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PF-3644022
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Catalog No. T16501Cas No. 1276121-88-0
PF-3644022 is an effective, selective, and ATP-competitive MAPKAPK2 (MK2) inhibitor (IC50: 5.2 nM and a Ki of 3 nM). PF-3644022 potently inhibits TNFα production and has an anti-inflammatory effect. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) (IC50s: 53 nM and 5.0 nM, respectively).
PF-3644022
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Purity: 98.13%
Catalog No. T16501Cas No. 1276121-88-0
PF-3644022 is an effective, selective, and ATP-competitive MAPKAPK2 (MK2) inhibitor (IC50: 5.2 nM and a Ki of 3 nM). PF-3644022 potently inhibits TNFα production and has an anti-inflammatory effect. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) (IC50s: 53 nM and 5.0 nM, respectively).
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $31 | In Stock | In Stock | |
| 5 mg | $113 | In Stock | In Stock | |
| 10 mg | $213 | In Stock | In Stock | |
| 25 mg | $438 | In Stock | In Stock | |
| 50 mg | $653 | In Stock | In Stock | |
| 100 mg | $876 | In Stock | In Stock | |
| 500 mg | $1,750 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $196 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.13%
Appearance:Solid
Color:Yellow
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | PF-3644022 is an effective, selective, and ATP-competitive MAPKAPK2 (MK2) inhibitor (IC50: 5.2 nM and a Ki of 3 nM). PF-3644022 potently inhibits TNFα production and has an anti-inflammatory effect. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) (IC50s: 53 nM and 5.0 nM, respectively). |
| Targets&IC50 | PRAK:5.0 nM, MK3:53 nM, MK2:(ki)3 nM, MK2:5.2 nM |
| In vitro | PF-3644022 potently inhibits TNFα production with similar activity (IC50 of 160 nM), in the human U937 monocytic cell line or peripheral blood mononuclear cells. PF-3644022 blocks TNFα and IL-6 production in LPS-stimulated human whole blood (IC50: 1.6 and 10.3 μM, respectively). The inhibitory activity of PF-3644022 against other MAPKAP kinase family members is evaluated. Other than MNK2 with an IC50 of 148 nM, other family members are largely not inhibited, showing at least several hundred-fold selectivity versus MK2[1]. |
| In vivo | PF-3644022 (3-100 mg/kg; oral gavage; twice daily for 12 days; Lewis rats) treatment exhibits dose-dependent inhibition of chronic paw swelling, measured on day 21 post-treatment (ED50: 20 mg/kg)[1]. |
| Molecular Weight | 374.46 |
| Formula | C21H18N4OS |
| Cas No. | 1276121-88-0 |
| Smiles | C[C@@H]1CNc2c(sc3ccc4nc(ccc4c23)-c2ccc(C)nc2)C(=O)N1 |
| Relative Density. | 1.298 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 41.67 mg/mL (111.28 mM), Sonication and heating to 80℃ are recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Keywords
TNFαSerineProteaseSerine ProteasesafetyPRAKPF-3644022PF3644022PF 3644022p38MAPKp38 MAPKorallymonocyticMK3MK2Mitogen-activated protein kinase activated protein kinase 2MAPKAPK2 (MK2)MAPKAP kinase 2MAPK activated protein kinase 2MAP kinase activated protein kinase 2lipopolysaccharideInhibitorinhibitIL-6efficaciousAnti-inflammatory
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