化学信息：
| 化学名 | 4-[4-(4-fluorophenyl)-2-(4-nitrophenyl)-1H-imidazol-5-yl]pyridine |
|
| 简称 | PD169316 | |
| 别名 |
PD 169316, PD-169316 |
|
| 中文名 | N/A | |
| 化学式 | C20H13FN4O2 | |
| 分子量 | 360.34 | |
| CAS号 | 152121-53-4 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO10mg/ml; Ethanol<1mg/ml |
|
| 溶液配制 | 5mg加入1.39ml DMSO，或者每3.6mg加入1ml DMSO，配制成10mM溶液。SD5946-10mM用DMSO配制。 |
生物信息：
| 产品描述 | PD 169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor (IC50=89nM). | ||||
| 信号通路 | MAPK | ||||
| 靶点 | p38 MAPK | － | － | － | － |
| IC50 | 89nM | － | － | － | － |
| 体外研究 | PD169316, a p38 MAPK inhibitor, abrogates signaling initiated by both TGFbeta and Activin A, but not bone morphogenetic protein (BMP) 4. Inhibition of TGFbeta signaling is dose dependent and results in reduced Smad2 and Smad3 phosphorylation, nuclear translocation, and up-regulation of the TGFbeta target gene Smad7. Reduced TGFbeta signaling is not due to abrogation of p38 MAPK activity, since blocking p38 MAPK activity with a dominant negative form of p38 MAPK has no effect on TGFbeta/Smad signaling. PD169316 at 5μM or higher can block TGFβ signaling activity and thus caution must be used when attributing cellular activities exclusively to p38 MAPK signaling when these inhibitors are used experimentally. PD169316 significantly attenuated apoptosis in potassium-deprived cells in a dose dependent manner. PD169316 rescued the inhibitory effect of sphingosine on the formation of inositol phosphates by PGF(2alpha) or NaF in osteoblast-like MC3T3-E1 cells. 6-keto-PGF(1alpha) release was increased in a concentration-dependent manner following LPS exposure (maximal at 10(-6)g/ml; EC(50)=1 x 10(-9)g/ml), and was significantly inhibited by p38 MAPK blockade (reduced from 1.6+/-0.3 x 10(-9)g/ml to 4+/-1 x 10(-10)g/ml and 4+/-2 x 10(-10)g/ml with 10(-6) M SB203580 or 10(-6) M PD169316, respectively). | ||||
| 体内研究 | N/A | ||||
| 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 | N/A |
| 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 | N/A |
| 配制 | N/A |
| 剂量 | N/A |
| 给药方式 | N/A |
| 产品编号 | 产品名称 | 包装 |
| SD5946-10mM | PD169316 (p38 MAPK抑制剂) | 10mM×0.2ml |
| SD5946-5mg | PD169316 (p38 MAPK抑制剂) | 5mg |
| SD5946-25mg | PD169316 (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。
