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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MEK162(ARRY-438162; ARRY-162)是MEK1/2抑制剂，IC50为12 nM。
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Pimasertib (AS-703026)作用于MM细胞系，是一种高度选择性的，有效的，ATP非竞争性的，MEK1/2变构抑制剂，IC50为0.005-2 μM。
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AZD8330是一种新型，选择性的，非ATP竞争性MEK 1/2抑制剂，IC50为7 nM。
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Refametinib是口服生物相容性的MEK抑制剂，对MEK1和MEK2的IC50分别为19 nM和47 nM，有抗肿瘤活性。
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PD318088是ATP非竞争性MEK1/2变构抑制剂，能与ATP同时结合于MEK1，且其结合位点与ATP结合位点相邻。
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