Description
LY294002 is a selective phosphatidylinositol 3-
kinase (PI3K) inhibitor with a 2.7-
fold greater potency than quercetin. LY294002 inhibits purified PI3K with an IC
50 of 1.4 μM.
Uses
LY 294002 is a Phosphatidylinositol 3-kinase (PI3K) inhibitor which has shown to block the formation of tumor tissues in bone marrow cavity an abolish multiple myeloma (MM) induced osteoclast formation and osteolysis in SCID mice.
Uses
A potent blocker of PI 3-kinase/Akt signaling.
Uses
LY 294002 Hydrochloride is a highly selective inhibitor of Phosphatidylinositol 3-kinase (PI3K). It is a salt analogue of LY 294002 (L486590).
Definition
ChEBI: LY294002 is a chromone substituted with a phenyl group at position 8 and a morpholine group at position 2. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor, an autophagy inhibitor and a geroprotector. It is a member of chromones, a member of morpholines and an organochlorine compound.
Biological Activity
A highly selective inhibitor of phosphatidylinositol 3-kinase (IC 50 values are 0.31, 0.73, 1.06 and 6.60 μ M for PI3K β , PI3K α , PI3K δ and PI3K γ respectively). Inhibits proliferation and induces apoptosis in human colon cancer cells in vitro and in vivo .
Background
LY294002 was shown to act in vivo as a highly selective inhibitor of phosphatidylinositol 3 kinase. When used at a concentration of 50 μM, it specifically abolished PI3 kinase activity 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.
References
[1] C. VLAHOS. A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY294002).[J]. The Journal of Biological Chemistry, 1994, 93 1: 5241-5248. DOI:
10.1016/s0021-9258(17)37680-9.
[2] SEVERINE I GHARBI. Exploring the specificity of the PI3K family inhibitor LY294002.[J]. ACS Applied Energy Materials, 2007: 15-21. DOI:
10.1042/BJ20061489.
[3] SANCHEZMARGALET V. Role of Phosphatidylinositol-3-Kinase in Insulin Receptor Signaling: Studies with Inhibitor, LY294002[J]. Biochemical and biophysical research communications, 1994, 204 2: Pages 446-452. DOI:
10.1006/bbrc.1994.2480.
