Kenpaullone
Chemical Name: 9-Bromo-7,12-dihydro-indolo[3,2-d][1]benzazepin-6(5H)-one
Purity: ≥98%
Biological Activity
Kenpaullone is a GSK-3beta inhibitor (IC50 = 0.23 μM). Also inhibits cyclin dependent kinases (cdks) in the sub micromolar range (reported IC50 values are 0.4, 0.68-7 and 0.85 μM for cdk1, cdk2 and cdk5, respectively). Generates induced pluripotent stem cells (iPSCs) from somatic cells when used in combination with reprogramming factors; can replace Klf4.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.
Background References
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How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
Jorda et al.
J.Med.Chem., 2018;61:9105 -
Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4.
Lyssiotis et al.
Proc.Natl.Acad.Sci.U.S.A., 2009;106:8912 -
Cell cycle targets in novel anticancer drug discovery.
Buolamwini
Curr.Pharm.Des., 2000;6:379 -
Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity.
Schultz et al.
J.Med.Chem., 1999;42:2909 -
Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases.
Zaharevitz et al.
Cancer Res., 1999;59:2566
Product Datasheets
Citations for Kenpaullone
The citations listed below are publications that use Tocris products. Selected citations for Kenpaullone include:
2 Citations: Showing 1 - 2
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Generation and expansion of highly pure motor neuron progenitors from human pluripotent stem cells.
Authors: Du Et al.
Nat Commun 2015;6:6626
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A meta analysis of pancreatic microarray datasets yields new targets as cancer genes and biomarkers.
Authors: Goonesekere Et al.
PLoS One 2014;9:e93046
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