PI4K alpha Inhibitor Small Molecule (Tool Compound)

Potent, small molecule inhibitor of PI4Ka, with no significant activity towards related kinases in the pathway

Contributors

Inventor Institute
Martin Swarbrick Cancer Research Technology AstraZeneca Metabolism Alliance Team
Cat. #: 153579
Tool sub type: Inhibitor
Research Fields: Drug development
Purpose: Inhibitor
Product description: Potent, small molecule inhibitor of PI4Ka, with no significant activity towards related kinases in the pathway. In a cellular environment, inhibition of PI4Ka 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.
Additional notes: Compound 7 (PMID: 24366037). AstraZeneca Alliance. Purity >99%
Molecular weight: 499.13
Selectivity: 5.9 (PI4Kβ); 5.2 (PI3Kι); <4.0 (PIP5Kɣ); activity against only 3 kinases in the Millipore kinase panel (FGR 98%; ZIPK 72%; STK17A 68%; 259 kinases; tested at 1¾M)
Shipping conditions: Dry Ice
Solubility: 22 ľM
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

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