• 产品描述： PKR-IN-C16 (C16, Imidazolo-oxindole PKR inhibitor C16) 是一种RNA-dependent protein kinase (PKR, Protein Kinase R, EIF2AK2)的特异性抑制剂。PKR-IN-C16 可在具有神经炎症成分的急性兴奋性毒性大鼠模型中阻止凋亡和 IL-1β 的产生

• 靶点： PKR; IL-1β

• 体外研究：
  PKR-IN-C16 suppresses proliferation of HCC cells in a dose-dependent manner in vitro. Transcript levels of vascular endothelial growth factor-A and factor-B, platelet-derived growth factor-A and factor-B, fibroblast growth factor-2, epidermal growth factor, and hepatocyte growth factor, which are angiogenesis-related growth factors, are significantly decreased by PKR-IN-C16 in vitro. PKR-IN-C16 blockes tumor cell growth and angiogenesis via a decrease in mRNA levels of several growth factors

• 体内研究：
  Inflammation is induced by unilateral striatal injection of quinolinic acid (QA) in 10-week-old normotensive rats. The highest dose of C16 (600 μg/kg; C16-2) in QA rats reduces expression of the active catalytic domain of the PKR vs. that in vehicle-injected QA rats. A robust increase of IL-1b levels on the contralateral side of QA rats is prevented by C16-2 (97% inhibition). Macroscopic and microscopic observation of cerebral tissue revealed that tissue integrity is more preserved with C16-2 treatment than its vehicle in QA rats. Furthermore, C16-2 treatment decreases by 47% the neuronal loss and by 37% the number of positive cleaved caspase-3 neurons induced by QA injection. In conclusion, C16 prevents not only the PKR-induced neuronal loss but also the inflammatory response in this acute excitotoxic in vivo model, highlighting its promising neuroprotective properties to rescue acute brain lesions

• 细胞实验： Cell lines: Huh7 cells Concentrations: 500–3000 nM Incubation Time: 120 min Method: In vitro cell viability is quantified with the MTS assay. Huh7 cells treated with several concentrations (500–3000  nM) of the PKR inhibitor are seeded in 96-well plates at 2 × 103 cells per well. At each time point, cells are treated with MTS reagent and incubated for 120 min. Absorbance at 450 nm is recorded. Cells treated with DMSO are used as controls. The wells are photographed under the microscope.

• 动物实验： Animal Models: 10-week-old male normotensive male Wistar rats Dosages: 60 μg/kg, 600 μg/kg Administration: IP

• 参考文献：
  1. C Tronel, et al. The specific PKR inhibitor C16 prevents apoptosis and IL-1β production in an acute excitotoxic rat model with a neuroinflammatory component. Neurochem Int. 2014 Jan;64:73-83. 2. Takao Watanabe, et al. Therapeutic effects of the PKR inhibitor C16 suppressing tumor proliferation and angiogenesis in hepatocellular carcinoma in vitro and in vivo. Sci Rep. 2020 Mar 20;10(1):5133.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.727 ml	18.637 ml	37.273 ml
  5 mM	0.745 ml	3.727 ml	7.455 ml
  10 mM	0.373 ml	1.864 ml	3.727 ml
  50 mM	0.075 ml	0.373 ml	0.745 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *