Ro106-9920

半岛bd体育手机客户端 说明

一般描述

A cell-permeable tetrazolopyridazine-phenylsulfoxide compound that displays anti-inflammatory properties. Acts as a highly selective, irreversible inhibitor of IκBαee ubiquitination (IC₅₀= 2.3 ?M). Also reported to prevent degradation of IκBαee in MM6 cells (complete inhibition at ~3-5 ?M). Shown to block NF-κB-dependent cytokine expression in human peripheral blood mononuclear cells (PBMN) (IC₅₀= 600-700 nM for TNF-α, IL-1β, and IL-6 inhibition). Also shown to lower circulating levels of TNFα in LPS-treated rats. Also shown to inhibit 5-lipoxygenase (89% inhibition) and EGFR kinase (63% inhibition) at higher concentrations (10 ?M).
A cell-permeable tetrazolopyridazine-phenylsulfoxide compound that displays anti-inflammatory properties. Acts as a highly selective, irreversible inhibitor of IκBαee ubiquitination (IC₅₀= 2.3 ?M). Blocks NF-κB-dependent cytokine expression in human PBMNs (IC₅₀’s = ~ 700 nM for TNF-α, IL-1β, and IL-6 inhibition) and rats. Does not inhibit SCF^βTRCP(IκBα ubiquitin ligase)-mediated β-catenin ubiquitination in Jurkat cells. At 10 ?M concentrations, also inhibits the activities of 5-lipoxygenase (by 89%) and EGFR kinase (by 63%).

包装

1 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Primary Target
IκBαee ubiquitination
Product does not compete with ATP.
Reversible: no
Target IC₅₀: 2.3 ?M against IκBαee ubiquitination

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 3 months at -70°C.

其他说明

Swinney, D.C., et al. 2002.J. Biol. Chem.277,23573.

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	C10H7N5OS
分子量	245.26

半岛bd体育手机客户端 性质

质量水平	100
测定	≥95% (HPLC)
形式	solid
manufacturer/tradename	Calbiochem?
储存条件	OK to freeze desiccated protect from light
颜色	white
溶解性	ethanol: 1 mg/mL DMSO: 25 mg/mL
运输	wet ice
储存温度	?70℃

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