p38 MAPK
p38 MAPK are a class of mitogen-activated protein kinases (MAPKs) that are responsive to stress stimuli, such as cytokines, ultraviolet irradiation, heat shock, and osmotic shock, and are involved in cell differentiation, apoptosis and autophagy. p38 MAPK is the mammalian orthologue of the yeast Hog1p MAP kinase, which participates in a signaling cascade controlling cellular responses to cytokines and stress. Four p38 MAP kinases, p38-α (MAPK14), -β (MAPK11), -γ (MAPK12 / ERK6), and -δ (MAPK13 / SAPK4), have been identified. Similar to the SAPK/JNK pathway, p38 MAP kinase is activated by a variety of cellular stresses including osmotic shock, inflammatory cytokines, lipopolysaccharides (LPS), Ultraviolet light, and growth factors.
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JX 401是活性的可逆的p38α 抑制剂。
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Losmapimod一种是口服活性的p38 MAPK抑制剂，对p38α和p38β的pKi为8.1和7.6。
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PH-797804是一种新型吡啶酮抑制剂，作用于p38α，IC50为26 nM；比作用于p38β选择性高4倍以上，不抑制JNK2。
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LY2228820是p38MAPK抑制剂，对p38αMAPK和p38βMAPK的IC50分别为7 nM和3 nM。
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VX-702是一种高选择性p38α MAPK抑制剂，作用于p38α比作用于p38β效果高14倍。
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