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Beschreibung

A cell permeable, ATP-competitive and selective tolyl quinazolinone inhibitor of PI 3-Kdelta (IC50 = 7 nM, 1300 nM, 85000 nM, and 740 nM for PI 3-Kdelta PI 3-Kgamma PI 3-Kalpha and PI 3-Kbeta, respectively) in an enzymatic assay with an EC50 = 16 nM for PI 3-Kdelta and 2.7 µ,M for PI 3-Kgamma in a cell based assay. It elicits an inflammatory marker suppression effect in co-cultures of HUVEC and PBMCs under superantigen stimulated conditions. This compound, at concentrations between 370 nM and 10 µ,M, leads to a dose-dependent decrease in E-selectin expression. Furthermore, it is not cytotoxic to HUVEC cells., A cell permeable, ATP-competitive and selective tolyl quinazolinone inhibitor of PI 3-Kdelta (IC50 = 7 nM, 1300 nM, 85000 nM, and 740 nM for PI 3-Kdelta, PI 3-Kgamma PI 3-Kalpha and PI 3-Kbeta, respectively) in an enzymatic assay with an EC50 = 16 nM for PI 3-Kdelta and 2.7 µ,M for PI 3-Kgamma in a cell based assay. It elicits an inflammatory marker suppression effect in co-cultures of HUVEC and PBMCs under superantigen stimulated conditions. This compound, at concentrations between 370 nM and 10 µ,M, leads to a dose-dependent decrease in E-selectin expression. Furthermore, it is not cytotoxic to HUVEC cells.