C16

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Description: PKR inhibitor
Chemical Name: 6,8-Dihydro-8-(1H-imidazol-5-ylmethylene)-7H-pyrrolo[2,3-g]benzothiazol-7-one
Purity: ≥98% (HPLC)
Datasheet
Citations (3)
Reviews

Biological Activity for C16

C16 is a 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 for C16

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for C16

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 13.41 50
ethanol 5.37 20

Preparing Stock Solutions for C16

The following data is based on the product molecular weight 268.29. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 7.45 mL 37.27 mL 74.55 mL
2.5 mM 1.49 mL 7.45 mL 14.91 mL
5 mM 0.75 mL 3.73 mL 7.45 mL
25 mM 0.15 mL 0.75 mL 1.49 mL

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References for C16

References are publications that support the biological activity of the product.

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


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Keywords: C16, C16 supplier, Double-stranded, RNA-dependent, proteins, kinases, PKR, inhibitors, inhibits, neuroprotective, neuroprotection, neuroinflammation, Other, Kinases, 5382, Tocris Bioscience

3 Citations for C16

Citations are publications that use Tocris products. Selected citations for C16 include:

Charles et al (2021) Exocyst protein subnetworks integrate Hippo and mTOR signaling to promote virus detection and cancer. Cell Rep 36 109491 PMID: 34348154

Sean P et al (2021) Activating transcription factor-4 promotes neuronal death induced by Parkinson's disease neurotoxins and α-synuclein aggregates. Cell Death Differ 28 1627-1643 PMID: 33277577

Jiang and Steinle (2019) Epac1 inhibits PKR to reduce NLRP3 inflammasome proteins in retinal endothelial cells. J Inflamm Res 12 153 PMID: 31354329


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