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BIX02189

CAS号

1265916-41-3

分子式

C27H28N4O2

主要靶点

ERK|MEK

仅限科研使用

Cat No : CM05057

Print datasheet

Synonyms

ERK|Extracellular signal regulated kinases|inhibit|BIX-02189|BIX02189|BIX 02189|MEK|Mitogen-activated protein kinase kinase|MAP2K|MAPKK|Inhibitor

验证数据展示

  • CAS No.: 1265916-41-3

    BIX02189
    CAS#: 1265916-41-3

产品信息

CAS号 1265916-41-3
分子式 C27H28N4O2
主要靶点 ERK|MEK
主要通路 MAPK 信号通路|MAPK 信号通路
分子量 440.54
纯度 97.84%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 ERK|Extracellular signal regulated kinases|inhibit|BIX-02189|BIX02189|BIX 02189|MEK|Mitogen-activated protein kinase kinase|MAP2K|MAPKK|Inhibitor

靶点活性

RPS6KA6/RSK4:990 nM|ERK5:59 nM|c-Kit:1.1 μM|RPS6KA3/RSK2:2.1 μM|FGFR1:1 μM|CSF1R (FMS):46 nM|Abl-1:2.4 μM|JAK3:440 nM|TGFβRI:580 nM|MEK5:1.5 nM|Lck:250 nM

体外活性

BIX02189, 它抑制了纯化的MEK5酶的催化功能。MEK5抑制剂阻止了ERK5的磷酸化，但不影响山梨醇刺激的HeLa细胞中ERK1/2的磷酸化。这些化合物还在细胞转录报告系统中抑制了MEK5/ERK5信号通路下游底物MEF2C的转录激活[1]。

溶解度

DMSO:49.4 mg/mL (112.14 mM)

参考文献

1.Tatake RJ, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun. 2008 Dec 5;377(1):120-5.
2.Kim M, et al. Laminar flow activation of ERK5 protein in vascular endothelium leads to atheroprotective effect via NF-E2-related factor 2 (Nrf2) activation. J Biol Chem. 2012 Nov 23;287(48):40722-31.
3.Hwang AR, et al. Fluvastatin inhibits AGE-induced cell proliferation and migration via an ERK5-dependent Nrf2 pathway in vascular smooth muscle cells. PLoS One. 2017 May 22;12(5):e0178278.

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