Cat. #153579
PI4K alpha Inhibitor Small Molecule (Tool Compound)
Cat. #: 153579
Sub-type: Inhibitor
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Contributor
Inventor: Martin Swarbrick
Institute: Cancer Research Technology AstraZeneca Metabolism Alliance Team
Tool Details
*FOR RESEARCH USE ONLY
- Tool name: PI4K alpha Inhibitor Small Molecule (Tool Compound)
- Molecular formula: C23H25N5O4S2
- Tool sub type: Inhibitor
- 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.
- Purpose: Inhibitor
- 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)
- Iupac: >99%
- Molecular weight: 499.13
- Solubility: 22 ľM
- Additional notes: Compound 7 (PMID: 24366037). AstraZeneca Alliance. Purity >99%
Handling
- Purity: 499.13 g/mol
- Shipping conditions: Dry Ice
Target Details
- Ic50: 8.2 (PI4KÎą)
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
