Ro106-9920

Descrição detalhada : A cell-permeable tetrazolopyridazine-phenylsulfoxide compound that displays anti-inflammatory properties. Acts as a highly selective, irreversible inhibitor of IκBαee ubiquitination (IC50 = 2.3 microM). Also reported to prevent degradation of IκBαee in MM6 cells (complete inhibition at ~3-5 microM). 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 microM)., A cell-permeable tetrazolopyridazine-phenylsulfoxide compound that displays anti-inflammatory properties. Acts as a highly selective, irreversible inhibitor of IκBαee ubiquitination (IC50 = 2.3 microM). 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(IκB? ubiquitin ligase)-mediated β-catenin ubiquitination in Jurkat cells. At 10 microM concentrations, also inhibits the activities of 5-lipoxygenase (by 89%) and EGFR kinase (by 63%).
Sinónimos : Ro106-9920
Fórmula molecula r: C10H7N5OS
Armazenamento : -70C
Embalagem : 1X1MG