IC-87114 is an ATP-competitive, purine-quinazoline-based inhibitor of PI3Kdelta with an IC50 of 0.5 uM. It is selective over other major isoforms of PI3K (PI3Ka = >100 uM; PI3Kb = 75 uM; PI3Kg = 29 uM) as well as a PIK-related kinases such as DNA-PK and mTOR. [1]
Studies with IC-87114 have assisted in showing that PI3Kdelta is responsible for fMLP-induced PIP3 generation in neutrophils and critical to chemotaxis, but not adhesion. Furthermore, inhibition of PI3Kdelta affects cell polarization and CD18 integrin-dependent chemotactic migration, but is less implicated in random movement. [1]