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).
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). 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 SCFβTRCP(IκBα ubiquitin ligase)-mediated β-catenin ubiquitination in Jurkat cells. At 10 µM concentrations, also inhibits the activities of 5-lipoxygenase (by 89%) and EGFR kinase (by 63%).
Biochem/physiol Actions
Cell permeable: yes
Primary Target IκBαee ubiquitination
Product does not compete with ATP.
Reversible: no
Target IC50: 2.3 µM against IκBαee ubiquitination
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 3 months at -70°C.
Other Notes
Swinney, D.C., et al. 2002. J. Biol. Chem.277, 23573.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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