IC87114

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Description

IC87114 (PIK-293) is the first isoform-selective PI3K inhibitor. This quinazolinone purine inhibits p110δ (IC50=0.13µM) at mid-nanomolar concentrations and shows 100-1000-fold selectivity over other class I PI3Ks (p110α, p110β and p110γ ). The selectivity of IC87114 is remarkable given that the residues that line the ATP binding pocket of the class I PI3Ks are highly conserved. IC87114 down-regulated p-Akt and p-FOXO3a, reduced proliferation and induced apoptosis in AML primary cells overexpressing p110δ PI3K. Inhibition of PI3K delta with IC87114 blocked both fMLP- and TNF1 alpha-induced neutrophil superoxide generation and elastase exocytosis. The PI3K delta inhibitor IC87114 also blocked TNF1 alpha-stimulated elastase exocytosis from neutrophils in a mouse model of inflammation.

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