BIX02189 (BIX 02189, BIX-02189) 属于二氢吲哚酮激酶抑制剂系列,是一种选择性的和可逆的MAPK激活酶(MAPK/ERK激酶、MEK)抑制剂,阻⽌上游激酶激活MEK5,也抑制 ERK5磷酸化活性,IC50值分别为1.5 nM和59 nM。BIX02189可阻断ERK5的磷酸化,而不会影响山梨糖醇刺激的HeLa细胞中ERK1/2的磷酸化。
参考文献
[1]. Tatake RJ, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun. 2008 Dec 5;377(1):120-5.
[2]. Seong Ji Park. et al. BIX02189 inhibits TGF-β1-induced lung cancer cell metastasis by directly targeting TGF-β type I receptor. Cancer letters, 2016;381(2), 314-322.
[3]. Kimura TE, et al. Targeted deletion of the extracellular signal-regulated protein kinase 5 attenuates hypertrophic response and promotes pressure overload-induced apoptosis in the heart. Circ Res. 2010 Mar 19;106(5):961-70.
冰袋运输。粉末直接保存于-20℃,有效期2年。溶于DMSO。建议分装后-20℃避光保存,避免反复冻融。