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PKR-IN-C16 (Compound C16) is a specific double-stranded RNA-dependent protein kinase (PKR) inhibitor. PKR-IN-C16 shows promising neuroprotective properties and can rescue acute brain lesions.

For research use only. We do not sell to patients.

PKR-IN-C16 Chemical Structure

PKR-IN-C16 Chemical Structure

CAS No. : 608512-97-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 139 In-stock
Solution
10 mM * 1 mL in DMSO USD 139 In-stock
Solid
1 mg USD 47 In-stock
5 mg USD 100 In-stock
10 mg USD 170 In-stock
25 mg USD 350 In-stock
50 mg USD 550 In-stock
100 mg USD 950 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PKR-IN-C16 (Compound C16) is a specific double-stranded RNA-dependent protein kinase (PKR) inhibitor. PKR-IN-C16 shows promising neuroprotective properties and can rescue acute brain lesions[1].

IC50 & Target

PKR[1]

In Vitro

PKR-IN-C16 (Compound C16) is able to unlock the translation blockade induced by PKR in primary neuronal cultures[1].
? PKR-IN-C16 (0.1 or 0.3 μM; 24 h) shows protective effect against the neuronal cell death induced by endoplasmic reticulum stress in SH-SY5Y cells[1].
? PKR-IN-C16 (1-1000 nM; 4 h) prevents not only PKR-phosphorylation but also the activation of caspase-3 induced by Amyloid β in SH-SY5Y cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: Human SH-SY5Y cells
Concentration: 1, 10, 20, 200, 1000 nM
Incubation Time: 4 h
Result: Markedly reduces the level of phosphorylated PKR in the cells exposed to 20 μM Amyloid β.
In Vivo

PKR-IN-C16 (Compound C16) (60 or 600 μg/kg; i.p.; 3 times) prevents not only the PKR-induced neuronal loss but also the inflammatory response in the Quinolinic acid (QA) (HY-100807) induced acute excitotoxic rat model[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Normotensive male Wistar rats, excitotoxic neuroinflammatory model, inflammation was induced by unilateral striatal injection of quinolinic acid (QA)[1]
Dosage: 60 or 600 μg/kg
Administration: Intraperitoneal injection; 24 h, 2 h before QA injection and 24 h post-QA injection
Result: Reduced expression of the active catalytic domain of the PKR, prevented increase of IL-1β levels on the contralateral side (97% inhibition) at 600 μg/kg. Decreased by 47% the neuronal loss and by 37% the number of positive cleaved caspase-3 neurons induced by QA injection at 600 μg/kg.
Molecular Weight

268.29

Formula

C13H8N4OS

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1/C(C2=C(SC=N3)C3=CC=C2N1)=C\C4=CN=CN4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (37.27 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7273 mL 18.6365 mL 37.2731 mL
5 mM 0.7455 mL 3.7273 mL 7.4546 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1 mg/mL (3.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.55%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7273 mL 18.6365 mL 37.2731 mL 93.1827 mL
5 mM 0.7455 mL 3.7273 mL 7.4546 mL 18.6365 mL
10 mM 0.3727 mL 1.8637 mL 3.7273 mL 9.3183 mL
15 mM 0.2485 mL 1.2424 mL 2.4849 mL 6.2122 mL
20 mM 0.1864 mL 0.9318 mL 1.8637 mL 4.6591 mL
25 mM 0.1491 mL 0.7455 mL 1.4909 mL 3.7273 mL
30 mM 0.1242 mL 0.6212 mL 1.2424 mL 3.1061 mL
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PKR-IN-C16 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PKR-IN-C16
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