REVIEW LY294002, a morpholine derivative of quercetin, is a potent inhibitor of phosphoinositide 3-kinases (PI3Ks). Two of these are the proto-oncogene serine/threonine-protein kinase (PIM1) and the phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform. With an IC50 of 1.4 µM it is somewhat less potent than wortmannin, another well-known early PI3 kinase inhibitor. However, LY294002 is a reversible inhibitor of PI3K whereas wortmannin acts irreversibly. 2-Morpholino-8-phenyl-4H-chromen-4-one LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97. LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. LY294002 demonstrates a remarkable growth-inhibitory and apoptosis-inducing effect in these colon cancer cell lines, with decreased expression of phosphorylated Akt (Ser473). LY294002 induces marked nuclear pyknosis and diminished cytoplasmic volume in the tumor cells. Thus, LY294002 markedly inhibits ovarian cancer cell proliferation in vitro. LY294002 induces specific G1 arrest in cell growth, leading to almost complete inhibition of melanoma cell proliferation and partial inhibition of MG-63 (osteosarcoma cell line) proliferation.
REFERENCES
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Vlahos, Chris J.; Matter, William F.; Hui, Kwan Y.; Brown, Raymond F. A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY294002), Journal of Biological Chemistry (1994), 269(7), 5241-8.
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Searl TJ, Silinsky EM. LY 294002 inhibits adenosine receptor activation by a mechanism independent of effects on PI-3 kinase or casein kinase II. Purinergic Signal. 2005 Dec;1(4):389-94. doi: 10.1007/s11302-005-0778-6.
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Phosphatidylinositol 3-kinase inhibitors: promising drug candidates for cancer therapy. Kong D, Yamori T.Cancer Sci. 2008 Sep;99(9):1734-40.
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Knight ZA. Small molecule inhibitors of the PI3-kinase family. Curr Top Microbiol Immunol. 2010;347:263-78.
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