Product overview

Name Kenpaullone
Purity >98%
Description Potent CDK inhibitor. Also GSK-3 inhibitor. Generates iPSCs.
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Biological Data

Biological description Potent, ATP-competitive CDK inhibitor (IC50 values are 0.4, 0.68, 7.5, 0.85 µM for CDK1/cyclinB, CDK2/cyclinA, CDK2/cyclinE and CDK5/p25 respectively). Also inhibits GSK-3β and LCK (IC50 values are 0.23 and 0.47 µM respectively) Displays reduced activity for other kinases (IC50 values are 15, 20, 20, 9 µM for c-src, casein kinase 2, ERK1 and ERK2 respectively). Also Generates iPSCs. Displays antiproliferative properties.

Solubility & Handling

Storage instructions Room temperature
Solubility overview Soluble in DMSO (100mM, gentle warming) or ethanol (5mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

Calculators

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Chemical Data

Purity >98%
Chemical name 9-Bromo-7,12-dihydro-indolo[3,2-d][1]benzazepin-6(5H)-one
Molecular Weight 327.18
Chemical structure Kenpaullone  [142273-20-9] Chemical Structure
Molecular Formula C16H11BrN2O
CAS Number 142273-20-9
PubChem identifier 3820
SMILES BrC1=CC=C2NC3=C(CC(=O)NC4=CC=CC=C34)C2=C1
InChiKey QQUXFYAWXPMDOE-UHFFFAOYSA-N

References for Kenpaullone

References are publications that support the biological activity of the product
  • New thiophene analogues of kenpaullone: synthesis and biological evaluation in breast cancer cells.

    Brault L et al (2005) Eur J Med Chem 40(8) : 757-63.
  • The specificities of protein kinase inhibitors: an update.

    Bain J et al (2003) Biochem J 371(Pt 1) : 199-204.
  • Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases.

    Zaharevitz DW et al (1999) Cancer Res 59(11) : 2566-9.

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