Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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 | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 119.00 | |
5 mg | In stock | $ 297.00 | |
10 mg | In stock | $ 472.00 | |
25 mg | In stock | $ 777.00 | |
50 mg | In stock | $ 1,090.00 | |
100 mg | In stock | $ 1,460.00 | |
500 mg | In stock | $ 2,930.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 327.00 |
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 | MK3:53 nM, PRAK:5.0 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 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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 41.67 mg/mL (111.28 mM), Sonification and heating to 80℃ are recommended.
You can also refer to dose conversion for different animals. More
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PF-3644022 1276121-88-0 MAPK Proteases/Proteasome p38 MAPK Serine Protease MAPKAP kinase 2 monocytic lipopolysaccharide IL-6 TNFα safety Anti-inflammatory orally PRAK efficacious PF3644022 inhibit Mitogen-activated protein kinase activated protein kinase 2 Inhibitor MK3 PF 3644022 MAP kinase activated protein kinase 2 MAPKAPK2 (MK2) MAPK activated protein kinase 2 inhibitor