Chemical Name: 2-(1-Piperazinyl)-8-phenyl-4H-1-benzopyran-4-one
Biological ActivityNegative control compound for LY 294002 PI 3-kinase inhibitory activity. Blocks voltage-gated potassium (Kv) channels (IC50 = 64.6 μM) and inhibits IL-1β-stimulated NF-κB activation, attenuating MCP-1 expression. Antiproliferative. Also inhibits the BET bromodomain proteins BRD2, BRD3 and BRD4.
Active Analog also available.
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The phosphatidylinositol 3-kinase inhibitor LY294002 potently blocks KV currents via a direct mechanism.
El-kholy et al.
FASEB J., 2003;17:720
LY294002 inhibits monocyte chemoattractant protein-1 expression through a phosphatidylinositol 3-kinase-independent mechanism.
Choi et al.
FEBS Letters., 2004;559:141
LY303511 (2-Piperazinyl-8-phenyl-4H-1-benzopyran-4-one) acts via phosphatidylinositol 3-kinase-independent pathways to inhibit cell proliferation via mammalian target rapamycin (mTOR)- and non-mTOR-dependent mechanisms.
Kristof et al.
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