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PI4K alpha Inhibitor Small Molecule (Tool Compound)

Info

Catalogue Number 153579
Type Inhibitor
Relevance Potent, small molecule inhibitor of PI4Kα, with no significant activity towards related kinases in the pathway. In a cellular environment, inhibition of PI4Kα led to a reduction in phosphatidylionositol-4-phosphate and phosphatidylionositol-4,5-biphosphate concentration, causing inhibition of inositol-1-phosphate formation and inhibition of proliferation in a panel of cancer cell lines.
On Target IC50 8.2 (PI4Kα)
Selectivity 5.9 (PI4Kβ); 5.2 (PI3Kα); <4.0 (PIP5Kɣ); activity against only 3 kinases in the Millipore kinase panel (FGR 98%; ZIPK 72%; STK17A 68%; 259 kinases; tested at 1µM)
Molecular Formula C23H25N5O4S2
Molecular Weight (g/mol) 499.13
Solubility 22 µM
Research Area Cancer
Notes Compound 7 (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