Description
PIK-75 is a potent, isoform-selective p110alpha inhibitor with IC50 of 0.3nM, displays >100-fold selectivity over p110beta, p110delta and PI3K C2b; blocks the phosphorylation of PKB induced by insulin on both Ser473 and Thr308 in CHO-IR cell (IC50=78nM), inhibits PI3K activation associated with dramatic suppression of downstream signaling events, including AKT phosphorylation, IKK activation, and NF-kappaB transcription; potently and dose dependently inhibits in vitro and in vivo production of TNF-alpha and IL-6, diminishes the induced expression of human endothelial cell adhesion molecules (E-selectin, ICAM-1, and VCAM-1), and blocks human monocyte-endothelial cell adhesion; exhibits significant anti-tumor effectiveness in vivo