Hassett, Matthew R.; Sternberg, Anna R.; Roepe, Paul D. published the artcile< Inhibition of Human Class I vs Class III Phosphatidylinositol 3'-Kinases>, Quality Control of 1223001-51-1, the main research area is inhibition class I III isoenzyme phosphatidylinositol kinase PI3K.
Most investigations of phosphatidylinositol 3′-kinase (PI3K) drug inhibition have been via assays based on ADP appearance or ATP consumption (e.g. Liu, Q. et al. (2011) J. Med. Chem. 54, 1473-1480). However, at least some PI3K isoforms show basal ATPase activity in the absence of PI lipid substrate(s), which may complicate quantification of drug potency, isoform specificity of some drugs, and synergy for drug combinations. In this study, we probe the class I vs. class III isoform specificity of a selected set of phosphatidylinositol 3′-kinase (PI3K) inhibitors using a simple, inexpensive, semi high-throughput assay that quantifies production of phosphatidylinositol 3′-phosphate (PI3P) from phosphatidylinositol (PI). Results are compared to previous data largely generated using ATPase activity assays. Good agreement between EC50 values computed via ATPase assays vs. the reported PI3P formation assay is found for most drugs, but with a few exceptions. Also, for the first time, drug inhibition of class I vs. class III enzymes is compared side-by-side with the same assay for the important class I specific inhibitors GSK2126458 (“”Omipalisib””) and NVP-BGT226 (“”BGT226″”) currently in clin. development for advanced solid tumors.
Biochemistry published new progress about Enzyme inhibition kinetics. 1223001-51-1 belongs to class naphthyridine, and the molecular formula is C24H15F3N4O, Quality Control of 1223001-51-1.
Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem