A cell-permeable tetrazolopyridazine-phenylsulfoxide compound that displays anti-inflammatory properties. Acts as a highly selective, irreversible inhibitor of IκBαee ubiquitination (IC50 = 2.3 µM). Also reported to prevent degradation of IκBαee in MM6 cells (complete inhibition at ~3-5 µM). 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 µM).
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 µM against IκBαee ubiquitination
包裝
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重構
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 3 months at -70°C.
其他說明
Swinney, D.C., et al. 2002. J. Biol. Chem.277, 23573.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Select different protease inhibitor types based on your needs to prevent protein degradation during isolation and characterization and safeguard proteins in sample prep.