PI4KIIIbeta-IN-9

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. IC50 & Target: IC50: 7 nM (PI4KIIIβ), 152 nM (PI3Kδ), 1046 nM (PI3Kγ), ~1 µM (PI3KC2γ), ~2 µM (PI3Kα), ~2.6 µM (PI4KIIIα), >20 μM (PI3Kβ), >20 μM (VPS34), >20 μM (PI4K2α), >20 μM (PI4K2β)^[1] In Vitro: 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].