PIK-294 can inhibit p110-beta, p110-gamma and p110-delta with IC50 of 490 nM, 160 nM and 10 nM. PIK-294 was designed based on the inhibitor PI-103, a potent PI3K inhibitor. PIK-294 projects a m-phenol into ATP binding site. PIK-294 is 20- to 60-fold more potent than the parent compound, PIK-293. PIK-294 is one of the most potent p110delta-selective inhibitors that has been reported.
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