Kenpaullone

Name: Kenpaullone
Brand: Tocris Bioscience
SKU: 1398

Tocris Bioscience, part of Bio-Techne | Catalog # 1398

Citations (21)

COA / SDS

GSK-3β inhibitor; also inhibits cdks

Key Product Details

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)
Molecular Weight:	327.18

View Full Technical Details for Kenpaullone

Technical Data
Citations

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 for Kenpaullone

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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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References for Kenpaullone

References are publications that support the biological activity of the product.

Jorda How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 2018 PMID: 30234987
Lyssiotis Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4. Proc.Natl.Acad.Sci.U.S.A. 2009 PMID: 19447925
Schultz Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity. J.Med.Chem. 1999 PMID: 10425100
Zaharevitz Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer Res. 1999 PMID: 10363974
Buolamwini Cell cycle targets in novel anticancer drug discovery. Curr.Pharm.Des. 2000 PMID: 10788588