Kenpaullone

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Cat.No. 1398 - Kenpaullone | C16H11BrN2O | CAS No. 142273-20-9
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)
Datasheet
Citations (2)
Reviews
Literature

Biological Activity

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

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 32.72 100
ethanol 1.64 5 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 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

Certificate of Analysis / Product Datasheet
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References

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


If you know of a relevant reference for Kenpaullone, please let us know.

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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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Literature in this Area

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