IC-87114

Description: IC-87114 is a novel, potent, selective and ATP-competitive PI3Kdelta inhibitor (p110delta-selective) with potential anticancer activity. It has an IC50 of 0.5 uM for inhibiting PI3Kdelta in a cell-free assay, which is 58-fold more selective for PI3Kdelta over PI3Kgamma, and > 100-fold more selective than PI3Kalpha/beta. It has been reported that IC87114 reduced FMLP-induced PIP3 synthesis and chemotaxis in neutrophils. IC87114 also blocked TNF1alpha-stimulated elastase exocytosis from neutrophils in a mouse model of inflammation. A role for PI3Kdelta in TNFalpha-induced signaling was demonstrated by a reduction in Akt-phosphorylation and PDK1 enzyme activity upon treatment of this cell type with IC87114. In human memory T cells, IC87114 largely inhibited T-cell receptor-induced PI(3)K signaling by both naive and effector.

References: Nat Chem Biol. 2010 Feb; 6(2):82-3; Blood. 2004 May 1; 103(9):3448-56.