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Beschreibung

A cell-permeable indolinone compound that interacts with both the ATP- and the adjacent hydrophobic binding pocket of Aurora B and acts as a rapid and reversible inhibitor of Aurora kinase B activity (IC50 ~250 nM) with moderate selectivity over Cdk1/B, Cdk2/E and Cdk4/D1 (IC50 = 1.2, >10 and >10 µ,M). Also, potently inhibits several kinases at 1 µ,M in a 25-kinase screening panel (100%, 100%, 96%, 88%, 87% and 84% against Lck, PHK, AMPK, MKK1, MAPKAP-K1 and Chk1, respectively). Reported to reduce histone H3-Ser10 phosphorylation, inhibit cytokinesis, promote chromosome biorientation, perturb mitosis and polyploidy in mammalian cells., A cell-permeable indolinone compound that interacts with both the ATP- and the adjacent hydrophobic binding pocket of Aurora B and acts as a rapid and reversible inhibitor of Aurora kinase B activity (IC50 ~ 250 nM) with moderate selectivity over Cdk1/B, Cdk2/E and Cdk4/D1 (IC50 = 1.2, >10 and >10 µ,M). Also, potently inhibits several kinases at 1 µ,M in a 25-kinase screening panel (100%, 100%, 96%, 88%, 87% and 84% against Lck, PHK, AMPK, MKK1, MAPKAP-K1 and Chk1, respectively). Reported to reduce histone H3-Ser10 phosphorylation, inhibit cytokinesis, promote chromosome biorientation, perturb mitosis and polyploidy in mammalian cells. Recently shown to potently inhibit MST4 kinase (IC50 = 6.18 nM) in an ATP-competitive manner. Dose-dependently accelerates hypoxia-induced apoptosis and decreases survival (EC50 = 10 nM in MST4 LbetaT2 gonadotrope cells).