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PF-3644022

PF-3644022 是可口服的，具有 ATP 竞争性的MAPKAPK2 (MK2)选择性抑制剂，IC50为 5.2 nM，Ki 为 3 nM。它有效抑制 TNFα 的产生并具有抗炎作用，还抑制 MK3 和 p38 调节/激活激酶，IC50分别为 53 和 5.0 nM。

CAS号

1276121-88-0

分子式

C21H18N4OS

主要靶点

Serine Protease|p38 MAPK|MAPK

仅限科研使用

Cat No : CM06684

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Synonyms

验证数据展示

  • CAS No.: 1276121-88-0

    PF-3644022
    CAS#: 1276121-88-0

产品信息

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).

CAS号 1276121-88-0
分子式 C21H18N4OS
主要靶点 Serine Protease|p38 MAPK|MAPK
主要通路 MAPK信号通路|蛋白酶体
分子量 374.46
纯度 99.12%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

PRAK:5.0 nM|MK2:(ki)3 nM|MK2:5.2 nM|MK3:53 nM

体内活性

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].

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].

溶解度

DMSO:41.67 mg/mL (111.28 mM),ultrasonic and warming and heat to 80°C

参考文献

1.Mourey RJ, et al. A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor alpha production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation. J Pharmacol Exp Ther. 2010 Jun;333(3):797-807

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