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PI4K alpha Inhibitor Small Molecule (Tool Compound)

Invented at Cancer Research Technology – AstraZeneca Metabolism Alliance Team

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.

Purity >99%

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