Cdk/CKI Inhibitor, (R)-DRF053 - CAS 1186647-87-9 - Calbiochem

A cell-permeable ATP-binding pocket-targeting (R)-Roscovitine (Cat. Nos. 550360 & 550364) derivative that is more potent than Roscovitine in inhibiting CDK1,CDK5, and CK1 activity (IC₅₀ = 220,80,14 vs. 350, 200, 2300 nM, respectively), while maintaining selectivity against GSK-3α/β (IC₅₀ = 4.1 µM). 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 (90% vs. 50% inhibition wtih 100 µM respective compound).

A cell-permeable ATP-binding pocket-targeting (R)-Roscovitine (Cat. Nos. 550360 & 550364) derivative that is more potent than Roscovitine in inhibiting CDK1/CDK5/CK1 activity (IC₅₀ = 220/80/14 vs. 350/200/2300 nM, respectively), while maintaining selectivity against GSK-3α/β (IC₅₀ = 4.1 µM). 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 (90% vs. 50% inhibition wtih100 µM respective compound).

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Oumata, N., et al. J. Med. Chem.51, 5229.
Bettayeb, K., et al. 2008. Oncogene27, 5797.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)