Kenpaullone

Cat. No. 1398

Kenpaullone C16H11BrN2O [142273-20-9]

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Chemical Name: 9-Bromo-7,12-dihydro-indolo[3,2-d][1]benzazepin-6(5H)-one

Biological Activity

Potent 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.

Technical Data

M.Wt:
327.18
Formula:
C16H11BrN2O
Solubility:
Soluble to 100 mM in DMSO and to 5 mM in ethanol with gentle warming
Purity:
>98 %
Storage:
Store at RT
CAS No:
142273-20-9

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

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

References

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 .

If you know of a relevant citation for this product please let us know.

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

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