Alsterpaullone
Chemical Name: 7,12-Dihydro-9-nitroindolo[3,2-d][1]benzazepin-6(5H)-one
Purity: ≥98%
Biological Activity
Alsterpaullone is a potent CDK1 and 2 inhibitor (IC50 values are 0.035 and 0.08 μM, respectively). Also inhibits GSK-3β and Lck (IC50 values are 0.11 and 0.47 μM, respectively). Induces apoptosis by activation of caspase-9; inhibits growth of cancer cell lines in vitro. Also glucocorticoid receptor inhibitor.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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Background References
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Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity.
Schulz et al.
J.Med.Chem., 1999;42:2909 -
The specificities of protein kinase inhibitors: an update.
Bain et al.
Biochem.J., 2003;371:199 -
Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential.
Lahusen et al.
Mol.Carcinog., 2003;36:183 -
A high-throughput chemical screen identifies novel inhibitors and enhancers of anti-inflammatory functions of the glucocorticoid receptor.
Jiang et al.
Sci.Rep., 2017;7:6405
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