Cayman 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 α (eIF2α), 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 eIF2α in the brain. Similar administration in mice enhances long-term memory storage, including contextual and auditory long-term fear memories.

WARNING This product is not for human or veterinary use.