Binds the ATP-binding site of PKR and blocks autophosphorylation (IC50 = 186-210 nM); protects neuroblastoma cells against cell damage triggered by ER stress; prevents phosphorylation of FADD

PKR Inhibitor – 25 mg

Brand:
Cayman
CAS:
608512-97-6
Storage:
-20
UN-No:
Non-Hazardous - /

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 α (eIF2α), 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 eIF2α in the brain.{25320} Similar administration in mice enhances long-term memory storage, including contextual and auditory long-term fear memories.{25322}  

 

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Description

Binds the ATP-binding site of PKR and blocks autophosphorylation (IC50 = 186-210 nM); protects neuroblastoma cells against cell damage triggered by ER stress; prevents phosphorylation of FADD, preventing apoptosis; reduces phosphorylation of PKR and eIF2α in the brain, enhancing long-term memory storage

Formal name: 6,8-dihydro-8-(1H-imidazol-5-ylmethylene)-7H-pyrrolo[2,3-g]benzothiazol-7-one

Synonyms:  C16|GW 506033X|Protein Kinase RNA-activated

Molecular weight: 268.3

CAS: 608512-97-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory

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