|3-(((3-((二甲基氨基)甲基)苯基)氨基)苯基亚甲基)-2,3-二氢-N,N-二甲基-2-氧代-1H-吲哚-6-甲酰胺|CsnPharm

CAS No.: 1094614-85-3

3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide Catalog No. CSN18791

BIX-02189(Random Configuration) is a selective and potent inhibitor of both MEK5 and ERK5 with IC50 values of 1.5 and 59 nM, respectively.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 MEK5

IC50:1.5nM ERK5

IC50:59nM
描述MEK5 is a dual specificity protein kinase that belongs to the mitogen-activated protein kinase family. This kinase specifically interacts with and activates MAPK7/ERK5. The signal cascade mediated by this kinase is involved in growth factor stimulated cell proliferation and muscle cell differentiation. BIX-02189 is a selective inhibitor of MEK5 with IC50 value of 1.5nM. BIX-02189 also inhibits ERK5, TGFβR1, ABL1, CSF1R, JAK3, KIT, LCK, MAPK14, RPS6KA3,RPS6KA6 and SRC with IC50 values of 59nM, 580nM, 2400nM, 46nM, 1000nM, 440nM, 1100nM, 250nM, 3700nM, 2100nM, 990nM and 7600nM, respectively. In vitro, BIX-02189 inhibited Hela and HEK293cells with IC50 values of 0.53nM and 0.26nM, respectively^[3]. Treatment A549 lung cancer cells with 2.5-10μM BIX-02189 completely hindered the EGF-induced phosphorylation of ERK5 in a concentration-dependent manner without affecting the phosphorylation of ERK1/2. BIX02189 significantly abolished TGF-β1-mediated E-cadherin repression and N-cadherin induction. In addition, BIX02189 inhibited TGF-β1-induced cell motility and activation of MMP-2 in A549 lung cancer cells. In vivo, Intraperitoneal administration of BIX-02189 at 20mg/kg once daily for 3 weeks inhibited TGF-β receptor type I (TβRI) derived lung metastasis in TβRI-derived A549 xenograft mouse model^[4].
作用机制BIX-02189 inhibits catalytic function of MEK5 and blocks phosphorylation of ERK. ^[5].
细胞研究
Cell Data
Cell Lines Concentration Assay Type Time Activity Description Data Sources
human HeLa cells - Function assay - Inhibition of ERK5 phosphorylation in sorbitol-stimulated human HeLa cells, IC50=0.059 μM 23656407
参考文献

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human HeLa cells	-	Function assay	-	Inhibition of ERK5 phosphorylation in sorbitol-stimulated human HeLa cells, IC50=0.059 μM	23656407

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
- 2.2699 mL
- 11.3497 mL
- 22.6994 mL
- 5 mM
- 0.4540 mL
- 2.2699 mL
- 4.5399 mL
- 10 mM
- 0.2270 mL
- 1.1350 mL
- 2.2699 mL

技术信息

CAS号

1094614-85-3

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H28N4O2

运输

蓝冰

分子量

440.54

别名

溶解度

DMSO	60.0 mg/mL (136.2 mM) warming
Water	Insoluble
Ethanol	80.0 mg/mL (181.6 mM)

动物实验配方

2% DMSO+30% PEG 300+5% Tween 80+water

10 mg/mL

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3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide Catalog No. CSN18791

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