LY294002 | CAS:154447-36-6

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Name:LY294002; NSC 697286; SF 1101
Cat. No. :CS-0150
CAS No. :154447-36-6
Formula:C19H17NO3
M. Wt. : 307.34
Solubility:DMSO: 14.9 mg/mL

LY294002 is a broad-spectrum inhibitor of PI3K, with IC50 of 0.5/0.57/0.97 μM for PI3Kα/δ/β, respectively, also potently inhibits CK2 with IC50 of 98 nM. IC50 & Target: IC50: 0.5/0.57/0.97 μM (PI3Kα/δ/β)[1]IC50: 98 nM (CK2)[2]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]. 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].

Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58. Ueda K, et al. Differential effects of LY294002 and wortmannin on neurons and vascular endothelial cells in the rat retina. Pharmacol Rep. 2013;65(4):854-62. Gharbi SI, et al. Exploring the specificity of the PI3K family inhibitor LY294002. Biochem J. 2007 May 15;404(1):15-21. Jiang H, et al. Phosphatidylinositol 3-kinase inhibitor(LY294002) induces apoptosis of human nasopharyngeal carcinoma invitro and in vivo. J Exp Clin Cancer Res. 2010 Apr 22;29:34.