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BIX 02189

现货
Catalog No.
A5801
MEK5抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,500.00
现货
5mg
¥ 1,200.00
现货
25mg
¥ 3,600.00
现货
100mg
¥ 9,800.00
现货

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Background

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.

文献引用

1. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9. PMID:31063758

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt440.54
Cas No.1094614-85-3
FormulaC27H28N4O2
Solubility≥22.05mg/mL in DMSO, ≥40.7 mg/mL in EtOH with ultrasonic, <1.7 mg/mL in H2O
Chemical Name(3Z)-3-[[3-[(dimethylamino)methyl]anilino]-phenylmethylidene]-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide
SDFDownload SDF
Canonical SMILESCN(C)CC1=CC(=CC=C1)NC(=C2C3=C(C=C(C=C3)C(=O)N(C)C)NC2=O)C4=CC=CC=C4
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

HeLa细胞

溶解方法

在DMSO中的溶解度大于22.1 mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

1.5 h,10 μM

应用

BIX02189抑制MEK5和ERK5的催化活性,IC50分别为1.5 nM和59 nM。在HeLa细胞中,BIX02189以剂量依赖的方式抑制山梨醇激活的ERK5磷酸化。在HeLa和293T细胞中,BIX02189以剂量依赖的方式抑制MEF2诱导的荧光素酶基因表达。

动物实验[2]:

动物模型

SPF级C57BL/6小鼠

剂量

腹腔注射,10 mg/kg

应用

BIX02189显著抑制博来霉素处理小鼠的肺组织中胶原蛋白积累和纤维化的组织学变化。BIX02189也会改善博来霉素接种小鼠的存活率。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Tatake R J, O’Neill M M, Kennedy C A, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway[J]. Biochemical and biophysical research communications, 2008, 377(1): 120-125.

[2]. Kim S, Lim J H, Woo C H. ERK5 inhibition ameliorates pulmonary fibrosis via regulating Smad3 acetylation[J]. The American journal of pathology, 2013, 183(6): 1758-1768.

生物活性

描述 BIX02189是一种选择性的MEK5抑制剂,IC50值为1.5 nM。
靶点 MEK5 ERK5 TGFβR1      
IC50 1.5 nM 59 nM 580 nM      

质量控制