|(Z)-3-(((3-((二甲基氨基)甲基)苯基)氨基)(苯基)亚甲基)-2-氧代吲哚-6-甲酰胺|CsnPharm

CAS No.: 334949-59-6

BIX02188 Catalog No. CSN12415

Synonyms: BIX02188 Z-Isomer

BIX-02188 is a selective inhibitor of MEK5 with IC50 of 4.3 nM, also inhibits ERK5 catalytic activity with IC50 of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.

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技术信息

生物活性

描述Mitogen-activated protein kinases/extracellular signal-regulated kinase (MAPK/ERK) pathway, also known as MEK pathway, is reported to be associated with the cell proliferation, differentiation, migration, senescence and apoptosis^[3]. BIX-02188 is a potent MEK5-selective inhibitor with an IC₅₀ of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC₅₀ of 810 nM^[4]. In activated HeLa cells, BIX-02188 blocks phosphorylation of ERK5, without affecting phosphorylation of ERK1/2, c-Jun amino terminal kinase (JNK) and p38 MAP kinases. Phosphorylated BMK1 (ERK5) is inhibited by BIX-02188 in a dose-dependent manner, with an IC₅₀ of 0.8±1.0 μM, and maximal inhibition at concentrations >3 μM, which confirms the selectivity of BIX-02188 for MEK5-induced BMK1 phosphorylation^[5]. When podocytes are pre-incubated in the absence or presence of BIX-02188 (10 μM) for 60 min, Inhibition of Erk5 activation with BIX-02188 incubation reduces podocyte cell number^[6].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4243 mL
- 12.1217 mL
- 24.2434 mL
- 5 mM
- 0.4849 mL
- 2.4243 mL
- 4.8487 mL
- 10 mM
- 0.2424 mL
- 1.2122 mL
- 2.4243 mL

技术信息

CAS号

334949-59-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H24N4O2

运输

蓝冰

分子量

412.48

别名

BIX02188 Z-Isomer

溶解度

DMSO	45.0 mg/mL (109.1 mM)

动物实验配方

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