PKR-IN-C16

Catalog No.S9668 Batch:S966802

Technical Data

Formula	C₁₃H₈N₄OS
Molecular Weight	268.29	CAS No.	608512-97-6
Solubility (25°C)*	In vitro	DMSO	14 mg/mL (52.18 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

PKR-IN-C16 (imoxin, C16, Imidazolo-oxindole PKR inhibitor C16) is a specific inhibitor of RNA-dependent protein kinase (PKR, Protein Kinase R, EIF2AK2). PKR-IN-C16 prevents apoptosis and IL-1β production in an acute excitotoxic rat model with a neuroinflammatory component.

Targets

PKR ^[1]

IL-1β ^[1]

In vitro

PKR-IN-C16 suppresses proliferation of HCC cells in a dose-dependent manner in vitro. Transcript levels of vascular endothelial growth factor-A and factor-B, platelet-derived growth factor-A and factor-B, fibroblast growth factor-2, epidermal growth factor, and hepatocyte growth factor, which are angiogenesis-related growth factors, are significantly decreased by PKR-IN-C16 in vitro. PKR-IN-C16 blockes tumor cell growth and angiogenesis via a decrease in mRNA levels of several growth factors.^[2]

In vivo

Inflammation is induced by unilateral striatal injection of quinolinic acid (QA) in 10-week-old normotensive rats. The highest dose of C16 (600 μg/kg; C16-2) in QA rats reduces expression of the active catalytic domain of the PKR vs. that in vehicle-injected QA rats. A robust increase of IL-1b levels on the contralateral side of QA rats is prevented by C16-2 (97% inhibition). Macroscopic and microscopic observation of cerebral tissue revealed that tissue integrity is more preserved with C16-2 treatment than its vehicle in QA rats. Furthermore, C16-2 treatment decreases by 47% the neuronal loss and by 37% the number of positive cleaved caspase-3 neurons induced by QA injection. In conclusion, C16 prevents not only the PKR-induced neuronal loss but also the inflammatory response in this acute excitotoxic in vivo model, highlighting its promising neuroprotective properties to rescue acute brain lesions.^[1]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines Huh7 cells Concentrations 500–3000 nM Incubation Time 120 min Method In vitro cell viability is quantified with the MTS assay. Huh7 cells treated with several concentrations (500–3000 nM) of the PKR inhibitor are seeded in 96-well plates at 2 × 10³ cells per well. At each time point, cells are treated with MTS reagent and incubated for 120 min. Absorbance at 450 nm is recorded. Cells treated with DMSO are used as controls. The wells are photographed under the microscope.
Animal Study:^{^[1]}	Animal Models 10-week-old male normotensive male Wistar rats Dosages 60 μg/kg, 600 μg/kg Administration IP

Cell Assay:^{^[2]}

Cell lines
Huh7 cells
Concentrations
500–3000 nM
Incubation Time
120 min
Method
In vitro cell viability is quantified with the MTS assay. Huh7 cells treated with several concentrations (500–3000 nM) of the PKR inhibitor are seeded in 96-well plates at 2 × 10³ cells per well. At each time point, cells are treated with MTS reagent and incubated for 120 min. Absorbance at 450 nm is recorded. Cells treated with DMSO are used as controls. The wells are photographed under the microscope.

Animal Study:^{^[1]}

Animal Models
10-week-old male normotensive male Wistar rats
Dosages
60 μg/kg, 600 μg/kg
Administration
IP

References

Selleck's PKR-IN-C16 has been cited by 4 publications

Nucleus pulposus cells regulate macrophages in degenerated intervertebral discs via the integrated stress response-mediated CCL2/7-CCR2 signaling pathway [ Exp Mol Med, 2024, 56(2):408-421.]	PubMed: 38316963
Sterile inflammation via TRPM8 RNA-dependent TLR3-NF-kB/IRF3 activation promotes antitumor immunity in prostate cancer [ EMBO J, 2024, 43(5):780-805.]	PubMed: 38316991
Exploiting polypharmacology to dissect host kinases and kinase inhibitors that modulate endothelial barrier integrity [ Cell Chem Biol, 2021, S2451-9456(21)00303-2]	PubMed: 34216546
PKR deficiency alleviates pulmonary hypertension via inducing inflammasome adaptor ASC inactivation [ Pulm Circ, 2021, 11(4):20458940211046156]	PubMed: 34540200

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SHIPPING AND STORAGE
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