PKM2-IN-3
Based on 1 publication(s) in Google Scholar
PKM2-IN-3 is an inhibitor of PKM2 kinase with an IC50 value of 4.1 μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation.
For research use only. We do not sell to patients.
- Purity: 99.44%
- CAS No.: 2408841-19-8
- Formula: C21H22O4
- Molecular Weight:338.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) PKM2-IN-3
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Biological Activity
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PKM2 4.1 μM (IC50) |
PKM2-IN-3 (compound 10i) inhibits the TNF-α release of LPS-stimulated RAW264.7 macrophages, with an IC50 value of 5.2 μM. PKM2-IN-3 exhibits the lowest toxicity with a CC50 value of 43.6 μM[1].
PKM2-IN-3 (0.1-100 μM; 20 min) inhibits PKM2 kinase activity in a cell-free molecular level with an IC50 value of 4.1 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PKM2-IN-3 (1, 10 mg/kg; i.v.; injected at 4 hours and 24 hours after ischemia onset) reduces the infarct volume and improves neurological deficits of tMCAO rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LPS-induced mice (male 6-8 weeks old; 20.0-22.0 g)[1]
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Dosage:1, 10 mg/kg
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Administration:i.p.; daily for 3 days
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Result:Reversed the LPS-induced mice behavior changes in open field test.
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Animal Model:tMCAO Sprague-Dawley rats (Male 8-10 weeks old; 250.0-280.0 g)[1]
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Dosage:1, 10 mg/kg
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Administration:i.v.; injected at 4 hours and 24 hours after ischemia onset
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Result:Reduced the infarct volume and improved neurological deficits of tMCAO rats.
Chemical Information
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CAS No. 2408841-19-8
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Appearance Solid
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Molecular Weight 338.40
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Formula C21H22O4
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Color Off-white to light yellow
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SMILES
COC1=C2C(OCC/C(C2=O)=C\C3=CC=C(C=C3)CC)=CC(OC)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Free Radic Biol Med
Cavidine alleviates paclitaxel-induced peripheral neuropathy by promoting mitochondrial autophagy through inhibiting PKM2-mediated histone lactylation. [Abstract]2025 Sep 24:241:367-383. PMID: 41005738
Solvent & Solubility
DMSO : 200 mg/mL (591.02 mM; Need ultrasonic; 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. 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. 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: ≥ 5 mg/mL (14.78 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
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 (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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. 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 | 2.9551 mL | 14.7754 mL | 29.5508 mL | 73.8771 mL |
| 5 mM | 0.5910 mL | 2.9551 mL | 5.9102 mL | 14.7754 mL | |
| 10 mM | 0.2955 mL | 1.4775 mL | 2.9551 mL | 7.3877 mL | |
| 15 mM | 0.1970 mL | 0.9850 mL | 1.9701 mL | 4.9251 mL | |
| 20 mM | 0.1478 mL | 0.7388 mL | 1.4775 mL | 3.6939 mL | |
| 25 mM | 0.1182 mL | 0.5910 mL | 1.1820 mL | 2.9551 mL | |
| 30 mM | 0.0985 mL | 0.4925 mL | 0.9850 mL | 2.4626 mL | |
| 40 mM | 0.0739 mL | 0.3694 mL | 0.7388 mL | 1.8469 mL | |
| 50 mM | 0.0591 mL | 0.2955 mL | 0.5910 mL | 1.4775 mL | |
| 60 mM | 0.0493 mL | 0.2463 mL | 0.4925 mL | 1.2313 mL | |
| 80 mM | 0.0369 mL | 0.1847 mL | 0.3694 mL | 0.9235 mL | |
| 100 mM | 0.0296 mL | 0.1478 mL | 0.2955 mL | 0.7388 mL |