BIO-acetoxime

製品コードS7915 バッチS791502

印刷

化学情報

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

C18H12BrN3O3
分子量 398.21 CAS No. 667463-85-6
Solubility (25°C)* 体外 DMSO 39 mg/mL warmed with 50ºC water bath (97.93 mM)
Water Insoluble
Ethanol Insoluble
* <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 BIO-acetoxime (GSK-3 Inhibitor X) is a potent dual GSK3α/β inhibitor with IC50 of 10 nM, >240-fold selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B.
in vitro In human oral epithelial cells, BIO-acetoxime suppresses viral gene expression and protects oral epithelial cells from HSV-1 infection. [2] In SY5Y-MYCN cells, BIO-acetoxime strongly reduces c-MYC expression and p-SMAD3 levels. BIO-acetoxime also decreases cell viability of KCN, KCNR, SY5Y, Kelly, and IMR32 cells by mediating apoptosis. [3] In HEK 293T cells, BIO-acetoxime is also found to reduce antiviral innate immunity downstream of IRF3 activation by inhibition of GSK3α/β activities. [4]

プロトコル(参考用のみ)

キナーゼアッセイ Kinase Assays
Kinases activities are assayed in Buffer A or C, at 30 °C, at a final ATP concentration of 15 μM. Blank values are subtracted and activities calculated as pmoles of phosphate incorporated for a 10 min incubation. The activities are expressed in % of the maximal activity, i.e., in the absence of inhibitors. Controls are performed with appropriate dilutions of DMSO. GSK-3α/β is purified from porcine brain by affinity chromatography on immobilized axin. It is assayed, following a 1/100 dilution in 1 mg BSA/mL 10 mM DTT, with 5 μL 40 μM GS-1 peptide as a substrate, in buffer A, in the presence of 15 μM [γ-33P] ATP (3000 Ci/mmol; 1 mCi/mL) in a final volume of 30 μL. After 30 min incubation at 30 °C, 25 μL aliquots of supernatant are spotted onto 2.5 × 3 cm pieces of Whatman P81 phosphocellulose paper, and, 20 s later, the filters are washed five times (for at least 5 min each time) in a solution of 10 mL phosphoric acid/liter of water. The wet filters are counted in the presence of 1 mL of ACS scintillation fluid. CDK1/cyclin B is extracted in homogenization buffer from M phase starfish (Marthasterias glacialis) oocytes and purified by affinity chromatography on p9CKShs1-sepharose beads, from which it is eluted by free p9CKShs1. The kinase activity is assayed in buffer C, with 1 mg histone H1 /mL, in the presence of 15 μM [γ-32P] ATP (3000 Ci/mmol; 1 mCi/mL) in a final volume of 30 μL. After 10 min incubation at 30 °C, 25 μL aliquots of supernatant are spotted onto P81 phosphocellulose papers and treated as described above. CDK5/p25 is reconstituted by mixing equal amounts of recombinant mammalian CDK5 and p25 expressed in E. coli as GST (Glutathione-S-transferase) fusion proteins and purified by affinity chromatography on glutathione-agarose (p25 is a truncated version of p35, the 35 kDa CDK5 activator). Its activity is assayed in buffer C as described for CDK1/cyclin B.0
細胞アッセイ 細胞株 KCN, KCNR, SY5Y, Kelly, and IMR32 cells
濃度 ~1 μM
反応時間 72 h
実験の流れ Cell viability is analyzed by CellTiter 96 AQueous One Solution Cell Proliferation Assay according to manufacturer's instructions, approximately 5,000 cells are plated per well of 96-well tissue culture plates with 100 μL of medium. To assess cell viability, rather than proliferation rate, inhibitor- and control-treated cells are assayed after the same growth time had elapsed. The results represent the mean ± SD of triplicate samples, expressed as a percentage of control.

カスタマーフィードバック

Data from [Data independently produced by , , Journal of Functional Foods, 2017, 31:217-228]

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：

Synthetic Lethality of Combined Bcl-2 Inhibition and p53 Activation in AML: Mechanisms and Superior Antileukemic Efficacy. [ Cancer Cell, 2017, 32(6):748-760] PubMed: 29232553
Carnosic acid alleviates hyperlipidemia and insulin resistance by promoting the degradation of SREBPs via the 26S proteasome [ZhishenXie, et al. J Funct Foods, 2017, 10.1016/j.jff.2017.01.040]
Carnosic acid alleviates hyperlipidemia and insulin resistance by promoting the degradation of SREBPs via the 26S proteasome [ Journal of Functional Foods, 2017, 31:217-228] PubMed: None
Overexpression of Suprabasin is Associated with Proliferation and Tumorigenicity of Esophageal Squamous Cell Carcinoma [ Sci Rep, 2016, 6:21549] PubMed: 26899563

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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