PX-316

PX-316 is a synthetic small molecule inhibitor of Akt (protein kinase B), a central node in the PI3K/Akt/mTOR signaling pathway that regulates cell survival, growth, and metabolism. Chemically classified as a D-3-deoxyphosphatidylinositol ether lipid analogue (PIELA), PX-316 was designed to mimic the natural substrate of Akt but lacks the 3-hydroxyl group required for phosphorylation by PI3K. It functions by binding to the pleckstrin homology (PH) domain of Akt, thereby preventing the kinase's translocation to the plasma membrane and its subsequent activation by upstream kinases. Preclinical studies demonstrated that PX-316 inhibits the phosphorylation of downstream targets such as GSK-3beta and exhibits antitumor activity in xenograft models of breast (MCF-7) and colon (HT-29) cancer. Developed by ProlX Pharmaceuticals, the compound was typically formulated with hydroxypropyl-beta-cyclodextrin for intravenous administration in research settings.

Other names

D-3-deoxyphosphatidylinositol ether lipidD3-deoxyphosphatidylinositol ether lipidD 3-deoxyphosphatidylinositol ether lipidD-3-deoxy-PI ether lipidD3-deoxy-PI ether lipidD 3-deoxy-PI ether lipid1-O-octadecyl-2-O-methyl-sn-glycero-3-phospho-(D-3-deoxy-myo-inositol)