Biaffin

Newsletter

kinases protein kinase inhibitors signaling activators kinase substrates antibodies bioluminescence assays
Kenpaullone, 1 mg  

Kenpaullone, 1 mg

9-Bromo-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one

Synonyms: NSC-664704
potent, cell-permeable inhibitor of GSK3b, Lck and Cdks

More details

PKI-KNP-001

Availability: on stock

70,00 €

Background: Kenpaullone is a potent, cell-permeable inhibitor of glycogen synthase kinase-3b (GSK3b, IC50 = 230 nM), Lck (IC50 = 470 nM) and cyclin-dependent kinases (Cdks). Inhibits Cdk1/cyclin B (IC50 = 400 nM), Cdk2/cyclin A (IC50 = 680 nM), and Cdk5/p25 (IC50 = 850 nM).

Chemical formula: C16H11BrN2O
Molecular weight: 327.2 g/mol
Purity: > 98%
Appearance: yellowish powder
Solubility: soluble in DMSO
CAS number: 142273-20-9

Also available predissolved at 10 mM in our CDK Inhibitor Set.

Product specific literature references:

Schultz C, Link A, Leost M, Zaharevitz DW, Gussio R, Sausville EA, Meijer L, Kunick C (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(15):2909-19.

Zaharevitz DW, Gussio R, Leost M, Senderowicz AM, Lahusen T, Kunick C, Meijer L, Sausville EA (1999) "Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases." Cancer Res. 59(11):2566-9.

Kunick C, Lauenroth K, Wieking K, Xie X, Schultz C, Gussio R, Zaharevitz D, Leost M, Meijer L, Weber A, Jorgensen FS, Lemcke T (2004) "Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones" J. Med. Chem. 47(1):22-36

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.