Description
AS-252424 is an inhibitor of p110γ PI3K that exhibits anti-inflammatory activity. In animal models of peritoneal inflammation, AS-252424 decreases leukocyte recruitment. In vascular smooth muscle cells, AS-252424 decreases endothelin A receptor-mediated activity of transient receptor potential canonical 1/5/6 channels (TRPC1/5/6) and potentiates related activity of TRPC3/7 channels.
References
Shi J, Ju M, Large WA, et al. Pharmacological profile of phosphatidylinositol 3-kinases and related phosphatidylinositols mediating endothelin(A) receptor-operated native TRPC channels in rabbit coronary artery myocytes. Br J Pharmacol. 2012 Aug;166(7):2161-75. PMID: 22404177.
Pomel V, Klicic J, Covini D, et al. Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma. J Med Chem. 2006 Jun 29;49(13):3857-71. PMID: 16789742.