An inhibitor of double-stranded RNA-activated protein kinase
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PKR Inhibitor

Item No. 15323

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 0.5 mg/mlDMSO: 2.5 mg/mlDMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    Product Description

    The activity of double-stranded RNA-activated protein kinase (PKR) is altered by viral infection as well as by various neuropathologies.1,2 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.3 PKR Inhibitor protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress.4 It also prevents phosphorylation of Fas-associated protein with a death domain (FADD) in neuroblastoma cells, preventing FADD-dependent activation of caspases and apoptosis.1 Intraperitoneal administration of PKR inhibitor in rats reduces phosphorylation of PKR and eIF2α in the brain.5 Similar administration in mice enhances long-term memory storage, including contextual and auditory long-term fear memories.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. 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. The Journal of Biological Chemisty 285(2), 1272-1282 (2010).

    2. 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).

    3. Jammi, N.V., Whitby, L.R., and Beal, P.A. Small molecule inhibitors of the RNA-dependent protein kinase. Biochem. Biophys. Res. Commun. 308(1), 50-57 (2003).

    4. Shimazawa, M., and Hara, H. Inhibitor of double stranded RNA-dependent protein kinase protects against cell damage induced by ER stress. Neurosci. Lett. 409(3), 192-195 (2006).

    5. Ingrand, S., Barrier, L., Lafay-Chebassier, C., et al. The oxindole/imidazole derivative C16 reduces in vivo brain PKR activation. FEBS Lett. 581(23), 4473-4478 (2007).