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PKR-IN-C16 PKR inhibitor

Name: PKR-IN-C16
Brand: Selleck Chemicals
SKU: S9668
Rating: 5 (7 reviews)

Cat.No.S9668

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

Chemical Structure

Molecular Weight: 268.29

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Quality Control

Batch: Purity: 99.79%

99.79

Related Targets	HSP JNK Antioxidant ROS eIF PERK IRE1 ASK PDI ATF-6
Other PKR Inhibitors	PKR-IN-2

Chemical Information, Storage & Stability

Molecular Weight	268.29	Formula	C₁₃H₈N₄OS	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	608512-97-6	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	imoxin, C16, Imidazolo-oxindole PKR inhibitor C16			Smiles	C1=CC2=C(C3=C1NC(=O)C3=CC4=CN=CN4)SC=N2

Solubility

In vitro
Batch:

DMSO : 14 mg/mL (52.18 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.350mg/ml (1.30mM)	Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.350mg/ml (1.30mM)	Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	PKR IL-1β
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 this compound in vitro. This chemical blocks tumour cell growth and angiogenesis via a decrease in mRNA levels of several growth factors.
In vivo	Inflammation is induced by unilateral striatal injection of quinolinic acid (QA) in 10-week-old normotensive rats. The highest dose of this compound (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 this compound (97% inhibition). Macroscopic and microscopic observation of cerebral tissue revealed that tissue integrity is more preserved with this chemical treatment than its vehicle in QA rats. Furthermore, this chemical treatment decreases by 47% the neuronal loss and by 37% the number of positive cleaved caspase-3 neurons induced by QA injection. In conclusion, this compound 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/24211709/ [2] https://pubmed.ncbi.nlm.nih.gov/32198380/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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