AS-252424 is a potent and selective small-molecule PI3Kgamma inhibitor. Oral administration of AS-252424 in a mouse model of acute peritonitis led to a significant reduction of leukocyte recruitment.
IC50 with 935 nM. When screening against 80 different Ser/Thr and Tyr kinases, AS-252424 doesn't show significant inhibit towards any of them at 10 μM except for CK2. AS-252424 inhibits C5a-mediated PKB/Akt phosphorylation in a concentration- dependent manner with submicromolar or low-micromolar IC50 value. AS-252424 inhibits MCP-1-mediated chemotaxis in wild-type primary monocytes in a concentration-dependent manner with an IC50 value of 52 μM, as well as in the monocytic cell line THP-1 with an IC50 value of 53 μM. AS252424 specifically blocks proliferation in the pancreatic cancer cell lines HPAF and Capan1, as assessed by cell counting. A recent research indicates 100 nM of AS-252424 significantly reduces [Ca2+]i, ICa and Ca2+ transients in HL-1 cardiomyocytes.
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Idelalisib; Almorexant HCL; IC-87114; Pictilisib; Pictilisib mesylate; XL147; PIK-90; Omipalisib; Buparlisib; TG100-115; A66; GSK2636771; CH5132799; 3-methyladenine; AS-604850