tcsc0150 LY294002

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.

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].