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.

Signaling Pathways >> PI3K/Akt/mTOR >> PI4K

Research Areas >> Cancer

PI4KIIIβ:7 nM (IC50)

PI4KIIIα:2.6 μM (IC50)

PI3Kδ:152 nM (IC50)

PI3Kγ:1046 nM (IC50)

PI3Kα:2 μM (IC50)

PI3KC2γ:1 μM (IC50)

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.

3-Methyladenine | LY294002 | Wortmannin | Alpelisib (BYL719) | BKM120 | Eganelisib(IPI-549) | BAY 80-6946 (Copanlisib) | Idelalisib (CAL-101) | Dactolisib (BEZ235) | Quercetin | SAR-405 | GDC-0941 | 740 Y-P | LY3023414 | 1,3-Dicaffeoylquinic acid