Kenpaullone

Pricing Availability Delivery Time Qty
Cat.No. 1398 - Kenpaullone | C16H11BrN2O | CAS No. 142273-20-9
Description: Potent cyclin-dependent kinase inhibitor. Also inhibits GSK-3
Chemical Name: 9-Bromo-7,12-dihydro-indolo[3,2-d][1]benzazepin-6(5H)-one
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
Select another batch:
Safety Datasheet

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: 9447925


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

View Related Products by Product Action

View all Cyclin-Dependent Protein Kinase Inhibitors

Keywords: Kenpaullone, supplier, GSK-3β, GSK-3beta, inhibitors, inhibits, cdks, Potent, cyclin-dependent, kinase, GSK, Glycogen, Synthase, Kinase, 3, beta, Kinases, Cdk, Cyclin-Dependent, Protein, Carbohydrate, Metabolism, CDK1/cyclin, B, CDK2/cyclin, A, E, CDK5/cyclin/p35, stem, cells, Cyclin-dependent, Kinase, Tocris Bioscience

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


Do you know of a great paper that uses Kenpaullone from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Neurodegeneration

Neurodegeneration Product Guide

A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:

  • Alzheimer's disease
  • Parkinson's disease
  • Huntington's disease
Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.

Pathways for Kenpaullone

Protocols

TODO: Add Protocols