SKI II (SphK-I2)是一种合成的、非ATP竞争性的、可口服的鞘氨醇激酶(SphK, SK)抑制剂,IC50值为0.5 μM,但对人蛋白激酶ERK2、PKC-I和脂质激酶PI3K没有抑制作用。SKI II可防止SK催化鞘氨醇-1-磷酸(S1P)生成,抑制细胞增殖,在体内能抑制肿瘤生长。
参考文献
1.French KJ, et al. Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res. 2003 Sep 15;63(18):5962-9.
2.French KJ, et al. Antitumor activity of sphingosine kinase inhibitors. J Pharmacol Exp Ther. 2006 Aug;318(2):596-603.
3.Zhu ZA, et al. Reversion of multidrug resistance by SKI-II in SGC7901/DDP cells and exploration of underlying mechanisms. Asian Pac J Cancer Prev. 2012;13(2):625-31.
4.Chiba Y, et al. SKI-II, an inhibitor of sphingosine kinase, ameliorates antigen-induced bronchial smooth muscle hyperresponsiveness, but not airway inflammation, in mice. J Pharmacol Sci. 2010;114(3), 304-310.
冰袋运输。粉末直接保存于-20℃,有效期2年。建议分装后-20℃干燥保存,避免反复冻融。