|PKR Inhibitor 目录号 GC17925|
Sample solution is provided at 25 µL, 10mM.
|别名||C16,GW 506033X,Protein Kinase RNA-activated|
|溶解度||≤2.5mg/ml in DMSO;0.5mg/ml in dimethyl formamide||储存条件||Store at -20°C|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
The activity of double-stranded RNA-activated protein kinase (PKR) is altered by viral infection as well as by various neuropathologies., 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. PKR Inhibitor protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress. It also prevents phosphorylation of Fas-associated protein with a death domain (FADD) in neuroblastoma cells, preventing FADD-dependent activation of caspases and apoptosis. Intraperitoneal administration of PKR inhibitor in rats reduces phosphorylation of PKR and eIF2α in the brain. Similar administration in mice enhances long-term memory storage, including contextual and auditory long-term fear memories.
. 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. J. Biol. Chem. 285(2), 1272-1282 (2010).
. 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).
. 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).
. 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).
. 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).