SMALL MOLECULES

Contributor Information
- Name Martin Swarbrick
- Institute Cancer Research Technology AstraZeneca Metabolism Alliance Team
Tool Details
- Tool name: PI4K beta Inhibitor Small Molecule (Tool Compound)
- Molecular formula: C23H25N5O4S2
- Tool type: Small molecules
- Tool sub-type: Inhibitor
- Purpose: Inhibitor
- Molecular weight of the target: 499.13
- Description: Potent and selective small molecule inhibitor of PI4K?, an isoform mainly associated with the Golgi complex where it functions in the generation of Golgi-derived carriers. In addition to the Golgi apparatus, PI4K? has also been visualised on lysosomes where it functions to maintain lysosomal membrane integrity. In a cellular environment, inhibition of PI4K? does not lead to a reduction in phosphatidylionositol-4-phosphate and phosphatidylionositol-4,5-biphosphate concentration
- Research area: Cancer
- Selectivity: 5.1 (PI4KÎą); 4.7 (PI3KÎą); <4.0 (PIP5KÉŁ); no activity against any kinase in the Millipore kinase panel (259 kinases; tested at 1ÂľM)
- IC50: 7.8 (PI4Kβ)
- Additional notes: Compound 3 (PMID: 24366037). AstraZeneca Alliance.
- For Research Use Only
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References
- • Raubo et al. 2015. Bioorg Med Chem Lett. 25(16):3189-93. PMID: 26087940. Waring et al. 2014. Chem Commun (Camb). 50(40):5388-90. PMID: 24366037.