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Description

A cell-permeable morpholino-thienopyrimidine compound that acts as a potent and isoform-selective inhibitor of PI 3-Ks (IC50 = 2 nM, 16 nM, 660 nM, and 220 nM for p110&alpha,, p110&beta, p110&gamma,, and PI 3-K C2&beta,, respectively) and inhibits non-PI 3-K kinases only at much higher concentrations (IC50 &ge, 3.4 microM for Cdk2/E, KDR, PKA, and PKC&alpha,). Shown to inhibit cell proliferation (IC50 = 580 nM) and serum-stimulated Akt phosphorylation (IC50<3 microM) in A375 melanoma cells., A cell-permeable morpholino-thienopyrimidine compound that acts as a potent and isoform-selective inhibitor of PI 3-kinases (IC50 = 2 nM, 16 nM, 660 nM, and 220 nM for p110&alpha,, p110&beta, p110&gamma,, and PI 3-K C2&beta,, respectively) and inhibits non-PI 3-K kinases only at much higher concentrations (IC50 &ge,3.4 microM for Cdk2/E, KDR, PKA, and PKC&alpha,). Shown to inhibit cell proliferation (IC50 = 580 nM) and serum-stimulated Akt phosphorylation (IC50<3 microM) in A375 melanoma cells.