BIO-acetoxime

製品コードS7915 バッチS791501

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 (warmed with 50ºC water bath) 19 mg/mL (47.71 mM)
Water Insoluble
Ethanol Insoluble
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 BIO-acetoxime (GSK-3 Inhibitor X) は、強力なデュアルGSK3α/β阻害剤であり、IC50は10 nMで、CDK5/p25、CDK2/サイクリンA、CDK1/サイクリンBに対して240倍以上の選択性を示します。
in vitro In human oral epithelial cells, BIO-acetoxime suppresses viral gene expression and protects oral epithelial cells from HSV-1 infection. In SY5Y-MYCN cells, this compound strongly reduces c-MYC expression and p-SMAD3 levels. It also decreases cell viability of KCN, KCNR, SY5Y, Kelly, and IMR32 cells by mediating apoptosis. In HEK 293T cells, this chemical is also found to reduce antiviral innate immunity downstream of IRF3 activation by inhibition of GSK3α/β activities.

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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/14761195/
  • https://pubmed.ncbi.nlm.nih.gov/23392633/
  • https://pubmed.ncbi.nlm.nih.gov/24282277/
  • https://pubmed.ncbi.nlm.nih.gov/26100021/

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：

Deferasirox Causes Leukaemia Cell Death through Nrf2-Induced Ferroptosis [ Antioxidants (Basel), 2024, 13(4)424] PubMed: 38671872
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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