Thiamet G

製品コードS7213 バッチS721302

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 6 mg/mL (24.16 mM)
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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. This compound (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] It (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, this compound 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. This compound is also orally bioavailable. [1] O-GlcNAc accumulation induced by this chemical 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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/18587388/
  • https://pubmed.ncbi.nlm.nih.gov/21712532/
  • https://pubmed.ncbi.nlm.nih.gov/23946484/
  • https://pubmed.ncbi.nlm.nih.gov/22859309/

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：

FBXO31-mediated ubiquitination of OGT maintains O-GlcNAcylation homeostasis to restrain endometrial malignancy [ Nat Commun, 2025, 16(1):1274] PubMed: 39894887
Renal tubular GSDME protects cisplatin nephrotoxicity by impeding OGT-STAT3-S100A7A axis in male mice [ Nat Commun, 2025, 16(1):6807] PubMed: 40707439
O-GlcNAc modulation of nuclear pore complexes orchestrates mRNA export efficiency [ Proc Natl Acad Sci U S A, 2025, 122(32):e2502687122] PubMed: 40773237
Upregulation of protein O-GlcNAcylation levels promotes zebrafish fin regeneration [ Mol Cell Proteomics, 2025, S1535-9476(25)00034-9] PubMed: 40044042
O-GlcNAc-modified HOXA9 suppresses ferroptosis via promoting UBR5-mediated SIRT6 degradation in nasopharyngeal carcinoma [ Neoplasia, 2025, 62:101142] PubMed: 40081214
O-GlcNAcylation Facilitates the Interaction between Keratin 18 and Isocitrate Dehydrogenases and Potentially Influencing Cholangiocarcinoma Progression [ ACS Cent Sci, 2024, 10(5):1065-1083] PubMed: 38799671
FOXP1 phosphorylation antagonizes its O-GlcNAcylation in regulating ATR activation in response to replication stress [ EMBO J, 2024, 44(2):457-483.] PubMed: 39623140
Tissue-specific O-GlcNAcylation profiling identifies substrates in translational machinery in Drosophila mushroom body contributing to olfactory learning [ Elife, 2024, 13e91269] PubMed: 38619103
KDM2B regulates stroke injury by modulating OGT-mediated 0-GlcNAcylation of SLC7A11 [ Commun Biol, 2024, 7(1):1530] PubMed: 39558086
Bisphenol A induces non-alcoholic fatty liver disease by promoting the O-GlcNAcylation of NLRP3 [ Arch Physiol Biochem, 2023, 1-9.] PubMed: 38038745

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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