化学信息：
| 化学名 | 4-[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)imidazol-1-yl]cyclohexan-1-ol |
|
| 简称 | SB239063 | |
| 别名 |
SB 239063, SB-239063 |
|
| 中文名 | N/A | |
| 化学式 | C20H21FN4O2 | |
| 分子量 | 368.4 | |
| CAS号 | 193551-21-2 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO60mg/ml; Ethanol7mg/ml warming |
|
| 溶液配制 | 5mg加入1.36ml DMSO，或者每3.68mg加入1ml DMSO，配制成10mM溶液。SD5937-10mM用DMSO配制。 |
生物信息：
| 产品描述 | SB239063是一种有效的选择性p38 MAPKα/β抑制剂，IC50为44nM，对γ-和δ-激酶亚型没有活性。 | ||||
| 信号通路 | MAPK | ||||
| 靶点 | p38α | p38β | － | － | － |
| IC50 | 44nM | 44nM | － | － | － |
| 体外研究 | SB 239063 potently inhibits IL-1 and TNF-α production in LPS-stimulated human peripheral blood monocytes with IC50 of 120 and 350nM, respectively. In oxygen-glucose-deprived hippocampal slice cultures, SB239063 strikingly reduces the levels of the pro-inflammatory cytokine IL-1beta, causes cell death after oxygen-glucose deprivation and significantly diminishes microglia activation. In human corneal endothelial cell, SB 239063 inhibits TGF-β(2) and FGF-2-induced cell migration. | ||||
| 体内研究 | In both guinea pigs and mice, SB 239063 (10mg/kg, p.o.) reduces antigen-induced airway eosinophilia. In air- and ozone-exposed C57/BL6 and MKP-1(-/-) mice, SB239063 inhibits bronchial contraction. | ||||
| 临床实验 | N/A | ||||
| 特征 | N/A | ||||
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
| 酶活性检测实验 | |
| 方法 | Yeast-expressed, activated, and purified p38α (3.55nM) is added to the reaction mixture (30μl) containing 25mM HEPES, pH 7.5; 10mM MgCl2; 0.2mM sodium orthovanadate; 1mM dithiothreitol; 0.1% BSA; 10% (w/v) glycerol; 0.17mM/2.5 μCi of [γ-32P]ATP; 0.67mM the endothelial growth factor receptor-derived T669 peptide as the substrate in the presence or absence of SB 239063. Incubation is for 25 min at 37℃ in 96-well plates, the reactions are stopped by adding 10μl of 0.3M phosphoric acid, and phosphorylated peptide is isolated from the reaction mixture on phosphocellulose (p81) filters. Filters are washed three times with 75mM phosphoric acid, followed by three times with H2O, and counted for bound 32P. The inhibitor is preincubated with the reaction mixture on ice for 30 min before starting the reactions with [γ-32P]ATP. |
| 细胞实验 | |
| 细胞系 | N/A |
| 浓度 | N/A |
| 处理时间 | N/A |
| 方法 | N/A |
| 动物实验 | |
| 动物模型 | Guinea pigs |
| 配制 | Acidified 0.5% Tragacanth |
| 剂量 | ~30mg/kg |
| 给药方式 | p.o. |
| 产品编号 | 产品名称 | 包装 |
| SD5937-10mM | SB239063 (p38 MAPK抑制剂) | 10mM×0.2ml |
| SD5937-5mg | SB239063 (p38 MAPK抑制剂) | 5mg |
| SD5937-25mg | SB239063 (p38 MAPK抑制剂) | 25mg |
| — | 说明书 | 1份 |
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
