PKR Inhibitor

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 alpha (eIF2alpha), blocking translation and driving apoptosis. 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 eIF2alpha in the brain. Similar administration in mice enhances long-term memory storage, including contextual and auditory long-term fear memories.Formal Name: 6,8-dihydro-8-(1H-imidazol-5-ylmethylene)-7H-pyrrolo[2,3-g]benzothiazol-7-one. CAS Number: 608512-97-6. Synonyms: C16, GW 506033X, Protein Kinase RNA-activated. Molecular Formula: C13H8N4OS. Formula Weight: 268.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.5 mg/ml, DMSO: 2.5 mg/ml, DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml. lambdamax: 244, 305, 363 nm. SMILES: O=C1NC2=CC=C3C(SC=N3)=C2/C1=C/C4=CNC=N4. InChi Code: InChI=1S/C13H8N4OS/c18-13-8(3-7-4-14-5-15-7)11-9(17-13)1-2-10-12(11)19-6-16-10/h1-6H,(H,14,15)(H,17,18)/b8-3-. InChi Key: VFBGXTUGODTSPK-BAQGIRSFSA-N.