Description |
A cell-permeable imidazoquinazoline compound that acts as a potent, reversible, and ATP-competitive inhibitor against all three classes of PI 3-K kinases (IC 50 = 11, 18, 47, 58, 64, 350, and 830 nM against p110α, p110γ, PI 3-KC2α, p110δ, PI 3-KC2β, p110β, and hsVPS34, respectively), as well as several PIKKs (IC 50 = 13, 610, and 1050 nM against DNA-PK, ATM, and mTORC1, respectively) and PI 4-KIIIα (IC 50 = 830 nM), while exhibiting much reduced potency against PI 4-KIIIβ and ATR (IC 50 = 3.1 and 15 µM, respectively) and little or no activity toward PI 4-KIIα, PIPKs (IC 50 >100 µM), and a panel of 36 commonly studied protein kinases (<15% inhibition at 10 µM)
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