| Name | PF-3644022 |
| 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). |
| 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]. |
| Storage | 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.
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| Keywords | TNFα | SerineProtease | Serine Protease | safety | PRAK | PF-3644022 | PF3644022 | PF 3644022 | p38MAPK | p38 MAPK | orally | monocytic | MK3 | MK2 | Mitogen-activated protein kinase activated protein kinase 2 | MAPKAPK2 (MK2) | MAPKAP kinase 2 | MAPK activated protein kinase 2 | MAP kinase activated protein kinase 2 | lipopolysaccharide | Inhibitor | inhibit | IL-6 | efficacious | Anti-inflammatory |
| Inhibitors Related | Undecane | Esculin | Bisphenol A | AEBSF hydrochloride | Fumaric acid | Imidazole | Subtilisin | Proteinase K | Afatinib | Ac-Ala-OH | Sodium new houttuyfonate | (Rac)-Hesperetin |
| Related Compound Libraries | Reprogramming Compound Library | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | HIF-1 Signaling Pathway Compound Library | Kinase Inhibitor Library | Anti-Obesity Compound Library | Inhibitor Library | Anti-Fibrosis Compound Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
