3-(4-Morpholinothieno[3,2-d]pyrimidin-2-yl)phenol is a selective inhibitor for the α-isoform of PI 3-Kinase (IC₅₀: PI 3-Kα = 2 nM, PI 3-Kβ = 16 nM, PI3-Kγ = 660 nM, PI3KC2β = 220 nM)). It showed >1000-fold selectivity vs. protein kinases such as PKA, KDR, PKCa, and E/CDK2 (IC₅₀ = 91, 3.4, 466, 288 μM). It inhibited proliferation of A375 melanoma cells at 580 nM. Also known as PI3-K Inhibitor 2, PIK2.

References

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1) M. Hayakawa, et al. “Synthesis and biological evaluation of 4-morpholino-2-phenyl quinazolines and related derivatives as novel PI3 kinase p110a inhibitors” Bioorg. Med. Chem. 2006, 14, 6847-6858.