PI4KIIIbeta-IN-9 is a potent PI4KIIIβ inhibitor with an IC50 of 7 nM. PI4KIIIbeta-IN-9 also inhibits PI3Kδ and PI3Kγ with IC50s of 152 nM and 1046 nM, respectively.
PI4KIIIbeta-IN-9 (Compound 9) shows weak inhibition of PI3KC2γ (IC50 ~1 µM), PI3Kα (~2 µM), and PI4KIIIα (~2.6 µM) and <50% inhibition at concentrations up to 20 µM for PI4K2α, PI4K2β, and PI3Kβ. PI4KIIIbeta-IN-9 (Compound 9) forms a crescent shape that conforms to the active site of PI4KIIIβ. This molecule makes extensive contacts with PI4KIIIβ[1].
[1]. Rutaganira FU, et al. Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase IIIβ. J Med Chem. 2016 Mar 10;59(5):1830-9.