LY294002, a morpholine-containing compound designed based on the flavonoid quercetin, is a potent and cell-permeable PI3K inhibitor, inhibiting PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively. Additionally, it inhibits BET (for example, BRD2, BRD3, and BRD4). It is more stable in solutions than the PI3K inhibitor Wortmannin. By acting on the ATP binding site of the catalytic subunit of PI3K, LY294002 is selective against p110α, p110β, p110γ and p110δ.
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