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LY294002 2-(4-Morpholinyl)-8-phenyl-4H-1- benzopyran-4-one

LY294002 2-(4-Morpholinyl)-8-phenyl-4H-1- benzopyran-4-one

Cat no: L1756

Supplier: United States Biological
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LY294002 is a potent and specific cell-permeable inhibitor of phosphatidylinositol 3-kinase (PI3-kinase). LY294002 at a concentration of 50uM completely abolishes the PI3-K activity of intact neutrophils stimulated with fMet-Leu-Phe, without apparent cell toxicity. While concentration of 50uM is observed to be efficacious for inhibiting PI3-K activity in stimulated neutrophils, this concentration produces no significant inhibition of other kinases including PKC, PKA, MAP kinase, S6 kinase, EGF receptor tyrosine kinase, Src, PI4-kinase, diacylglycerol kinase, or rabbit kidney ATPase. This compound is a useful tool for identifying cellular event that are regulated by the PI3-kinase/Akt axis and is observed to induce apoptosis in many cell types by blocking the PI3-kinase/Akt anti-apoptotic pathway. Molecular Weight: ~307.4 Biological Activity: IC50=1.4uM Solubility: DMSO (~25mg/ml), warm ethanol (~25mg/ml) Storage and Stability: Lyophilized powder may be stored at -20 degrees C. Stable for 12 months at -20 degrees C. Reconstitute with sterile dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20 degrees C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
Catalogue number: L1756
Size: 5mg
Form: Supplied as a off-white to pale-yellow lyophilized powder. Reconstitute with sterile dH2O to 0.1-1mg/ml.
Purity: ~99% (TLC)
References: 1. Vlahos, C.J., et al. (1994) A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4- morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY294002). J. Biol. Chem. 269(7):5241-5248. 2. Sanchez-Margalet, V., et al. (1994) Role of phosphatidylinositol-3-kinase in insulin receptor signaling: studies with inhibitor, LY294002. Biochem. Biophys. Res. Commun. 204(2):446-452. 3. Bancroft, C.C., et al. (2002) Effects of pharmacologic antagonists of epidermal growth factor receptor, PI3K and MEK signal kinases on NF-kappaB and AP-1 activation and IL-8 and VEGF expression in human head and neck squamous cell carcinoma lines. Int. J. Cancer 99(4):538-548. 4. Williamson, R., et al. (2002) Rapid tyrosine phosphorylation of neuronal proteins including tau and focal adhesion kinase in response to amyloid-beta peptide exposure: involvement of Src family protein kinases. J. Neurosci. 22(1):10-20. 5. Shoba, L.N., et al. (2001) LY294002, an inhibitor of phosphatidylinositol 3-kinase, inhibits GHmediated expression of the IGF-I gene in rat hepatocytes. Endocrinology 142(9):3980-3986.

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