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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 | Availability | Quantity |
---|---|---|---|
1 mg | $31 | In Stock | |
5 mg | $113 | In Stock | |
10 mg | $213 | In Stock | |
25 mg | $438 | In Stock | |
50 mg | $653 | In Stock | |
100 mg | $876 | In Stock | |
500 mg | $1,750 | In Stock | |
1 mL x 10 mM (in DMSO) | $196 | In Stock |
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 |
Targets&IC50 | PRAK:5.0 nM, MK2:(ki)3 nM, MK2:5.2 nM, MK3:53 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 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 41.67 mg/mL (111.28 mM), Sonication and heating to 80℃ are recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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