White solid. PROTECT FROM LIGHT. PROTECT FROM MOISTURE. PACKAGED UNDER INERT GAS. A cell-permeable tetrazolopyridazine-phenylsulfoxide compound that displays anti-inflammatory properties. Acts as a highly selective, irreversible inhibitor of IkBaee ubiquitination (IC50 = 2.3 µM). Blocks NF-kB-dependent cytokine expression in human PBMNs (IC50’s ~ 700 nM for TNF-a, IL-1b, and IL-6 inhibition) and rats. Does not inhibit SCFbTRCP(IkBa ubiquitin ligase)-mediated b-catenin ubiquitination in Jurkat cells. At 10 µM concentrations, also inhibits the activities of 5-lipoxygenase (by 89%) and EGFR kinase (by 63%). Purity: ≥95% by HPLC. CAS 62645-28-7. Ref.: Swinney, D.C., et al. 2002. J. Biol. Chem. 277, 23573. |
