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Beschreibung

A cell-permeable imidazoquinazoline compound that acts as a potent, reversible, and ATP-competitive inhibitor against all three classes of PI 3-K kinases (IC50 = 11, 18, 47, 58, 64, 350, and 830 nM against p110alpha, p110gamma, PI 3-KC2alpha, p110delta, PI 3-KC2beta, p110beta, and hsVPS34, respectively), as well as several PIKKs (IC50 = 13, 610, and 1050 nM against DNA-PK, ATM, and mTORC1, respectively) and PI 4-KIIIalpha (IC50 = 830 nM), while exhibiting much reduced potency against PI 4-KIIIbeta and ATR (IC50 = 3.1 and 15 µ,M, respectively) and little or no activity toward PI 4-KIIalpha, PIPKs (IC50 >100 µ,M), and a panel of 36 commonly studied protein kinases (<15% inhibition at 10 µ,M). Effectively suppreses insulin-stimulated phosphorylations of Akt and rpS6 in 3T3-L1 adipocytes and L6 myotubes in a dose-dependent manner in vitro (by >90% at 2.5 µ,M) and completely prevents insulin-induced blood glucose decline in mice in vivo (10 mg/ml, i.p.).