A Specific Inhibitor of PI 3-Kinase
PI 3-kinase is an enzyme implicated in growth factor signal transduction by associating with receptor and non-receptor tyrosine kinases. LY-294002 is a potent and specific cell-permeable inhibitor of Pl 3-kinase that acts on the ATP-binding site of the enzyme. In in vitro assays it displays an IC50 of 1.4 μM on purified PI 3-kinase, but did not inhibit PKC, PKA, MAP kinase and PI 4-kinase. In fMet-Leu-Phe stimulated neutrophils, LY-294002 completely abolished PI 3-kinase activity at 50 μM. LY-294002 induces apoptosis in many cell types by blocking the PI3-K/Akt anti-apoptotic pathway. Thus LY-294002 is useful tool for identifying the biochemical events regulated by the PI3-K/Akt pathway. This pathway has important relevance to the cellular events involved in cancer.
Protein Kinase Inhibitors and Activators; PI3-Kinase Inhibitors
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