IC-87114 selectively inhibits PI3Kδ, and is not sensitive to PI3Kα, β, or γ. In human neutrophils, IC-87114 (5 μM) potently inhibits N-formyl-methionyl-leucyl-phenylalanine (fMLP)-stimulated phosphatidylinositol triphosphate (PIP3) biosynthesis and chemotaxis. In human acute myeloid leukemia (AML) blast cells, such as bone marrow mononuclear cells (BMMCs), IC-87114 (10 μM) inhibits both constitutive and Flt-3-stimulated Akt phosphorylation and cell proliferation. It is also found that IC-87114 (5 μM–30 &mui;M) inhibits SCF- or IL-3-stimulated BMMC responses, which are not observed in PI3Kδ mutant (p110δD910A) cells.
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