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PF-3644022

CAS No. : 1276121-88-0

MCE 站：PF-3644022

产品活性：PF-3644022 是一种有效的，选择性的，口服活性的，具有 ATP 竞争性的 MAPKAPK2 (MK2) 抑制剂，IC₅₀ 为 5.2 nM，K_i 为 3 nM。PF-3644022 还抑制 MK3 和 p38 调节/激活激酶 (PRAK)，IC₅₀ 分别为 53 nM 和 5.0 nM。PF-3644022 有效抑制 TNFα 的产生并具有抗炎作用。

研究领域：MAPK/ERK Pathway

作用靶点：MAPKAPK2 (MK2)  |  p38 MAPK

In Vitro: 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.
In the human U937 monocytic cell line or peripheral blood mononuclear cells, PF-3644022 potently inhibits TNFα production with similar activity (IC₅₀ of 160 nM). PF-3644022 blocks TNFα and IL-6 production in LPS-stimulated human whole blood with IC₅₀ values of 1.6 and 10.3 μM, respectively. Inhibition of TNFα in U937 cells and blood correlates closely with inhibition of phospho-heat shock protein 27, a target biomarker of MK2 activity.

In Vivo: PF-3644022 (3-100 mg/kg; oral gavage; twice a day; for 12 days; Lewis rats) treatment shows dose-dependent inhibition of chronic paw swelling measured on day 21 after 12 days of oral dosing, with ED₅₀ value of 20 mg/kg.

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