Thiamet G

製品コードS7213 バッチS721301

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C9H16N2O4S
分子量 248.3 CAS No. 1009816-48-1
Solubility (25°C)* 体外 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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]

プロトコル(参考用のみ)

キナーゼアッセイ Kinetic Analysis with O-GlcNAcase
All assays are carried out in triplicate at 37 °C using para-nitrophenyl β-2-acetamido-2-deoxy-D-glucopyranoside (pNP-GlcNAc) as a substrate in a continuous assay procedure in which the linear rate of liberation of 4-nitrophenolate is monitored by measuring the absorption at 400 nm using a Varian Cary 3E UV-VIS spectrophotometer equipped with a Peltier temperature controller. Reactions (final volume of 50 μL) are initiated by the addition, via syringe, of enzyme (3 μL, 0.27 μg/mL final concentration) and monitored for 5 minutes. Recombinant human O-GlcNAcase is stable in the assay buffer (50 mM NaPi, 100 mM NaCl, 0.1% BSA, pH 7.4) over the time period of the assay. Thiamet G is tested at six concentrations ranging from 0 to 160 nM. The Ki value is determined by linear regression of data from a Dixon plot.
動物実験 動物モデル Healthy Sprague-Dawley rats.
投薬量 200 mg/kg (p.o.), ~50 mg/kg (i.v.)
投与方法 Administrated by p.o. or i.v.

カスタマーフィードバック

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の高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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
Comparative proteomic profiling reveals a pathogenic role for the O-GlcNAcylated AIMP2-PARP1 complex in aging-related hepatic steatosis in mice [ FEBS Lett, 2021, 10.1002/1873-3468.14242] PubMed: 34817071

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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