| 货号 | 15323-1mg |
| 描述 | The activity of double-stranded RNA-activated protein kinase (PKR) is altered by viral infection as well as by various neuropathologies.1,2 A primary phosphorylation target of PKR is eukaryotic initiation factor 2 subunit α (eIF2α), blocking translation and driving apoptosis.3 PKR Inhibitor is an oxindole/imidazole derivative that binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM.3 PKR Inhibitor protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress.4 It also prevents phosphorylation of Fas-associated protein with a death domain (FADD) in neuroblastoma cells, preventing FADD-dependent activation of caspases and apoptosis.1 Intraperitoneal administration of PKR inhibitor in rats reduces phosphorylation of PKR and eIF2α in the brain.5 Similar administration in mice enhances long-term memory storage, including contextual and auditory long-term fear memories.2 |
| 别名 | C16;GW 506033X;Protein Kinase RNA-activated; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Couturier, J.,Morel, M.,Pontcharraud, R., et al. Interaction of double-stranded RNA-dependent protein kinase (PKR) with the death receptor signaling pathway in amyloid β (Aβ)-treated cells and in APPSLPS1 knock-in mice. The Journal of Biological Chemisty 285(2), 1272-1282 (2010). 2.Zhu, P.J.,Huang, W.,Kalikulov, D., et al. Suppression of PKR promotes network excitability and enhanced cognition by interferon-γ-mediated disinhibition. Cell 147(6), 1384-1396 (2011). 3.Jammi, N.V.,Whitby, L.R. and Beal, P.A. Small molecule inhibitors of the RNA-dependent protein kinase. Biochemical and Biophysical Research Communications 308(1), 50-57 (2003). 4.Shimazawa, M. and Hara, H. Inhibitor of double stranded RNA-dependent protein kinase protects against cell damage induced by ER stress. Neuroscience Letters 409(3), 192-195 (2006). 5.Ingrand, S.,Barrier, L.,Lafay-Chebassier, C., et al. The oxindole/imidazole derivative C16 reduces in vivo brain PKR activation. FEBS Letters 581(23), 4473-4478 (2007). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 268.3 |
| 分子式 | C13H8N4OS |
| CAS号 | 608512-97-6 |
| 稳定性 | ≥ 2 years |
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