PIK-75 HCl (CAS 372196-77-5) is a potent selective inhibitor of the phosphoinositide 3-kinase (PI3K) p110 isoform exhibiting an IC50 of 5 8 nM In acute myeloid leukemia cells PIK-75 disrupts PI3K signaling by targeting p110 leading to loss of interaction between Bcl-xL and Bak and transient reduction of Cdk7/9 which diminishes Mcl-1 and enhances pro-apoptotic responses In endothelial and monocytic cells PIK-75 suppresses downstream PI3K pathways including AKT phosphorylation IKK activation and NF- B transcription thereby reducing expression of adhesion molecules and production of TNF- and IL-6 Additional studies report modulatory effects on CD38 expression in airway smooth muscle cells and promotion of insulin secretion in pancreatic -cells In vivo PIK-75 attenuates experimental colitis and inflammatory responses supporting its utility in studies of PI3K signaling apoptosis and inflammation