The family members of the mitogen-activated protein kinase (MAPK) mediate a wide variety of cellular behaviors in response to extracellular stimuli. One of the four main sub-groups, the p38 group of MAP kinases, serve as a nexus for signal transduction and play a vital role in numerous biological processes[3]. SB-239063 is a potent, selective and orally active p38 MAPK inhibitor, exhibits an IC50 of 44 nM for recombinant purified human p38α, with equipotent inhibitory activity against p38α and p38β. It has no effect on p38γ or p38δ[4]. In lipopolysaccharide-stimulated human peripheral blood monocytes, SB-239063 inhibited interleukin-1 and tumor necrosis factor-alpha production with IC50 values of 0.12 and 0.35 μM, respectively[4]. SB-239063 provided substantial protection against cell death induced by either oxygen glucose deprivation (OGD) or magnesium deprivation in cultured neurons[5]. In oxygen-glucose-deprived hippocampal slice cultures, SB-239063 strikingly reduces the levels of the pro-inflammatory cytokine IL-1β, causes cell death after oxygen-glucose deprivation and significantly diminishes microglia activation[6]. In human corneal endothelial cell, SB-239063 inhibits TGF-β (2) and FGF-2-induced cell migration[7]. In both guinea pigs and mice, SB-239063 (10 mg/kg, p.o.) reduces antigen-induced airway eosinophilia, SB-239063 (12 mg/kg; p.o.) almost abolishes ovalbumin (OA)-induced airway eosinophilia (~ 93% inhibition) by inhalation[4].
SB 239063 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
THP1 cells
Function assay
Inhibition of LPS-stimulated TNFalpha production in human THP1 cells, IC50=0.12 μM
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