MEK
MEK (Mitogen-activated protein kinase kinase,MAP2K,MAPKK) ) is a kinase enzyme which phosphorylates mitogen-activated protein kinase (MAPK). MEK is a member of the MAPK signaling cascade that is activated in melanoma. When MEK is inhibited, cell proliferation is blocked and apoptosis (controlled cell death) is induced. The activators of p38 (MKK3 and MKK6), JNK (MKK4 and MKK7), and ERK (MEK1 and MEK2) define independent MAP kinase signal transduction pathways.
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PD184352 (CI-1040)是一种ATP非竞争性的MEK1/2抑制剂，IC50为17 nM，对MEK1/2的选择性比MEK5高100倍。
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PD0325901是一种选择性的，ATP非竞争性的MEK抑制剂，IC50为0.33 nM，对ERK1和ERK2磷酸化抑制作用比CI-1040强500倍左右。
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PD98059是一种非ATP竞争性的MEK抑制剂，IC50为2 μM，特异性抑制MEK-1介导的MAPK激活；不直接抑制ERK1或ERK2。
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BIX 02188是一种选择性的MEK5抑制剂，IC50为4.3 nM，也抑制ERK5催化活性，IC50为810 nM，且不抑制与其密切相关的激酶MEK1， MEK2， ERK2，和JNK2。
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Trametinib (GSK1120212)是一种高特异性的，有效的MEK1/2抑制剂，IC50为0.92 nM/1.8 nM，对c-Raf， B-Raf， ERK1/2没有抑制活性。
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