Cat. No. 1398
Chemical Name: 9-Bromo-7,12-dihydro-indolo[3,2-d][
Biological ActivityPotent inhibitor of CDK1/cyclin B and GSK-3β (IC50 values are 0.4 and 0.23 μM respectively). Also inhibits CDK2/cyclin A, CDK2/cyclin E and CDK5/cyclin/p35 (IC50 values are 0.68, 7.5 and 0.85 μM respectively). Selective over c-src (IC50 = 15 μM), casein kinase 2 (IC50 = 20 μM), ERK1 (IC50 = 20 μM), ERK2 (IC50 = 9 μM) and a range of other protein kinases (IC50 values > 35 μM). Generates induced pluripotent stem cells (iPSCs) from somatic cells when used in combination with reprogramming factors; can replace Klf4.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Schultz et al (1999) Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity. J.Med.Chem. 42 2909. PMID: 10425100.
Zaharevitz et al (1999) Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer Res. 59 2566. PMID: 10363974.
Buolamwini (2000) Cell cycle targets in novel anticancer drug discovery. Curr.Pharm.Des. 6 379. PMID: 10788588.
Lyssiotis et al (2009) Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4. Proc.Natl.Acad.Sci.U.S.A. 106 8912. PMID: 19447925 .
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Keywords: Kenpaullone, supplier, GSK-3β, GSK-3beta, inhibitors, cdks, Potent, cyclin-dependent, kinase, GSK, Glycogen, Synthase, Kinase, 3, beta, Kinases, Cdk, Cyclin-Dependent, Protein, Carbohydrate, Metabolism, CDK1/cyclin, B, CDK2/cyclin, A, E, CDK5/cyclin/p35, stem, cells, Tocris Bioscience, Cyclin-Dependent Protein Kinase Inhibitors
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March 14 - 16, 2016
New Orleans, LA, USA