产品说明
一般描述
A cell-permeable phenylacetate based compound that specifically blocks the Nur77-p38α interaction by directly targeting the ligand-binding domain of Nur77 (~1 to 10 µM) and impedes Nur77 phosphorylation by p38α. Does neither modulate p38α kinase activity nor affects the stability of the p38α-Nur77 complex. Inhibits p65 binding to DNA and blocks LPS-induced (100 ng/ml) NF-κB activity in RAW264.7 cells (IC50 = 1.6 µM), but does not affect the interaction between Nur77 and p65. Shown to reduce IL-6 concentration and prolong the lifespan of wild type mice treated with LPS. Also increases the survival rate of wild-type mice subjected to cecal ligation and puncture (CLP)-induced sepsis.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
A cell-permeable phenylacetate based compound that specifically blocks the Nur77-p38α interaction by directly targeting the ligand-binding domain of Nur77 (~1 to 10 µM) and impedes Nur77 phosphorylation by p38α. Does neither modulate p38α kinase activity nor affects the stability of the p38α-Nur77 complex. Inhibits p65 binding to DNA and blocks LPS-induced (100 ng/ml) NF-κB activity in RAW264.7 cells (IC50 = 1.6 µM), but does not affect the interaction between Nur77 and p65. Shown to reduce IL-6 concentration and prolong the lifespan of wild type mice treated with LPS. Also increases the survival rate of wild-type mice subjected to cecal ligation and puncture (CLP)-induced sepsis.
生化/生理作用
Cell permeable: yes
Primary Target
Nur77
Reversible: yes
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Li, L., et al. 2015. Nat. Chem. Biol.11, 339.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C22H34O5 |
分子量 | 378.50 |
产品性质
质量水平 | 100 |
测定 | ≥97% (HPLC) |
形式 | solid |
效能 | 1.6 μM IC50 |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | white |
溶解性 | DMSO: 100 mg/mL |
储存温度 | −20℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |