BIX02189

BIX02189CAS号: 1265916-41-3分子式: C27H28N4O2分子量: 440.54描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)

产品描述
描述
BIX02189 is a potent and selective inhibitor of MEK5 and ERK5(IC50 : 1.5 nM and 59 nM).
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:49.4 mg/mL (112.14 mM)
生物活性
靶点
RPS6KA6 (RSK4):990 nM, ERK5:59 nM, Kit:1.1 μM, RPS6KA3 (RSK2):2.1 μM, CSF1R (FMS):46 nM, Abl1:2.4 μM, FGFR1:1 μM, JAK3:440 nM, TGFβR1:580 nM, Lck:250 nM, MEK5:1.5 nM
In vitro(体外研究)
BIX02189, which inhibited catalytic function of purified, MEK5 enzyme.?The MEK5 inhibitors blocked phosphorylation of ERK5, without affecting phosphorylation of ERK1/2 in sorbitol-stimulated HeLa cells.?The compounds also inhibited transcriptional activation of MEF2C, a downstream substrate of the MEK5/ERK5 signaling cascade, in a cellular trans-reporter assay system[1].