PKR-IN-C16

For research use only.

Catalog No.S9668 Synonyms: imoxin, C16, Imidazolo-oxindole PKR inhibitor C16

2 publications

PKR-IN-C16 Chemical Structure

CAS No. 608512-97-6

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.

Selleck's PKR-IN-C16 has been cited by 2 publications

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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

Cell Research:

[2]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: 10-week-old male normotensive male Wistar rats
  • Dosages: 60 μg/kg, 600 μg/kg
  • Administration: IP
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 13 mg/mL (48.45 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 268.29
Formula

C13H8N4OS

CAS No. 608512-97-6
Storage powder
in solvent
Synonyms imoxin, C16, Imidazolo-oxindole PKR inhibitor C16
Smiles C1=CC2=C(C3=C1NC(=O)C3=CC4=CN=CN4)SC=N2

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04716452 Not yet recruiting Drug: Ceramide NanoLiposome (Ceraxa) Acute Myeloid Leukemia in Relapse|Acute Myeloid Leukemia Refractory Keystone Nano Inc|University of Virginia|Memorial Sloan Kettering Cancer Center|Milton S. Hershey Medical Center February 15 2021 Phase 1
NCT04832217 Completed Other: Pyrenees´ Beef diet Body Weight Changes|Habits Diet|Habit Food|Life Change Events Universidad de Zaragoza January 20 2019 Not Applicable
NCT03691402 Active not recruiting Behavioral: MCT-Silver|Behavioral: Cognitive Remediation Depression Universitätsklinikum Hamburg-Eppendorf November 18 2018 Not Applicable
NCT03937115 Unknown status Device: Active tDCS|Device: Sham tDCS Healthy Volunteers|High-level Sportsman Centre Hospitalier Universitaire de Besancon November 21 2018 Not Applicable
NCT03327402 Completed Drug: SHP465 Attention Deficit Hyperactivity Disorder (ADHD) Shire|Takeda March 13 2018 Phase 1
NCT03196219 Completed Drug: C16G2|Other: Placebo Dental Caries Armata Pharmaceuticals Inc. July 7 2017 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID