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PI4K beta Inhibitor Small Molecule (Tool Compound)

Info

Catalogue Number 153578
Type Inhibitor
Relevance Potent and selective small molecule inhibitor of PI4Kβ, an isoform mainly associated with the Golgi complex where it functions in the generation of Golgi-derived carriers. In addition to the Golgi apparatus, PI4Kβ has also been visualised on lysosomes where it functions to maintain lysosomal membrane integrity. In a cellular environment, inhibition of PI4Kβ does not lead to a reduction in phosphatidylionositol-4-phosphate and phosphatidylionositol-4,5-biphosphate concentration
On Target IC50 7.8 (PI4Kβ)
Selectivity 5.1 (PI4Kα); 4.7 (PI3Kα); <4.0 (PIP5Kɣ); no activity against any kinase in the Millipore kinase panel (259 kinases; tested at 1µM)
Molecular Formula C23H25N5O4S2
Molecular Weight (g/mol) 499.13
Solubility 5 µM
Research Area Cancer
Notes Compound 3 (PMID: 24366037). AstraZeneca Alliance.

References

There are 4 reference entries for this reagent.

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References: 4 entries

Raubo et al. 2015. Bioorg Med Chem Lett. 25(16):3189-93. PMID: 26087940.

Discovery of potent, selective small molecule inhibitors of α-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIα).

Europe PMC ID: 26087940

Waring et al. 2014. Chem Commun (Camb). 50(40):5388-90. PMID: 24366037.

Potent, selective small molecule inhibitors of type III phosphatidylinositol-4-kinase α- but not β-inhibit the phosphatidylinositol signaling cascade and cancer cell proliferation.

Europe PMC ID: 24366037


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References: 4 entries

Raubo et al. 2015. Bioorg Med Chem Lett. 25(16):3189-93. PMID: 26087940.

Discovery of potent, selective small molecule inhibitors of α-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIα).

Waring et al. 2014. Chem Commun (Camb). 50(40):5388-90. PMID: 24366037.

Potent, selective small molecule inhibitors of type III phosphatidylinositol-4-kinase α- but not β-inhibit the phosphatidylinositol signaling cascade and cancer cell proliferation.


Add a reference

Inventor Information