AQX-200 series

The AQX-200 series is a group of preclinical-stage small molecule activators of the Src homology 2 domain-containing inositol 5-phosphatase 1 (SHIP1), developed by Aquinox Pharmaceuticals. SHIP1 is a phosphatase primarily expressed in hematopoietic cells that serves as a critical negative regulator of the phosphoinositide 3-kinase (PI3K) signaling pathway. By dephosphorylating phosphatidylinositol-3,4,5-trisphosphate (PIP3) into phosphatidylinositol-3,4-bisphosphate (PIP2), SHIP1 activation inhibits the recruitment of pleckstrin homology (PH) domain-containing proteins like Akt, thereby dampening pro-inflammatory signaling and cellular activation. The AQX-200 series was designed as a follow-on program to Aquinox's lead candidate, rosiptor (AQX-1125), with the goal of treating various inflammatory diseases.