PIK-294 has been used as PI3K inhibitor in drug combination studies and their synergy quantification using the Chou-Talalay method.[1]
生化/生理作用
PIK-294 is a highly selective inihibitor of the phosphoinositide 3-kinase (PI3K) p110δ with an IC50 value of 10 nM compared to IC50 values of 10 μM, 490 nM and 160 nM for PI3Kα/β/γ, respectively. PIK-294 has been used to help distinguish the unique roles of the various PI3-K isoforms. For example, in a study of CXCL8-induced neutrophil migration, PIK-294 inhibited both chemokinetic and chemotactic CXCL8-induced migration whereas PI3Kγ inhibitor AS-605240 markedly reduced CXCL8 induced chemokinetic migration but had no effect on CXCL8 induced chemotactic migration.
PIK-294 is a highly selective inihibitor of the phosphoinositide 3-kinase (PI3K) p110δ.
Toxicology in vitro : an international journal published in association with BIBRA, 65, 104777-104777 (2020-01-22)
The serine/arginine protein kinases respond to the EGFR-PI3K-AKT signaling module in the context of pre-mRNA alternative splicing regulation. These enzymes (notably SRPK1 and SRPK2) have been found dysregulated in a variety of cancers, which suggests them as promising drug targets
