In vitro
LY294002 completely and specifically abolished PI3K activity with IC50 of 1.40 uM, by binding ATP binding site of PI3K, but did not inhibit PtdIns 4-kinase. LY294002 was shown to completely abolish PtdIns 3-kinase activity in fMet-Leu-Phe-stimulated human neutrophils, as well as inhibit proliferation of smooth muscle cells in cultured rabbit aortic segments. LY294002 partially inhibited insulin stimulated glucose uptake, amino acid uptake and protein synthesis, while it completely inhibited insulin stimulation of DNA synthesis and p70 S6 kinase activation. The autokinase activity of mTOR was also sensitive to the structurally distinct PI 3-kinase inhibitor, LY294002, at concentrations 1-30 uM, nearly identical to those required for inhibition of the lipid kinase activity of the mammalian p85-p110 heterodimer.
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