Cas No.: | 154447-36-6 |
Chemical Name: | 2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |
Synonyms: | 2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one hydrochloride;LY 294002 hydrochloride;2-Morpholino-8-phenylchromone;LY 294002;2-Morpholino-8-phenyl-4H-chromen-4-one;LY240092;LY-294002;2-Morpholino-8-phenyl-4-oxo-4H-1-benzopyran;NSC 697286;SF 1101;8-Phenyl-2-(morpholin-4-yl)chromen-4-one;2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one;LY294002HCl;LY294002 (HCI Salt);LY294002, NSC 697286;InSolution? LY 294002;LY 294002, 99+%;LY294002;2-morpholin-4-yl-8-phenyl-4H-chromen-4-one;2-(morpholin-4-yl)-8-phenyl-4H-chromen-4-one;31M2U1DVID;2-MORPHOLIN-4-YL-7-PHENYL-4H-CHROMEN-4-ONE;4H-1-Benzopyran-4-one, 2-(4-morpholinyl)-8-phenyl-;InSolution™ LY 294002;2-morpholino-8-phenyl-chromen-4-one;AK162301;2-(morpholin-4-yl)-8-phenylchro |
SMILES: | O1CCN(CC1)C2OC3C(=CC=CC=3C4=CC=CC=C4)C(=O)C=2 |
Formula: | C19H17NO3 |
M.Wt: | 307.3432 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. It also inhibits CK2 with an IC50 of 98 nM. |
In Vivo: | Treatment with LY294002 (i.p.,50 mg/kg, 75 mg/kg) significantly reduces mean NPC tumor burden as compared with the control group. Treatment with 10 mg/kg or 25 mg/kg LY294002 is less effective in decreasing tumor burden. Mean NPC tumor burden treated with LY294002 is remarkably decreased in a dose-dependent manner, whereas mean body weight is no obvious difference between control and treated groups (LY294002, 10 mg/kg, 25 mg/kg, 50 mg/kg, and 75 mg/kg)[3]. |
In Vitro: | LY294002 (5 μM) completely inhibits the phosphorylation of PKB In HepG2 cells. LY294002 (5 μM) is also shown to block insulin-induced phosphorylation of PKB Ser473 in CHO-IR cells[1]. LY294002 is also a potent inhibitor of CK2 (casein kinase 2) with IC50 of 98 nM. LY294002 is also able to reduce the kinase activity of both isoforms of the serine/threonine kinases GSK3α and β[2]. When the CNE-2Z cell line is cultured in medium containing LY294002(0 μM, 10 μM, 25 μM, 50 μM, and 75 μM) for 24 h and 48 h, cell proliferation is remarkably decreased in a dose-dependent fashion[3]. |