PI4K alpha Inhibitor Small Molecule (Tool Compound)
Invented at Cancer Research Technology – AstraZeneca Metabolism Alliance Team
- Datasheet
- References (4)
- Inventor Info
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: 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
Add a reference
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
