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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SB202190 (FHPI)是一种有效的p38 MAPK抑制剂,靶向作用于p38α/β,IC50为50 nM/100 nM。
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Doramapimod (BIRB 796)是高度选择性p38α MAPK抑制剂,Kd为0.1 nM,对JNK2,c-RAF,Fyn,Lck,ERK-1,SYK,IKK2,ZAP-70,EGFR,HER2,PKA,PKC和PKCα/β/γ的抑制性较弱。
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SB203580, a selective inhibitor of p38MAPK, controls the various inflammatory responses and cellular stresses. SB203580是一种p38 MAPK抑制剂,IC50为0.3-0.5 μM,与SAPK3(106T)和SAPK4(106T)相比选择性低10倍,且抑制PKB磷酸化,IC50为3-5 μM。
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Skepinone-L是一种选择性p38 MAPK抑制剂,IC50为5 nM。
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Asiatic acid是积雪草苷的糖苷配基,从植物积雪草中分离而来的,常用于伤口愈合。
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