Chemical Name: 6,8-Dihydro-8-(1H-imidazol-5-ylmethylene)-7H-pyrrolo[2,3-g]benzothiazol-7-one
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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
Certificate of Analysis / Product Datasheet
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References
References are publications that support the products' biological activity.
Jammiet al (2003) Small molecule inhibitors of the RNA-dependent protein kinase. Biochem.Biophys.Res.Comm. 308 50 PMID: 12890478
Ingrandet al (2007) The oxindole/imidazole derivative C16 reduces in vivo brain PKR activation. FEBS Lett. 581 4473 PMID: 17761171
Couturieret 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
Tronelet 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