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A cell-permeable morpholino-pyrimidinone compound that acts as a reversible, ATP-competitive, selective, and highly potent inhibitor of PI 3-Kb (p110b IC50 = 0.005 µM, p110d IC50 = 0.1 µM, p110a IC50 = 5 µM, and p110b IC50 ≥3.5 µM) with little activity against a panel of 15 commonly studied protein kinases even at concentrations as high as 10.0 µM. An excellent tool for studying p110b-dependent responses both in cells in vitro and in animals in vivo.