计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
BIX 02189, 丝裂原活化蛋白激酶 7 抑制剂；丝裂原活化蛋白激酶激酶 5 抑制剂；转化生长因子 beta 受体 1 抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
BIX 02189是一种选择性的MEK5抑制剂，IC50为1.5 nM，也抑制ERK5催化活性，IC50为810 nM，且不抑制与其密切相关的激酶MEK1， MEK2， ERK2，和JNK2。
Information
BIX02189 is a selective inhibitor ofMEK5withIC50of 1.5 nM, also inhibits ERK5 catalytic activity withIC50of 59 nM in cell-free assays, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.
In vitro
BIX02189 blocks MEK5 and ERK5 catalytic activity with IC50 values of 1.5 nM and 59 nM, respectively. They are more potent than the effect caused by BIX02188 with IC50 values of 4.3 nM and 810 nM, respectively. BIX02189 shows inhibitory activity against CSF1R (FMS) with IC50 of 46 nM but displays no activity against related kinases MEK1, MEK2, ERK1, p38α, JNK2, EGFR, and STK16 with IC50 values of >3.7 μM. Pretreatment with BIX02189 inhibits sorbitol-induced phosphorylation of ERK5 in HeLa cells in a dose dependent manner, and displays no inhibitory activity against the phosphorylation of ERK1/2, p38, and JNK1/2 MAPKs. Treatment with only BIX02189 for 24 hours in HeLa or HEK293 cells does not show any cytotoxic effect. BIX02189 inhibits MEK5/ERK5/MEF2C-driven luciferase expression in HeLa and HEK293 cells with IC50 values of 0.53 μM and 0.26 μM, respectively. This is a more significant than the effect caused by BIX02188. BIX02189 inhibits the activation of ERK5, and suppresses C-terminus of Hsc70-interacting protein (CHIP) mediated p53 ubiquitination, leading to the reverse of the protective effect caused by laminar flow (L-flow) in human umbilical vein endothelial cells (HUVECs) exposed to 15d-PGJ2. BIX02189 (10 uM) inhibits ERK5 phosphorylation, and reduces myocyte enhancer factor 2 (MEF2) transcriptional activity in neonatal rat cardiomyocytes (NRCMs) stimulated by isoproterenol. BIX02189 enhances the sorbitol induced apoptosis in NRCMs, confirming the protective role of ERK5 in cardiomyocytes.
In vivo
Cell Data
cell lines：B16F10, A549, and HT29 cells
Concentrations：Dissolved in DMSO, final concentration ~10 μM
Incubation Time：Pretreatment for 1.5 hours
Powder Purity:≥99%
规格
英文别名
(Z)-3-((3-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-N,N-dimethyl-2-oxoindoline-6-carboxamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
BIX 02189
生化机理
BIX02189 是 MEK5 的选择性抑制剂，IC50 为 1.5 nM；在无细胞实验中，它也能抑制 ERK5 的催化活性，IC50 为 59 nM，但对密切相关的激酶 MEK1、MEK2、ERK2 和 JNK2 没有抑制作用。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
丝裂原活化蛋白激酶 7 抑制剂；丝裂原活化蛋白激酶激酶 5 抑制剂；转化生长因子 beta 受体 1 抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CN(C)CC1=CC(=CC=C1)N=C(C2=CC=CC=C2)C3=C(NC4=C3C=CC(=C4)C(=O)N(C)C)O
关联CAS
MeSH Entry Terms
BIX 02189;BIX-02189;BIX02189
分子量
440.54
Reaxy-Rn
60405313
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=60405313&ln=
技术文档
高级数据
关联靶点（人）
TGFBR1
Tchem
TGF-β受体1型(TGF-beta receptor type-1)
(1 活性数据)
MAPK7
Tchem
丝裂原活化蛋白激酶 7(Mitogen-activated protein kinase 7)
(1 活性数据)
MAP2K5
Tchem
双特异性丝裂原活化蛋白激酶激酶 5(Dual specificity mitogen-activated protein kinase kinase 5)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 48 mg/mL warmed with 50ºC Water: bath (196.53 mM); Water: Insoluble; Ethanol: Insoluble;
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
Copyright © 2023至今 上海阿拉丁生化科技股份有限公司 保留所有权利。
危险品化学品经营许可证（带存储）