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PF-3644022
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PF-3644022
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).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $119 | In Stock | |
| 5 mg | $297 | In Stock | |
| 10 mg | $472 | In Stock | |
| 25 mg | $777 | In Stock | |
| 50 mg | $1,090 | In Stock | |
| 100 mg | $1,460 | In Stock | |
| 500 mg | $2,930 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $327 | In Stock |
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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 |
| 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 a day; for 12 days; Lewis rats) treatment displays dose-dependent inhibition of chronic paw swelling. It is measured on day 21 after 12 days of oral dosing (ED50: 20 mg/kg)[1]. |
| Molecular Weight | 374.46 |
| Formula | C21H18N4OS |
| Cas No. | 1276121-88-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 41.67 mg/mL (111.28 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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