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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PLX 4720是B-RafV600E和c-Raf-1Y340D/Y341D的抑制剂，IC50分别为13 nM和6.7 nM。
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SCH772984是一种新型特异性的ERK1/2抑制剂， IC50分别为4 Nm/1 nM。
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Selumetinib (AZD6244)是一种高选择性的MEK1抑制剂，IC50为14 nM，也抑制ERK1/2磷酸化，IC50为10 nM，但对p38α， MKK6， EGFR， ErbB2， ERK2， B-Raf等没有抑制作用。
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GDC-0623是一种有效的 ATP 非竞争性MEK1抑制剂，Ki为 0.13 nM。
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SL-327是可渗透入细胞的MEK-1和MEK-2抑制剂，IC50分别为180nM和220nM。
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