BIRB 796,又称为BIRB-796、Doramapimod,是一种高效的p38 MAPK抑制剂(Kd=0.1 nM),在LPS刺激的THP-1细胞中BIRB 796可以抑制TNF α释放(IC50=18 nM)。另外,BIRB 796抑制所有的p38 MAPK亚型和c-Jun N末端激酶(JNK)亚型。BIRB 796也会抑制SAPK3/p38γ的活性和激活,并抑制压力诱导的SAP97蛋白磷酸化,在HEK293细胞中,BIRB 796抑制JNK1/2的活性和激活反应。
参考文献
[1] Pargellis C, et al. Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. Nat. Struct. Biol. 9: 268-272 (2002).
[2] Branger J, et al. Anti-Inflammatory Effects of a p38 Mitogen-Activated Protein Kinase Inhibitor During Human Endotoxemia. J. Immunol. 168: 4070-4077 (2002).
[3] Regan J, et al. Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. J Med Chem 45(14): 2994-3008 (2002).
[4] Branger J, et al. Inhibition of coagulation, fibrinolysis, and endothelial cell activation by a p38 mitogen-activated protein kinase inhibitor during human endotoxemia. Blood 101: 4446-4448 (2003).
[5] Kuma Y, et al. BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo. J. Biol. Chem. 280(20): 19472-19479 (2005).
冰袋运输。粉末直接保存于-20ºC,有效期2年。溶于DMSO。建议分装后-20ºC避光保存,避免反复冻存,至少可存放6个月。