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.

LY294002 (5 μM) completely inhibits the phosphorylation of PKB In HepG2 cells. LY294002 (5 μM) is also shown to block 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.

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).

DMSO : 14.9 mg/mL (48.48 mM; Need ultrasonic and warming)

• 1.

  Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (8.13 mM); Clear solution

• 2.

  Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (8.13 mM); Clear solution

• 3.

  Add each solvent one by one:  10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (8.13 mM); Clear solution