PI 3-kinase p85α Inhibitors

Common PI 3-kinase p85α Inhibitors include, but are not limited to Wortmannin CAS 19545-26-7, LY 294002 CAS 154447-36-6, GDC-0941 CAS 957054-30-7, Quercetin CAS 117-39-5 and Autophagy Inhibitor, 3-MA CAS 5142-23-4.

PI 3-kinase p85α inhibitors are a specialized class of chemical agents designed for research purposes, focusing on the modulation of the phosphoinositide 3-kinase (PI3K) pathway, particularly through targeting the p85α regulatory subunit of PI3K. These inhibitors are crucial in the study of cellular processes and signal transduction pathways in various biochemical and molecular biology research fields. The p85α subunit plays a significant role in the PI3K enzyme family, involved in a range of cellular functions such as growth, proliferation, differentiation, motility, survival, and intracellular trafficking. Class I PI3Ks, the most studied group, are heterodimeric molecules composed of a regulatory (p85) and a catalytic (p110) subunit, with p85α stabilizing and regulating p110. It also aids in recruiting PI3K to the cell membrane upon activation by receptors like receptor tyrosine kinases (RTKs), leading to the phosphorylation of phosphatidylinositol (4,5)-bisphosphate (PIP2) into phosphatidylinositol (3,4,5)-trisphosphate (PIP3), a key second messenger.

The mechanism of action of PI 3-kinase p85α inhibitors varies, including direct inhibition, where the inhibitor binds to the p85α subunit, altering its conformation and interaction with the p110 subunit, thus reducing PI3K activation and PIP3 production. Indirect inhibition involves interference with the interaction between p85α and other signaling molecules or receptors, preventing PI3K complex activation at the cell membrane. Some inhibitors function allosterically, binding to sites other than the active site on p85α, inducing conformational changes that diminish enzyme activity. These inhibitors are invaluable in research for dissecting the PI3K signaling pathway, allowing the study of signal transduction and the effects of PI3K inhibition on cell behavior. They are also instrumental in investigating the role of PI3K signaling in disease mechanisms and probing the interactions between PI3K and other cellular proteins or pathways.