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Description: GSK-3β inhibitor; also inhibits cdks
Chemical Name: 9-Bromo-7,12-dihydro-indolo[3,2-d][1]benzazepin-6(5H)-one
Purity: ≥98% (HPLC)
Biological Activity for Kenpaullone
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.
Compound Libraries for Kenpaullone
Kenpaullone is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Epigenetics Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.
Technical Data for Kenpaullone
| M. Wt | 327.18 |
| Formula | C16H11BrN2O |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 142273-20-9 |
| PubChem ID | 3820 |
| InChI Key | QQUXFYAWXPMDOE-UHFFFAOYSA-N |
| Smiles | BrC1=CC=C2NC3=C(CC(=O)NC4=CC=CC=C34)C2=C1 |
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.
Solubility Data for Kenpaullone
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.72 | 100 |
Preparing Stock Solutions for Kenpaullone
The following data is based on the product molecular weight 327.18. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.06 mL | 15.28 mL | 30.56 mL |
| 5 mM | 0.61 mL | 3.06 mL | 6.11 mL |
| 10 mM | 0.31 mL | 1.53 mL | 3.06 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.61 mL |
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Product Datasheets for Kenpaullone
References for Kenpaullone
References are publications that support the biological activity of the product.
Buolamwini (2000) Cell cycle targets in novel anticancer drug discovery. Curr.Pharm.Des. 6 379 PMID: 10788588
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
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
Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987
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2 Citations for Kenpaullone
Citations are publications that use Tocris products. Selected citations for Kenpaullone include:
Du et al (2015) Generation and expansion of highly pure motor neuron progenitors from human pluripotent stem cells. Nat Commun 6 6626 PMID: 25806427
Goonesekere et al (2014) A meta analysis of pancreatic microarray datasets yields new targets as cancer genes and biomarkers. PLoS One 9 e93046 PMID: 24740004
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Pathways for Kenpaullone
