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Beschreibung

A cell-permeable phenylacetate based compound that specifically blocks the Nur77-p38alpha interaction by directly targeting the ligand-binding domain of Nur77 (~1 to 10 µ,M) and impedes Nur77 phosphorylation by p38alpha. Does neither modulate p38alpha kinase activity nor affects the stability of the p38alpha-Nur77 complex. Inhibits p65 binding to DNA and blocks LPS-induced (100 ng/ml) NF-kappaB activity in RAW264.7 cells (IC50 = 1.6 µ,M), but does not affect the interaction between Nur77 and p65. Shown to reduce IL-6 concentration and prolong the lifespan of wild type mice treated with LPS. Also increases the survival rate of wild-type mice subjected to cecal ligation and puncture (CLP)-induced sepsis., A cell-permeable phenylacetate based compound that specifically blocks the Nur77-p38alpha interaction by directly targeting the ligand-binding domain of Nur77 (~1 to 10 µ,M) and impedes Nur77 phosphorylation by p38alpha. Does neither modulate p38alpha kinase activity nor affects the stability of the p38alpha-Nur77 complex. Inhibits p65 binding to DNA and blocks LPS-induced (100 ng/ml) NF-kappaB activity in RAW264.7 cells (IC50 = 1.6 µ,M), but does not affect the interaction between Nur77 and p65. Shown to reduce IL-6 concentration and prolong the lifespan of wild type mice treated with LPS. Also increases the survival rate of wild-type mice subjected to cecal ligation and puncture (CLP)-induced sepsis. Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.