PI4K beta Inhibitor Small Molecule (Tool Compound)
Invented at Cancer Research Technology – AstraZeneca Metabolism Alliance Team
- Datasheet
- References (4)
- Inventor Info
Info
| Catalogue Number | 153578 |
| Type | Inhibitor |
| Relevance | Potent and selective small molecule inhibitor of PI4Kβ, an isoform mainly associated with the Golgi complex where it functions in the generation of Golgi-derived carriers. In addition to the Golgi apparatus, PI4Kβ has also been visualised on lysosomes where it functions to maintain lysosomal membrane integrity. In a cellular environment, inhibition of PI4Kβ does not lead to a reduction in phosphatidylionositol-4-phosphate and phosphatidylionositol-4,5-biphosphate concentration |
| On Target IC50 | 7.8 (PI4Kβ) |
| Selectivity | 5.1 (PI4Kα); 4.7 (PI3Kα); <4.0 (PIP5Kɣ); no activity against any kinase in the Millipore kinase panel (259 kinases; tested at 1µM) |
| Molecular Formula | C23H25N5O4S2 |
| Molecular Weight (g/mol) | 499.13 |
| Solubility | 5 µM |
| Research Area | Cancer |
| Notes | Compound 3 (PMID: 24366037). AstraZeneca Alliance. |
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
