In vitro
As a potent, selective, and cell membrane permeable inhibitor, TGX-221 can inhibit PI3K p110beta with IC50 of 10 nM. TGX-221, acting as a competitive ATP antagonist, can also inhibit other isoforms of PI3K, but shows less potent inhibition. TGX-221 can inhibit PI3K-alpha, PI3K-gamma, and PI3K-delta with IC50 of 784 nM, 3240 nM and 65 nM, respectively. As TGX-221 was developed based on detailed structure and function analysis of LY294002, TGX-221 is similar to LY294002. TGX-221 had minimal inhibitory effect on Type II PI3K C2 and PI4K and showed >1,000-fold selectivity for PI3K p110 over a broad range of protein kinases. The inhibitory effects of TGX-221 were influenced by the concentration of ATP. TGX-221 inhibited shear-induced PI(3,4)P2 production in a dose-dependent manner.
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