U0126是一种选择性、非竞争性MAPK激酶抑制剂，作用于MEK1和MEK2，IC50分别是70 nM和60 nM，比PD 98059的抑制活性高100倍左右，而对其他MAPK激酶如PKC、Ab1、Raf、MEKK、ERK和JNK等没有或微弱抑制作用。U0126具有抗炎症作用，抑制AP-1转录，并抑制多种参与炎症反应的细胞因子和金属蛋白酶活性。在小鼠哮喘模型中，U0126显著抑制OVA诱导的总细胞数增加，并显著降低血清中总IgE、OVA特异的IgE和IgG1水平，组化结果显示，U0126明显抑制OVA诱导的肺组织嗜酸细胞增多，及VCAM-1表达。

参考文献：

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[2] Duncia JV, et al. MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products. Bioorganic & Medicinal Chemistry Letters,8(20): 2839-2844 (1998).

[3] DeSilva DR, et al. Inhibition of mitogen-activated protein kinase kinase blocks T cell proliferation but does not induce or prevent anergy. J Immunol. 160(9): 4175-4181 (1998).

[4] Duan W, et al. Anti-Inflammatory Effects of Mitogen-Activated Protein KinaseKinase Inhibitor U0126 in an Asthma Mouse Model. J Immunol 172:7053-7059 (2004).

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