AS-252424

AS-252424 is a potent inhibitor of PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ IC50= 30 nM, PI3Ka IC50=940 nM, PI3Kb IC50=20,000 nM and PI3Kd IC50= 20,000 nM respectively. AS-252424 also inhibits C5a-mediated phosphorylation of Akt in RAW 264.7 macrophages with an IC50=230 nM. In a mouse model of peritonitis, PI 3-Kᵧ this compound inhibited neutrophil recruitment 35% at a dose of 10 mg/kg.