Physical Appearance:  Off-white-pale yellow solid (m.p. 182-184°C)

Molecular Formula:  C₁₉H₁₇NO₃

Molecular Weight:  307.4

Purity:  99% (TLC)

Solubility:  Soluble in DMSO (25 mg/ml warm) and ethanol (25 mg/ml warm)

Storage:  Store, as supplied, at –20°C for up to 1 year. Store solutions at -20°C for up to 3 months.

Description:  LY294002 (PI3 Kinase Inhibitor) was shown to act in vivo as a highly selective inhibitor of phosphatidylinositol 3 (PI3) kinase. When used at a concentration of 50 µM, it specifically abolished PI 3-kinase activity (IC₅₀=0.43 µg/ml; 1.40 µM) but did not inhibit other lipid and protein kinases such as PI4 kinase, PKC, MAP kinase or c-Src. LY294002 is soluble in DMSO or ethanol. For use with in vitro or cell-based assays, it may be diluted into aqueous buffers to yield the desired concentrations. For experiments with cultured cells, KangChen recommends treating the cells with LY294002 for one hour prior to, and for the duration of, the stimulation. LY294002 has been shown to block PI3 kinase–dependent Akt phosphory-lation and kinase activity.

Directions for Use: For 10 mM stock, reconstitute 1 mg in 325 µl DMSO. For 50 mM stock, reconstitute 1 mg in 65 µl DMSO. Store aliquots at -20°C. Store solutions at -20°C for up to 3 months.

References:

1.      C.J.Vlahos et al. J.Biol.Chem. 1994 269 5241

2.      V.Sanchez Margalet et al. Biochem.Biophys.Res.Commun. 1994 204 446

3.      T.J.Kovacsovics et al. J.Biol.Chem. 1995 270 11358

4.      R.Yao and G.M.Cooper Science 1995 267 2003

The pharmacological and toxicological properties of this product have not been fully investigated.  Exercise caution in use and handling.  This product must not be used in humans.