PI4KIIIβ-IN-10

PI4KIIIβ-IN-10 is an inhibitor of PI4KIIIβ (IC₅₀ = 0.0036 µM).¹ It is selective for PI4KIIIβ over PI3Kγ, PI3Kδ, and vacuolar protein sorting 34 (VPS34; IC₅₀s = ~20, 0.72, and >20 µM, respectively). PI4KIIIβ-IN-10 inhibits the replication of hepatitis C virus (HCV) in a reporter assay using Huh7.5 cells (IC₅₀ = 1.3 µM). PI4KIIIβ-IN-10 reduces muscle endosome accumulation and crawling defects in Drosophila expressing a null mutation in Vap33, a homolog of a mutated protein found in patients with amyotrophic lateral sclerosis type 8 (ALS8).² It also reduces BODIPY-labeled C5 ceramide transport from the endoplasmic reticulum (ER) to the Golgi in HeLa cells in a ceramide transport protein (CERT)-dependent manner at 25 and 50 nM.³

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1. Rutaganira, F.U., Fowler, M.L., McPhail, J.A., et al. Design and structural characterization of potent and selective inhibitors of phosphatidylinositol 4 kinase IIIβ. J. Med. Chem. 59(5), 1830-1839 (2016).

2. Mao, D., Lin, G., Tepe, B., et al. VAMP associated proteins are required for autophagic and lysosomal degradation by promoting a PtdIns4P-mediated endosomal pathway. Autophagy 15(7), 1214-1233 (2019).

3. Crivelli, S.M., Giovagnoni, C., Zhu, Z., et al. Function of ceramide transfer protein for biogenesis and sphingolipid composition of extracellular vesicles. J. Extracell. Vesicles 11(6), e12233 (2022).