BIX02189 | MEK | AmBeed-信号通路专用抑制剂

BIX02189 {[allProObj[0].p_purity_real_show]}

货号：A511821

BIX02189是一种选择性的 MEK5/ERK5 抑制剂，IC50 为 59 nM。

BIX02189 化学结构
CAS号：1265916-41-3

BIX02189 3D分子结构
CAS号：1265916-41-3

规格	价格	会员价	库存	数量
{[ item.pr_size ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]}	现货	1周咨询	- +

购物车0 收藏询单

sales@ambeed.cn tech@ambeed.cn 400-920-2911 产品手册产品订购技术咨询
快速发货顺丰冷链运输，1-2 天到达

品质保证

技术支持

免费溶解

BIX02189 纯度/质量文件产品仅供科研

货号：A511821 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

全球学术期刊中引用的产品: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 更多 >

BIX02189 质控信息

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			✔				99%
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。

BIX02189 生物活性

描述

BIX02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM.

BIX02189 细胞实验

Cell Line Human umbilical vein endothelial cells (HUVECs) HEK293 cells HeLa cells neonatal rat cardiomyocytes (NRCMs) LN229 cells U251 cells PC12 cells	Concentration	Treated Time	Description	References
Human umbilical vein endothelial cells (HUVECs)	10 μM	16–24 h	To investigate the effect of ERK5 inhibitor BIX02189 on laminar flow-induced Nrf2 nuclear translocation. Results showed that BIX02189 significantly inhibited laminar flow-induced Nrf2 nuclear translocation.	J Biol Chem. 2012 Nov 23;287(48):40722-31.
HEK293 cells	1.5 nM		Inhibition of MEK5 activity	Clin Cancer Res. 2011 Jun 1;17(11):3527-32.
HeLa cells	1.5 nM		Inhibition of MEK5 activity	Clin Cancer Res. 2011 Jun 1;17(11):3527-32.
neonatal rat cardiomyocytes (NRCMs)	10μM	2 h	inhibition of ERK5 kinase activity, reduction of MEF2 transcriptional activity, and blunting of hypertrophic responses	Circ Res. 2010 Mar 19;106(5):961-70.
LN229 cells	5μM	72 h	Inhibited the protein expression of GINS2, EGR1, and ECT2	Cell Death Dis. 2024 Mar 11;15(3):205.
U251 cells	5μM	72 h	Inhibited the protein expression of GINS2, EGR1, and ECT2	Cell Death Dis. 2024 Mar 11;15(3):205.
PC12 cells	30 μM	30 min	To investigate the role of ERK5 signaling in PC12 cells, results showed that BIX02189 selectively inhibited ERK5 phosphorylation without affecting ERK1/2 phosphorylation.	J Biol Chem. 2009 Aug 28;284(35):23564-73.

Cell Line

Human umbilical vein endothelial cells (HUVECs) HEK293 cells HeLa cells neonatal rat cardiomyocytes (NRCMs) LN229 cells U251 cells PC12 cells

Concentration

Treated Time

Description

References

Human umbilical vein endothelial cells (HUVECs)

10 μM

16–24 h

To investigate the effect of ERK5 inhibitor BIX02189 on laminar flow-induced Nrf2 nuclear translocation. Results showed that BIX02189 significantly inhibited laminar flow-induced Nrf2 nuclear translocation.

J Biol Chem. 2012 Nov 23;287(48):40722-31.

HEK293 cells

1.5 nM

Inhibition of MEK5 activity

Clin Cancer Res. 2011 Jun 1;17(11):3527-32.

HeLa cells

1.5 nM

Inhibition of MEK5 activity

Clin Cancer Res. 2011 Jun 1;17(11):3527-32.

neonatal rat cardiomyocytes (NRCMs)

10μM

2 h

inhibition of ERK5 kinase activity, reduction of MEF2 transcriptional activity, and blunting of hypertrophic responses

Circ Res. 2010 Mar 19;106(5):961-70.

LN229 cells

5μM

72 h

Inhibited the protein expression of GINS2, EGR1, and ECT2

Cell Death Dis. 2024 Mar 11;15(3):205.

U251 cells

5μM

72 h

Inhibited the protein expression of GINS2, EGR1, and ECT2

Cell Death Dis. 2024 Mar 11;15(3):205.

PC12 cells

30 μM

30 min

To investigate the role of ERK5 signaling in PC12 cells, results showed that BIX02189 selectively inhibited ERK5 phosphorylation without affecting ERK1/2 phosphorylation.

J Biol Chem. 2009 Aug 28;284(35):23564-73.

BIX02189 动物实验

Species C57BL/6 mice Mice	Animal Model Aortic endothelial cells Pregnant mouse model	Administration	Dosage	Frequency	Description	References
C57BL/6 mice	Aortic endothelial cells	Intraperitoneal injection	10 mg/kg	Single dose	To investigate the effect of ERK5 inhibitor BIX02189 on laminar flow-induced Nrf2 nuclear translocation. Results showed that BIX02189 significantly inhibited laminar flow-induced Nrf2 nuclear translocation.	J Biol Chem. 2012 Nov 23;287(48):40722-31.
Mice	Pregnant mouse model	Intraperitoneal injection	10 mg/kg	Once daily from gestational day 1 to day 15	Suppression of ERK5 activation reduced beta-cell proliferation, leading to increased random blood glucose levels and impaired glucose response.	Cell Prolif. 2018 Jun;51(3):e12410

Species

C57BL/6 mice Mice

Animal Model

Aortic endothelial cells Pregnant mouse model

Administration

Dosage

Frequency

Description

References

C57BL/6 mice

Aortic endothelial cells

Intraperitoneal injection

10 mg/kg

Single dose

J Biol Chem. 2012 Nov 23;287(48):40722-31.

Mice

Pregnant mouse model

Intraperitoneal injection

10 mg/kg

Once daily from gestational day 1 to day 15

Suppression of ERK5 activation reduced beta-cell proliferation, leading to increased random blood glucose levels and impaired glucose response.

Cell Prolif. 2018 Jun;51(3):e12410

BIX02189 参考文献

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

BIX02189 技术信息

CAS号	1265916-41-3
分子式	C₂₇H₂₈N₄O₂
分子量	440.54
SMILES Code	O=C(N(C)C)C1=CC(NC2=O)=C(/C2=C(C3=CC=CC=C3)/NC4=CC=CC(CN(C)C)=C4)C=C1
MDL No.	MFCD18074528

别名
运输	蓝冰
InChI Key	ZGXOBLVQIVXKEB-UHFFFAOYSA-N
Pubchem ID	135659062

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C

溶解方案

细胞实验：

DMSO: 50 mg/mL(113.5 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

方案三

BIX02189 {[allProObj[0].p_purity_real_show]}

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

BIX02189 质控信息

BIX02189 生物活性

BIX02189 细胞实验

BIX02189 动物实验

BIX02189 参考文献

BIX02189 实验方案

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

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

BIX02189 {[allProObj[0].p_purity_real_show]}

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

BIX02189 质控信息

BIX02189 生物活性

BIX02189 细胞实验

BIX02189 动物实验

BIX02189 参考文献

BIX02189 实验方案

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

请登录您的专属账户

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

BIX02189 纯度/质量文件产品仅供科研