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LY294002
Chemical compound / From Wikipedia, the free encyclopedia
LY294002 is a morpholine-containing chemical compound that is a potent inhibitor of numerous proteins, and a strong inhibitor of phosphoinositide 3-kinases (PI3Ks).[1] It is generally considered a non-selective research tool, and should not be used for experiments aiming to target PI3K uniquely.[2]
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Names | |
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Preferred IUPAC name
2-(Morpholin-4-yl)-8-phenyl-4H-1-benzopyran-4-one | |
Other names
2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one | |
Identifiers | |
3D model (JSmol) |
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ChEMBL | |
ChemSpider |
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PubChem CID |
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UNII | |
CompTox Dashboard (EPA) |
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Properties | |
C19H17NO3 | |
Molar mass | 307.349 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Two of these are the proto-oncogene serine/threonine-protein kinase (PIM1) and the phosphatidylinositol-4,5-bisphosphate 3-kinase P110 gamma|catalytic subunit gamma isoform.[3] With an IC50 of 1.4 μM it is somewhat less potent than wortmannin, another well-known PI3 kinase inhibitor. However, LY294002 is a reversible inhibitor of PI3K whereas wortmannin acts irreversibly.[4]
Application of LY294002 causes a substantial acceleration of MEPP frequency (150 μM) at the frog neuromuscular junction through a mechanism that is independent of intraterminal calcium. LY294002 causes the release of MEPPs through a perturbation of synaptotagmin function.[5]
LY294002 is also a BET inhibitor (e.g. of BRD2, BRD3, and BRD4).[6]