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Category: EnzymesarrowKinasesarrowCyclin-dependent Kinase
Cat.No. Product Name
1398 Kenpaullone
Price and Availability

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Kenpaullone
Chemical Name: 9-Bromo-7,12-dihydro-indolo[3,2-d][1]benzazepin-6(5H)-o ne

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).

Technical Data:

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M.Wt: 327.18
Formula: C16H11BrN2O
Storage: Store at RT
Solubility: Soluble to 100 mM in DMSO and to 5 mM in Ethanol
Purity: >98%
CAS No: [142273-20-9]

Resources:

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    References:

    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. 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. Buolamwini (2000) Cell cycle targets in novel anticancer drug discovery. Curr.Pharm.Des. 6 379. Bain et al (2003) The specificities of protein kinase inhibitors: an update. Biochem.J. 371 199.
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    Keywords: Kenpaullone, Kinases, Potent Cyclin-dependent Kinase Inhibitor. Also Inhibits GSK-3, Tocris Bioscience
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