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Kenpaullone

Cat. No. 1398

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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.

Resources

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.

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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

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