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Beschreibung

A purine-2,6-dione compound that targets the ATP-binding pocket of B-Raf and effectively inhibits the phosphorylation of MEK by wild-type B-Raf in cell-free in vitro kinase assays (IC50 = 1.7 µ,M and Ki, app = 106 nM with 100 µ,M ATP). Reported to be equally potent against the oncogenic V600E B-Raf mutant and exhibit much less activity against PI 3-Kgamma (IC50 = 25 µ,M) and more than 50-fold selectivity over PAK1, GSK-3beta, PAK4, MST1, and PIM1 (IC50 >= 100 µ,M)., A purine-2,6-dione compound that targets the ATP-binding pocket of B-Raf and effectively inhibits the phosphorylation of MEK by wild-type B-Raf in cell-free in vitro kinase assays (IC50 = 1.7 µ,M and Ki, app = 106 nM with 100 µ,M ATP). Reported to be equally potent against the oncogenic V600E B-Raf mutant and exhibit much less activity against PI 3-Kgamma (IC50 = 25 µ,M) and more than 50-fold selectivity over PAK1, GSK-3beta, PAK4, MST1, and PIM1 (IC50 >=100 µ,M).