BIX 02189 |
| Catalog No.GC12220 |
BIX 02189 es un inhibidor de MEK5 potente y selectivo con una IC50 de 1,5 nM. BIX 02189 también inhibe la actividad catalítica de ERK5 con un IC50 de 59 nM.
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Cas No.: 1265916-41-3
Sample solution is provided at 25 µL, 10mM.
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BIX 02189 is a selective inhibitor of MEK5 with IC50 value of 1.5 nM 1.
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 μM 1,2.
References:
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.
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