tissue-specific O-GlcNAcylation profiling identifies substrates in translational machinery in Drosophila mushroom body contributing to olfactory learning [ Elife, 2024, 13e91269] PubMed: 38619103
Bisphenol A induces non-alcoholic fatty liver disease by promoting the O-GlcNAcylation of NLRP3 [ Arch Physiol Biochem, 2023, 1-9.] PubMed: 38038745
FOXA1 O-GlcNAcylation-mediated transcriptional switch governs metastasis capacity in breast cancer [ Sci Adv, 2023, 9(33):eadg7112] PubMed: 37595040
FOXA1 O-GlcNAcylation-mediated transcriptional switch governs metastasis capacity in breast cancer [ Sci Adv, 2023, 9(33):eadg7112] PubMed: 37595040
Increased glucose metabolism in TAMs fuels O-GlcNAcylation of lysosomal Cathepsin B to promote cancer metastasis and chemoresistance [ Cancer Cell, 2022, 40(10):1207-1222.e10] PubMed: 36084651
O-GlcNAcylation and stablization of SIRT7 promote pancreatic cancer progression by blocking the SIRT7-REGγ interaction [ Cell Death Differ, 2022, 10.1038/s41418-022-00984-3] PubMed: 35422493
O-GlcNAcylation of ZEB1 facilitated mesenchymal pancreatic cancer cell ferroptosis [ Int J Biol Sci, 2022, 18(10):4135-4150] PubMed: 35844792
Writing and Erasing O-GlcNAc on Casein Kinase 2 Alpha Alters the Phosphoproteome [ ACS Chem Biol, 2022, 17(5):1111-1121] PubMed: 35467332
Quantitative chemoproteomics reveals O-GlcNAcylation of cystathionine γ-lyase (CSE) represses trophoblast syncytialization [ Cell Chem Biol, 2021, 28(6):788-801.e5] PubMed: 33626323
O-GlcNAc modified-TIP60/KAT5 is required for PCK1 deficiency-induced HCC metastasis [ Oncogene, 2021, 10.1038/s41388-021-02058-z] PubMed: 34650217

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.