Home ER stress & UPR PKR inhibitor - Apoptosis related inhibitor - Interleukins inhibitor - eIF inhibitor PKR-IN-C16 For research use only.

PKR-IN-C16

Synonyms: imoxin, C16, Imidazolo-oxindole PKR inhibitor C16

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.

PKR-IN-C16 Chemical Structure

PKR-IN-C16 Chemical Structure

CAS No. 608512-97-6

Purity & Quality Control

PKR-IN-C16 Related Products

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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models 10-week-old male normotensive male Wistar rats
Dosages 60 μg/kg, 600 μg/kg
Administration IP
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04716452 Not yet recruiting
Acute Myeloid Leukemia in Relapse|Acute Myeloid Leukemia Refractory
Keystone Nano Inc|University of Virginia|Milton S. Hershey Medical Center
 June 1 2024 Phase 1
NCT06180837 Recruiting
Lifestyle Factors|Overweight and Obesity|Insulin Sensitivity|Eating Habit|Sleep Hygiene|Type 2 Diabetes|Sleep|Sleep Deprivation|Insufficient Sleep Syndrome
University of Utah
 February 12 2024 Not Applicable
NCT05554627 Withdrawn
Depressive Disorder Major
VA Office of Research and Development
 October 27 2023 Phase 4
NCT05280015 Recruiting
Depression|Depressive Disorder|Depressive Disorder Major
Centre Hospitalier Universitaire de Besancon|Fondation FondaMental|GYNOV
 June 8 2022 Phase 2
NCT05791370 Completed
Diet|Healthy
Malaysia Palm Oil Board|Universiti Putra Malaysia
 January 1 2019 Not Applicable

Chemical Information & Solubility

Molecular Weight 268.29 Formula

C13H8N4OS
CAS No. 608512-97-6 SDF --
Smiles C1=CC2=C(C3=C1NC(=O)C3=CC4=CN=CN4)SC=N2
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 13 mg/mL ( (48.45 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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