General description

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 µM). Also, potently inhibits several kinases at 1 µM 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 µM). Also, potently inhibits several kinases at 1 µM 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 LβT2 gonadotrope cells).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Xiong, W., et al. 2016. Mol. Cancer Ther.15, In press.Knowlton, A.L., et al. 2006. Curr. Biol.16, 1705.Kapoor, T.M., et al. 2006. Science311, 388.Hirota, T., et al. 2005. Nature438, 1176.Sessa, F., et al. 2005. Mol. Cell.18, 379.Lampson, M.A., et al. 2004. Nat. Cell Biol.6, 232.Hauf, S., et al. 2003. J. Cell Biol.161, 281.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot freeze at -(20°C). Stock solutions are stable for up to 6 months at -20°C..

Warning

Toxicity: Regulatory Review (Z)