Catalog Number: 5382
Chemical Name: 6,8-Dihydro-8-(1H-imidazol-5-ylmethylene)-7H-pyrrolo[2,3-g]benzothiazol-7-one
Biological Activity
PKR inhibitor (IC50 = 210 nM). Rescues PKR-dependent translation block in vitro. Decreases Aβ42-induced inflammatory cytokine release and apoptosis in neuronal cultures. Prevents neuroinflammation and neuronal loss in an acute excitotoxic rat model. Brain penetrant.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 50 mM in DMSO and to 20 mM in ethanol
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Small molecule inhibitors of the RNA-dependent protein kinase.
    Jammi et al.
    Biochem.Biophys.Res.Comm., 2003;308:50
  2. The oxindole/imidazole derivative C16 reduces in vivo brain PKR activation.
    Ingrand et al.
    FEBS Lett., 2007;581:4473
  3. Prevention of the β-amyloid peptide-induced inflammatory process by inhibition of double-stranded RNA-dependent protein kinase in primary murine mixed co-cultures.
    Couturier et al.
    J.Neuroinflammation, 2011;8
  4. The specific PKR inhibitor C16 prevents apoptosis and IL-1� production in an acute excitotoxic rat model with a neuroinflammatory component.
    Tronel et al.
    Neurochem.Int., 2014;64:73
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