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BIX 02189
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BIX 02189图片
CAS NO:1094614-85-3
规格:98%
分子量:440.54
包装与价格:
包装价格(元)
5mg电议
25mg电议
100mg电议

产品介绍
Selective MEK5 inhibitor
CAS:1094614-85-3
分子式:C27H28N4O2
分子量:440.54
纯度:98%
存储:Store at -20°C

Background:

BIX 02189 is a selective inhibitor of MEK5 with IC50 value of 1.5 nM1.


BIX 02189 belongs to the indolinone kinase inhibitor series. It selectively inhibited the catalytic activity of MEK5 but not other closely related kinases such as MEK1, MEK2, ERK2 and JNK2. BIX 02189 also inhibited ERK5 with IC50 value of 59 nM. In HeLa cells, treatment of BIX 02189 inhibited the phosphorylation of ERK5 but not ERK1/2. Besides that, BIX 02189 prevented the transcription of the downstream substrate MEF2C in HeLa and HEK293 cells. Moreover, in a three-dimensional lymphangiogenic sprouting assay, BIX 02189 resulted in an inhibition of lymphangiogenic sprouting with a minimal effective concentration of 1 μM1,2.


参考文献:
1. Tatake R J, O’Neill M M, Kennedy C A, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochemical and biophysical research communications, 2008, 377(1): 120-125.
2. Schulz M M P, Reisen F, Zgraggen S, et al. Phenotype-based high-content chemical library screening identifies statins as inhibitors of in vivo lymphangiogenesis. Proceedings of the National Academy of Sciences, 2012, 109(40): E2665-E2674.