| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| B407824-1ml |
1ml |
现货  |
|
| 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。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 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 |
| 产品介绍 |
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. 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 lines：B16F10, A549, and HT29 cells Concentrations：Dissolved in DMSO, final concentration ~10 μM Incubation Time：Pretreatment for 1.5 hours Powder Purity:≥99% |
| 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 | 1265916-41-3 |
| 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= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 48 mg/mL warmed with 50ºC Water: bath (196.53 mM); Water: Insoluble; Ethanol: Insoluble; |
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