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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10Z-Hymenialdisine是广谱激酶抑制剂, 高活性抑制 MEK1。
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PD 334581是MEK1 抑制剂。
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PD 198306是MEK1/2的选择性抑制剂。
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BIX 02189是一种选择性的MEK5抑制剂,IC50为1.5 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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U0126-EtOH(U-0126)是MEK1和2选择性抑制剂,IC50分别为70nM和60nM,对ΔN3-S218E/S222D MEK的亲和力比PD098059强100倍。
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