LY294002 is a selective, cell permeable, potent and specific inhibitor of phosphatidylinositol 3-kinase (IC50 = 1.4 μM; purified PI 3-kinase). It does not significantly inhibit PKC, PKA, MAP kinase, S6 kinase, EGFrK, c-src kinase, PI 4-kinase, DAG kinase or rabbit kidney ATPase at concentrations of 50 μM. Induces apoptosis. In intact neutrophils stimulated with fMet-Leu-Phe, LY294002 completely abolished PI 3-kinase activity at 50 μM without cell toxicity.
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1. Coronas-Serna JM, Fernández-Acero T, Molina M, Cid VJ. A humanized yeast-based toolkit for monitoring phosphatidylinositol 3-kinase activity at both single cell and population levels. Microbial Cell. 2018;5(12):545-54.2. Chang P, Walker MC, Williams RS. Seizure-induced reduction in PIP3 levels contributes to seizure-activity and is rescued by valproic acid. Neurobiol Dis. 2014;62:296-306.3. Fernández-Acero T, Rodr?guez-Escudero I, Vicente F, Monteiro MCn, Tormo JR, Cantizani J, et al. A Yeast-Based In Vivo Bioassay to Screen for Class I Phosphatidylinositol 3-Kinase Specific Inhibitors. Journal of Biomolecular Screening. 2012;17(8):1018-29.