PIK-294 displays selectivity with respect to the inhibition of PI3K isoforms p110β, p110δ, and p110γ, however it is most selective for PI3Kδ (IC 50 = 490, 10, and 160 nM, respectively). PIK-294 exhibits low sensitivity to p110Yalpha; with an IC50 value of 10 μM. The m-phenol moiety of PIK-294 is able to penetrate the deep-affinity pocket of the ATP binding site, and thus increases in vitro inhibitory activity.
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