| 货号 | 5989/50 |
| 别名 | N-[3-(1,1-Dimethylethyl)-1-(4-methy |
| 供应商 | Tocris |
| 生物活性 | High affinity and selective p38 kinase inhibitor (Kd = 50-100 pM). Exhibits no significant inhibition on a panel of related kinases. Inhibits LPS-induced TNFα production in human PBMCs and whole blood (IC50 values are 21 and 960 nM, respectively). Also inhibits JNK2α2 and c-Raf-1 (IC50 values are 98 nM and 1.4 μM, respectively). Cell permeable. |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 纯度 | >99 % |
| 计算分子量 | 527.66 |
| 分子式 | C31H37N5O3 |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO and to 50 mM in ethanol |
| 参考文献 | Goldsteinet al (2010) Selective p38α inhibitors clinically evaluated for the treatment of chronic inflammatory disorders. J.Med.Chem. 53 2345. PMID: 19950901. Lauferet al (2008) Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzymes surface-exposed front region. J.Med.Chem. 51 4122. PMID: 18578517. Kumaet al (2005) BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo. J.Biol.Chem. 280 19472. PMID: 15755732. Reganet al (2003) Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). J.Med.Chem. 46 4676. PMID: 14561087. |