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Description

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