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.
Compound Libraries
Kenpaullone is also offered as part of the Tocriscreen Plus and Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.72 | 100 | |
| ethanol | 1.64 | 5mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 327.18. Batch specific molecular weights may vary from batch to batch due to solvent 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
References
References are publications that support the products' biological activity.
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
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