Cayman Chemical | AS-252424 | Description (CAS 900515-16-4)

10009052 AS-252424

(CAS 900515-16-4)

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• See more Lipid Mediators; Inflammation; Signal Transduction

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Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of Pl at the 3 position to produce the second messengers PtdIns-(3,4)-P₂ and PtdIns-(3,4,5)-P₃. ^1,2,3 PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits. ⁴ AS-252424 is a potent inhibitor of PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ, α, β, and δ with IC₅₀ values of 30, 940, 20,000, and 20,000 nM respectively. ⁵ AS-252424 also inhibits C5a-mediated phosphorylation of Akt in RAW 264.7 macrophages with an IC₅₀ value of 0.23 µM. In a mouse model of peritonitis, AS-252424 inhibited neutrophil recruitment 35% at a dose of 10 mg/kg. ⁵

1 Rameh, L.E., Cantley, L.C. The role of phosphoinositide 3-kinase lipid products in cell function. J Biol Chem 274 8347-8350 (1999).

2 Vivanco, I., Sawyers, C.L. The phosphatidylinositol 3-kinase-AKT pathway in human cancer. Nature Reviews Cancer 2 489-501 (2002).

3 Hennessy, B.T., Smith, D.L., Ram, P.T., et al. Exploiting the PI3K/AKT pathway for cancer drug discovery. Nature Reviews Drug Discovery 4 988-1004 (2005).

4 Rückle, T., Schwarz, M.K., Rommel, C. PI3Kγ inhibition: Towards an 'aspirin of the 21^st century'?. Nature Reviews Drug Discovery 5 903-918 (2006).

5 Pomel, V., Klicic, J., Covini, D., et al. Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase γ J Med Chem 49, 3857-3871 (2006).

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Pricing updated 2010-03-19.
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