AS-252424

AS-252424 is a potent and selective small molecule inhibitor of the gamma isoform of Class I phosphoinositide 3-kinase (PI3Kγ), with an IC50 of approximately 30 nM. It demonstrates high selectivity (over 30-fold) for PI3Kγ compared to the α, β, and δ isoforms. Developed as part of a series of thiazolidinedione derivatives, AS-252424 is primarily utilized as a chemical probe in preclinical research to investigate the role of PI3Kγ in inflammatory responses, immune cell trafficking, and oncology. In the context of pancreatic cancer, research has shown that AS-252424 can effectively induce apoptosis and alter global phosphorylation patterns, although its therapeutic potential may be hindered by adaptive resistance mechanisms like Akt reactivation, suggesting a need for combination strategies with other isoform-selective inhibitors.

Other names

5-[5-(4-Fluoro-2-hydroxy-phenyl)-furan-2-ylmethylene]-thiazolidine-2,4-dione