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 | 268.29 |
| Formula | C13H8N4OS |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 608512-97-6 |
| PubChem ID | 6490494 |
| InChI Key | VFBGXTUGODTSPK-BAQGIRSFSA-N |
| Smiles | O=C2NC1=CC=C4C(SC=N4)=C1/C2=C/C3=CNC=N3 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 13.41 | 50 | |
| ethanol | 5.37 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 268.29. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.73 mL | 18.64 mL | 37.27 mL |
| 5 mM | 0.75 mL | 3.73 mL | 7.45 mL |
| 10 mM | 0.37 mL | 1.86 mL | 3.73 mL |
| 50 mM | 0.07 mL | 0.37 mL | 0.75 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Jammi et al (2003) Small molecule inhibitors of the RNA-dependent protein kinase. Biochem.Biophys.Res.Comm. 308 50 PMID: 12890478
Ingrand et al (2007) The oxindole/imidazole derivative C16 reduces in vivo brain PKR activation. FEBS Lett. 581 4473 PMID: 17761171
Couturier et al (2011) Prevention of the β-amyloid peptide-induced inflammatory process by inhibition of double-stranded RNA-dependent protein kinase in primary murine mixed co-cultures. J.Neuroinflammation 8 PMID: 21699726
Tronel et al (2014) The specific PKR inhibitor C16 prevents apoptosis and IL-1 beta production in an acute excitotoxic rat model with a neuroinflammatory component. Neurochem.Int. 64 73 PMID: 24211709
Keywords: C16, supplier, Double-stranded, RNA-dependent, proteins, kinases, PKR, inhibitors, inhibits, neuroprotective, neuroprotection, neuroinflammation, Other, Kinases, Other, Kinases, Tocris Bioscience
