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Beschreibung

A cell-permeable thiazolidinedione compound that acts as a potent, selective, and ATP-competitive inhibitor of phosphatidylinositol 3-kinase gamma (PI 3-Kgamma) (Ki = 7.8 nM, IC50 = 8 nM, 60 nM, 270 nM, 300 nM for p110-gamma, alpha, beta and delta-isoforms, respectively). Does not affect the activity of a wide panel of kinases, receptors, enzymes, and ion channels even at concentrations as high as 1 µ,M. Selectively blocks MCP-1-, but not CSF-1-, dependent Akt phosphorylation and chemotaxis in primary Pik3cg+/+ murine monocytes and in a human monocytic cell line THP-1 (IC50 = 181 nM). Also shown to exhibit in vivo efficacy in reducing neutrophil chemotaxis in murine peritonitis and arthritis models., A cell-permeable, potent, selective, and ATP-competitive inhibitor of phosphatidylinositol 3-kinase gamma (PI 3-Kgamma) (Ki = 7.8 nM, IC50 = 8 nM, 60 nM, 270 nM, 300 nM for p110-gamma, alpha, beta and delta-isoforms, respectively). Does not affect the activity of a wide panel of kinases, receptors, enzymes, and ion channels even at concentrations as high as 1 µ,M. Selectively blocks MCP-1-, but not CSF-1-, dependent Akt phosphorylation and chemotaxis in primary Pik3cg+/+ murine monocytes and in a human monocytic cell line THP-1 (IC50 = 181 nM). Also shown to exhibit in vivo efficacy in reducing neutrophil chemotaxis in murine peritonitis and arthritis models.