AS252424, AS-252424

BackgroundAS-252424 has been described as a potent p110γ selective PI 3-kinase inhibitor (class Ib), which is capable of attenuating GPCR-mediated activation of AKT/PKB [1]. It has no effect on insulin signalling in liver cell lines [2].

References

1Pomel, V., Klicic, J., Covini, D., Church, D. D., Shaw, J. P., Roulin, K., Burgat-Charvillon, F., Valognes, D., Camps, M., Chabert, C., Gillieron, C., Francon, B., Perrin, D., Leroy, D., Gretener, D., Nichols, A., Vitte, P. A., Carboni, S., Rommel, C., Schwarz, M. K. and Ruckle, T. (2006) Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.Journal of Medicinal Chemistry 49, 3857-71

2Chaussade, C., Rewcastle, G. W., Kendall, J. D., Denny, W. A., Cho, K., Gronning, L. M., Chong, M. L., Anagnostou, S. H., Jackson, S. P., Daniele, N. and Shepherd, P. R. (2007) Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling.Biochem J 404, 449-58