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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

Kenpaullone

Cayman Chemical Item Number 10010239

NSC 664704; 9-Bromopaullone (CAS 142273-20-9)

Kenpaullone (CAS 142273-20-9)

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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 (GSK-3β).1,2,3 It inhibits GSK-3β with an IC50 value of 0.023 µM3 (0.23 µM)2 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.1

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 2566-2569 (1999).

2 Bain, J., McLauchlan, H., Elliot, M., et al. The specificities of protein kinase inhibitors: An update. Biochem J 371 199-204 (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? J Biol Chem 276(1) 251-260 (2001).

Synonyms
  • NSC 664704
  • 9-Bromopaullone
Formal Name 9-​bromo-​7,​12-​dihydro-​indolo[3,​2-​d][1]benzazepin-​6(5H)-​one
CAS Number 142273-20-9
Molecular Formula C16H11BrN2O
Formula Weight 327.2
Formulation A crystalline solid
Purity >98%
λmax 230, 320 nm
Stability 2 years
Storage -20°C
Shipping Wet ice in continental US; may vary elsewhere
SMILES
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O=C1Nc2ccccc2c2[nH]​c3ccc(Br)​cc3c2C1

Background Reading

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 2566-2569 (1999).

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

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? J Biol Chem 276(1) 251-260 (2001).

Kenpaullone is available in the following screening library:

Size Price Quantity Subtotal
1 mg $39.00 $0.00
5 mg $176.00 $0.00
10 mg $312.00 $0.00
50 mg $1,365.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-02-12. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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