概述规格名称和识别符技术文档高级数据质检证书（CoA,COO,BSE/TSE 和分析图谱) 化学和物理性质安全和危险性（GHS）此产品的引用文献技术文档和文章溶液计算器

🧪

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 6 篇同行评审文献引用。

概述

BAY 11-7082是一种NF-κB抑制剂，抑制TNFα诱导的IκBα磷酸化，IC50为10 μM。同时对泛素化系统的组分也有抑制作用。An anti-inflammatory agent and NFκB inhibitor

Information

BAY 11-7082 (BAY 11-7821) is aNF-κBinhibitor, inhibits TNFα-inducedIκBαphosphorylation withIC50of 10 μM in tumor cells. BAY 11-7082 inhibitsubiquitin-specific protease USP7andUSP21with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 inducesapoptosi
In vitro

BAY 11-7082 completely and specifically abrogates NF-κB DNA binding, downregulating the NF-κB-inducible cytokine IL-6 and inducing apoptosis. BAY 11-7082 (< 8 μM) is able to effectively inhibit both basal and TNFα stimulated NFκB luciferase activity in a dose dependent manner. BAY 11-7082 (8 μM) strongly inhibits the rate of proliferation in NCI-H1703 cells. Bay 11-7082 (5 μM) rapidly and efficiently reduces the DNA binding of NF-kappaB in HTLV-I-infected T-cell lines and down-regulates the expression of the antiapoptotic gene, Bcl-x(L), whereas it has little effect on the DNA binding of another transcription factor, AP-1. Bay 11-7082-induced apoptosis of primary ATL cells is more prominent than that of normal peripheral blood mononuclear cells, and apoptosis of these cells is also associated with down-regulation of NF-kappaB activity. Bay 11-7082 (5 μM) selectively induces apoptosis of HTLV-I–infected T-cell lines associated with down-regulation of the expression of cyclin D1, cyclin D2, and Bcl-xL. BAY 11-7082 (100 μM) prevents the nuclear translocation of p65 elicited by NMDA and the NMDA-induced increase of NF-κB binding in mouse hippocampal slices. BAY 11-7082 prevents NMDA toxicity occurring in CA1 region of hippocampal slices with 40% neuroprotection at 20 μM and 70% neuroprotection at 100 μM. BAY 11-7082 at all concentrations tested significantly inhibits NF-κB p65 DNA-binding activity in adipose tissue, whereas in skeletal muscle, BAY 11-7082 at 50 μM and 100 μM significantly inhibits NF-κB p65 DNA-binding activity. BAY 11-7082 (100 μM) reduces IKK-β protein in human adipose tissue and skeletal muscle. BAY 11-7082 (100 μM) significantly decreases the release of TNF-α from adipose tissue, whereas the release of IL-6 and IL-8 is significantly inhibited at all concentrations of BAY 11-7082 tested. BAY 11-7082 (50 μM) significantly decreases the release of TNF-α, IL-6, and IL-8 in skeletal muscle. BAY 11-7082 is also found to inactivate the E2-conjugating enzymes Ubc (ubiquitin conjugating) 13 and UbcH7 and the E3 ligase LUBAC (linear ubiquitin assembly complex), and thus induces B-cell lymphoma and leukaemic T-cell death. ^[6]

In vivo

Cell Data

cell lines：

Concentrations：~8 μM

Incubation Time：12 hours

Powder Purity:≥99%

规格

英文别名

BAY 11-7821 | 2-Propenenitrile, 3-[(4-methylphenyl)sulfonyl]-, (2E)-

规格或纯度

Moligand™, 10mM in DMSO

英文名称

BAY 11-7082

生化机理

BAY 11-7082 (BAY 11-7821) 是一种 NF-κB 抑制剂，可抑制 TNFα 诱导的肿瘤细胞 IκBα 磷酸化，IC50 为 10 μM。BAY 11-7082 可抑制泛素特异性蛋白酶 USP7 和 USP21，其 IC50 分别为 0.19 μM 和 0.96 μM。BAY 11-7082 可诱导胃癌细胞凋亡和 S 期停滞。

储存条件

-80℃储存

运输条件

特低温运输

名称和识别符

EC号

805-917-7

分子类型

小分子

Isomeric SMILES

CC1=CC=C(C=C1)S(=O)(=O)/C=C/C#N

分子量