PKR-IN-C51
Based on 1 Customer Validation
PKR-IN-C51 is an ATP-competitive protein kinase R (PKR) inhibitor with a human IC50 of 9 μM and a human Ki of 3.4 μM. PKR-IN-C51 blocks the activation of PKR, inhibits intracellular PKR activation in primary mouse macrophages, and shows no obvious cytotoxicity. PKR-IN-C51 can be used in studies related to the regulation of PKR-mediated signaling pathways.
For research use only. We do not sell to patients.
- Purity: 99.79%
- CAS No.: 1314594-23-4
- Formula: C23H21N5
- Molecular Weight:367.45
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
IC50: 9 μM (double-stranded RNA-activated protein kinase (PKR))[1]
PKR-IN-C51 (compound 51) acts as an ATP-competitive inhibitor of recombinant human PKR with a Ki of 3.4 μM and an IC50 of 9 μM at 10 μM ATP[1].
PKR-IN-C51 (0.1-100 μM; 24 h) exhibits minimal toxicity to monkey Vero cells and primary mouse bone marrow macrophages[1].
PKR-IN-C51 (20-40 μM; 30 min) inhibits poly[I:C]-induced intracellular PKR activation in a concentration-dependent manner in primary wild-type mouse bone marrow macrophages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:primary wild-type mouse bone marrow macrophages
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Concentration:20, 40 μM
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Incubation Time:30 min
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Result:Inhibited poly[I:C]-induced intracellular PKR activation in a concentration-dependent manner in primary wild-type mouse bone marrow macrophages.
Chemical Information
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CAS No. 1314594-23-4
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Appearance Solid
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Molecular Weight 367.45
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Formula C23H21N5
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Color Light yellow to yellow
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SMILES
CC(NC1=C2C=CC=C1)=C2C3=NC(NCCC4=CNC5=C4C=CC=C5)=NC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 125 mg/mL (340.18 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)
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7215 mL | 13.6073 mL | 27.2146 mL | 68.0365 mL |
| 5 mM | 0.5443 mL | 2.7215 mL | 5.4429 mL | 13.6073 mL | |
| 10 mM | 0.2721 mL | 1.3607 mL | 2.7215 mL | 6.8036 mL | |
| 15 mM | 0.1814 mL | 0.9072 mL | 1.8143 mL | 4.5358 mL | |
| 20 mM | 0.1361 mL | 0.6804 mL | 1.3607 mL | 3.4018 mL | |
| 25 mM | 0.1089 mL | 0.5443 mL | 1.0886 mL | 2.7215 mL | |
| 30 mM | 0.0907 mL | 0.4536 mL | 0.9072 mL | 2.2679 mL | |
| 40 mM | 0.0680 mL | 0.3402 mL | 0.6804 mL | 1.7009 mL | |
| 50 mM | 0.0544 mL | 0.2721 mL | 0.5443 mL | 1.3607 mL | |
| 60 mM | 0.0454 mL | 0.2268 mL | 0.4536 mL | 1.1339 mL | |
| 80 mM | 0.0340 mL | 0.1701 mL | 0.3402 mL | 0.8505 mL | |
| 100 mM | 0.0272 mL | 0.1361 mL | 0.2721 mL | 0.6804 mL |
PKR-IN-C51 Related Classifications
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