| 名称 | PF-3644022 |
| 描述 | 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). |
| 体外活性 | 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]. |
| 体内活性 | 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]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 41.67 mg/mL (111.28 mM), Sonication and heating to 80℃ are recommended.
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| 关键字 | TNFα | safety | PRAK | PF-3644022 | PF3644022 | PF 3644022 | p38 MAPK | orally | monocytic | MK3 | 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 |
| 相关产品 | Exarafenib | Doramapimod | PMSF | Nafamostat mesylate | Vemurafenib | AEBSF hydrochloride | sodium lauroyl-α-hydroxyethyl sulfonate | Bakuchiol | SB 202190 | (-)-Bornyl acetate | MW-150 | Benzamidine hydrochloride |
| 相关库 | 抗结直肠癌化合物库 | 神经再生化合物库 | 经典已知活性库 | 疼痛相关化合物库 | 激酶抑制剂库 | 蛋白酶抑制剂库 | 抑制剂库 | NO PAINS 化合物库 | 抗衰老化合物库 | 免疫/炎症分子化合物库 | 已知活性化合物库 | 抗癌化合物库 |
United States
