(E/Z)-BIX02189 | BIX 02189 | BIX 02189 | MEK | AmBeed-信号通路专用抑制剂

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(E/Z)-BIX02189 {[allProObj[0].p_purity_real_show]}

货号：A140614 同义名： BIX 02189

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.

(E/Z)-BIX02189 化学结构
CAS号：1094614-85-3

(E/Z)-BIX02189 3D分子结构
CAS号：1094614-85-3

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(E/Z)-BIX02189 纯度/质量文件产品仅供科研

货号：A140614 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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MEK 亚型比较

产品名称	MEK ↓ ↑	MEK1 ↓ ↑	MEK1/2 ↓ ↑	MEK2 ↓ ↑	MEK5 ↓ ↑	其他靶点	纯度
Honokiol	✔						98%
Mirdametinib	++++ MEK, IC50: 0.33 nM						99%+
Binimetinib	+++ MEK, IC50: 12 nM						99%+
BI-847325		++ MEK1, IC50: 25 nM		+++ MEK2, IC50: 4 nM			99%+
U0126-EtOH		+ MEK1, IC50: 0.07 μM		++ MEK2, IC50: 0.06 μM			98%
GDC-0623		++++ MEK1, IC50: 0.13 nM					99%+
TAK-733		++++ MEK1, IC50: 3.2 nM					99%+
Trametinib		++++ MEK1, IC50: 0.92 nM		++++ MEK2, IC50: 1.8 nM			99%+
Selumetinib		+++ MEK1, IC50: 14 nM MEK1, Kd: 99 nM		+ MEK2, Kd: 530 nM			99%+
CI-1040		++ MEK1, IC50: 17 nM		++ MEK2, IC50: 17 nM			99%+
Myricetin		✔					98%
Refametinib		++ MEK1, IC50: 19 nM		++ MEK2, IC50: 47 nM			99%+
Cobimetinib		+++ MEK1, IC50: 4.2 nM					99%+
PD98059		+ MEK1, IC50: 2 μM					99%+
SL327		+ MEK1, IC50: 0.18 μM		+ MEK2, IC50: 0.22 μM		AP-1	98+%
PD318088			✔				98%
AZD8330			+++ MEK1/2, IC50: 7 nM				99%+
Pimasertib							98%
(E/Z)-BIX02189					++++ MEK5, IC50: 1.5 nM		99%+
(E/Z)-BIX02188					+++ MEK5, IC50: 4.3 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

(E/Z)-BIX02189 生物活性

靶点	MEK5 MEK5, IC50:1.5 nM
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].

(E/Z)-BIX02189 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
human HeLa cells		Function assay		Inhibition of ERK5 phosphorylation in sorbitol-stimulated human HeLa cells, IC50=0.059 μM	23656407

(E/Z)-BIX02189 参考文献

[1]Lim JH, Woo CH. Laminar flow activation of ERK5 leads to cytoprotective effect via CHIP-mediated p53 ubiquitination in endothelial cells. Anat Cell Biol. 2011 Dec;44(4):265-73.

[2]Tatake RJ, O'Neill MM, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun. 2008 Dec 5;377(1):120-5.

[3]TTatake RJ, O'Neill MM, Kennedy CA, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun. 2008;377(1):120-125

[4]Park SJ, Choi YS, Lee S, et al. BIX02189 inhibits TGF-β1-induced lung cancer cell metastasis by directly targeting TGF-β type I receptor. Cancer Lett. 2016;381(2):314-322

[5]Tatake RJ, O'Neill MM, Kennedy CA, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun. 2008;377(1):120-125

(E/Z)-BIX02189 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.35mL

2.27mL

1.13mL

22.70mL

4.54mL

2.27mL

(E/Z)-BIX02189 技术信息

CAS号	1094614-85-3
分子式	C₂₇H₂₈N₄O₂
分子量	440.54

别名	BIX 02189
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

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

溶解度

动物实验配方

2% DMSO+30% PEG 300+5% Tween 80+water 10 mg/mL

(E/Z)-BIX02189 {[allProObj[0].p_purity_real_show]}

(E/Z)-BIX02189 纯度/质量文件产品仅供科研

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(E/Z)-BIX02189 质控信息

(E/Z)-BIX02189 生物活性

(E/Z)-BIX02189 细胞研究

(E/Z)-BIX02189 参考文献

(E/Z)-BIX02189 实验方案

(E/Z)-BIX02189 技术信息

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(E/Z)-BIX02189 {[allProObj[0].p_purity_real_show]}

(E/Z)-BIX02189 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

(E/Z)-BIX02189 质控信息

(E/Z)-BIX02189 生物活性

(E/Z)-BIX02189 细胞研究

(E/Z)-BIX02189 参考文献

(E/Z)-BIX02189 实验方案

(E/Z)-BIX02189 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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(E/Z)-BIX02189 纯度/质量文件产品仅供科研