PKR Inhibitor

Territorial Availability: Available through Bertin Technologies only in France

• Synonyms
  • 6,8-dihydro-8-(1H-imidazol-5-ylmethylene)-7H-pyrrolo[2,3-g]benzothiazol-7-one
• Correlated keywords
  • 1159885-47-8 nootropics apoptosis neurosciences inhibitors inhibits inhibitions proteins kinases PKRs oxindole imidazole derivatives ATP autophosphorylation neuroblastoma cells FADD fas associated Fas-associated protein death domains caspases long-term long term memory storage contextual auditory fear memories GWs 506033X GW506033X GW-506033X PXRi double-stranded double stranded RNA-activated RNAs activated viral infections neuropathologies primary phosphorylation targets eukaryotic initiation factors 2 two subunit .alpha. alpha ? eIF2? eIF2alpha eIF2.alpha. eIF2-alpha blocking blocks translation apoptosis ATP-binding site binding sites humans damages tunicamycin-mediated tunicamycin endoplasmic reticulum stress prevents protects intraperitoneal administrations rats brains mice
• Product Overview:
  The activity of double-stranded RNA-activated protein kinase (PKR) is altered by viral infection as well as by various neuropathologies.{25319,25322} A primary phosphorylation target of PKR is eukaryotic initiation factor 2 subunit ? (eIF2?), blocking translation and driving apoptosis.{25323} 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.{25323} PKR Inhibitor protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress.{25321} It also prevents phosphorylation of Fas-associated protein with a death domain (FADD) in neuroblastoma cells, preventing FADD-dependent activation of caspases and apoptosis.{25319} Intraperitoneal administration of PKR inhibitor in rats reduces phosphorylation of PKR and eIF2? in the brain.{25320} Similar administration in mice enhances long-term memory storage, including contextual and auditory long-term fear memories.{25322}