LY294002

A classic, broad-spectrum PI3K inhibitor with IC50 of 0.5/0.57/0.97 uM for PI3Kα/δ/β, respectively; completely and specifically abolishes PI3K activity (IC50=1.4 uM), but does not inhibit PI4K or other lipid kinases; demonstrates growth-inhibitory and apoptosis-inducing effect in colon cancer cell lines, with decreased phosphorylated Akt Ser (473) ; suppresses tumor growth in mouse xenografts; also is a potent inhibitor of CK2 with IC50 of 98 nM. (In Vitro) :LY294002 (0-75 μM; 24 hours and 48 hours) remarkably decreases human nasopharyngeal carcinoma CNE-2Z cells in a dose-dependent fashion.LY294002 (0-75 μM; 24 hours and 48 hours) induces CNE-2Z cells apoptosis rate in dose-dependent.LY294002 (10-75 μM) significantly decreases p-Akt (S473) expression levels and up-regulates caspase-9 activity in CNE-2Z cells. Total Akt protein level is not difference with different concentration.LY294002 (5, 10, 100 μM; for 2 hours) treatment partially suppresses Lysophosphatidic acid (LPA) -induced (20 μM; for 4 hours) nuclear translocation of YAP, accompanied by a reduction in p-AKT levels. (In Vivo) :LY294002 (10, 25, 50, 75 mg/kg; i.p.; twice weekly; for 4 weeks) significantly reduces mean NPC tumor burden in a dose-dependent manner. LY294002 (10, 25 mg/kg) is less effective in decreasing tumor burden.LY294002 (1.2 mg/kg per day; i.p.; for 14 days) prevents Leptin (60 ug/kg) -induced adverse effects on spermatozoa in Sprague-Dawley rats.