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Beschreibung
A cell-permeable thiazolidinedione compound that acts as a potent and ATP-competitive inhibitor of PI 3-Kgamma (Ki = 180 nM, IC50 = 250 nM). Exhibits great selectivity over PI 3-Kalpha (IC50 = 4.5 µ,M), PI 3-Kbeta and delta (IC50 >20 µ,M), and shows little effect towards a large panel of receptors, unrelated enzymes, ion channels, and 38 commonly studied kinases. Shown to block MCP-1-mediated monocyte chemotaxis in vitro and exhibit better in vivo efficacy than LY294002 (Cat. No. 440202 and 440204) in blocking RANTES- or thioglycollate-induced peritoneal neutrophil recruitment by oral administration in a murine peritonitis model.
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