Cdk/CKI Inhibitor, (R)-DRF053 is a cell-permeable ATP-binding pocket-targeting (R)-Roscovitine derivative that is more potent than Roscovitine in inhibiting Cdc2 (CDK1)/CDK5/Casein Kinase (CK1) activity while maintaining selectivity against GSK-3α/β. The CDK/CK1 dual-specificity nature of (R)-DRF053 most likely accounts for its superior activity to that of (R)-Roscovitine against β40 production from APP-expressing N2A cells. Cdk/CKI Inhibitor, (R)-DRF053 is an inhibitor of cyclin B and p35.
1. Oumata, N., et al. 2008. J. Med. Chem. 51: 5229-5242. PMID: 18698753
2. Bettayeb, K., et al. 2008. Oncogene. 27: 5797-5807. PMID: 18574471
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PMID: # 18574471 Bettayeb, K. et al. 2008. Oncogene. 27: 5797-5807.
PMID: # 18698753 Oumata, N. et al. 2008. J. Med. Chem. 51: 5229-5242.