A inhibitor of cyclin-dependent kinase and GSK3β
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Kenpaullone

Item No. 10010239

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
9-bromo-7,12-dihydro-indolo[3,2-d][1]benzazepin-6(5H)-one
CAS Number
142273-20-9
Synonyms
  • 9-Bromopaullone
  • NSC 664704
Molecular Formula
C16H11BrN2O
Formula Weight
327.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
230, 320 nm
SMILES
O=C1Nc2ccccc2c2[nH]c3ccc(Br)cc3c2C1
InChi Code
InChI=1S/C16H11BrN2O/c17-9-5-6-14-11(7-9)12-8-15(20)18-13-4-2-1-3-10(13)16(12)19-14/h1-7,19H,8H2,(H,18,20)
InChi Key
QQUXFYAWXPMDOE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $132

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    10 mg

    $201

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    25 mg

    $432

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    Product Description

    The development of selective, cell-permeable protein kinase inhibitors for the treatment of cancer, inflammation, and other diseases, is a major focus of drug development efforts. Kenpaullone is an ATP-competitive inhibitor of several cyclin-dependent kinases (CDKs) as well as glycogen synthase kinase 3β (GSK3β).1,2,3 It inhibits GSK3β with an IC50 value of 0.23 µM and Cdk1/cyclin B, Cdk2/cyclin A, Cdk5/p25, and lymphocyte kinase with IC50 values of 0.4, 0.68, 0.85, and 0.47 µM, respectively.2,1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zaharevitz, D.W., Gussio, R., Leost, M., et al. Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer Res. 59(11), 2566-2569 (1999).

    2. Bain, J., McLauchlan, H., Elliot, M., et al. The specificities of protein kinase inhibitors: An update. Biochem. J. 371(Pt. 1), 199-204 (2003).

    3. LeClerc, S., Garnier, M., Hoessel, R., et al. Indirubins inhibit glycogen synthase kinase-3β and CDK5/P25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer’s disease. A property common to most cyclin-dependent kinase inhibitors? The Journal of Biological Chemisty 276(1), 251-260 (2001).