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Stock availabilitIn Stock
In Stock
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CAS number
608512-97-6
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Description
PKR kinase inhibitor
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Molecular weight
268,3 g/mol
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Primary research fields
Cell Signaling, Cancer, Apoptosis, Cancer Growth Inhibitors, Tyrosine Kinase Inhibitors
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Other name
Imidazolo-oxindole PKR inhibitor C16, 6,8-Dihydro-8-(1H-imidazol-5-ylmethylene)-7H-pyrrolo[2,3-g]benzothiazol-7-one
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Product category
Small Molecules
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Product type
Inhibitor
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Chemical formula
C13H8N4OS
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Origin
Synthetic
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Purity pourcentage
≥98% (HPLC)
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Soluble in
Soluble in DMSO 12 mg/ml
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Physical appearance
Solid
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Storage recommendations
-20ºC
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Shipping recommendations
Shipped Ambient
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Safety information
Classification: Chronic aquatic toxicity (Category 4), H413 Safety Phrases: S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. Hazard statements: H413 May cause long lasting harmful effects to aquatic life. Precautionary statements: P273 Avoid release to the environment. P501 Dispose of contents/ container to an approved waste disposal plant.
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PubChem number
67016828
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Scientific context
C16 is a derivative of imidazolo-oxindole and inhibits RNA-dependent protein kinases (PKR). Its inhibition effect on PKR is ATP-binding site directed. C16 has been shown to specifically inhibit the apoptotic PKR/eIF2a signaling pathway.
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Bibliography
1. Couturier J., et al. (2010) J. Biol. Chem. 285(2): 1272–1282. 2. Jammi N.V., Whitby L.R., & Beal P.A. (2003) Biochem. Biophys.Res. Comm. 308(1):50–57.
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Release date
1-Oct-2014
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PubMed number
Refer to PubMed
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Tested applications
To be tested
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Tested reactivity
To be tested
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Representative figure legend
Chemical structure of C16 (SIH-498), a PKR kinase inhibitor. CAS #: 608512-97-6. Molecular Formula: C13H8N4OS. Molecular Weight: 268.3 g/mol. Chemical structure of C16, a PKR kinase inhibitor (SIH-498). CAS # 608512-97-6. Molecular Formula: C13H8N4OS.
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Warning information
Non-hazardous
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Country of production
Canada
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Total weight kg
0.25
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Net weight g
0.025
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Additional description
Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.
