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Description
General description
A cell-permeable 2,6,9-trisubstituted purine analog that acts as a potent, reversible, and ATP-competitive inhibitor of Cdk1/B with an IC50 of 20 nM and displays increased potency over purvalanol A (Cat. No. 540500; IC50 = 50 nM), Roscovitine (Cat. No. 557360; IC50 = 450 nM), Bohemine (Cat. No. 203600; IC50 = 1.1 µM) and Olomoucine (Cat. No. 495620; IC50 = 7.0 µM). Further, exerts greater in vitro cytotoxicity in various cancer cell lines (IC50 = 3.0 µM, 5.3 µM, 6.3 µM, 6.3 µM and 11.1 µM for CEM, MCF7, HOS, G631 and K562, respectively).
A cell-permeable, potent, reversible, and ATP-competitive inhibitor of Cdk1/cyclin B (IC50 = 20 nM) that displays increased potency over purvalanol A (Cat. No. 540500; IC50 = 50 nM), Roscovitine (Cat. No. 557360; IC50 = 450 nM), Bohemine (Cat. No. 203600; IC50 = 1.1 µM), and Olomoucine (Cat. No. 495620; IC50 = 7.0 µM). Also exhibits greater in vitro cytotoxicity in various cancer cell lines (IC50 = 3.0 µM, 5.3 µM, 6.3 µM, 6.3 µM, and 11.1 µM for CEM, MCF7, HOS, G631, and K562, respectively).
Packaging
5 mg in Plastic ampoule
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Cdk1/B
Product competes with ATP.
Reversible: yes
Target IC50: 20 nM against Cdk1/B
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Krystof, V., et al. 2002. Bioorg. Med. Chem. Lett.12, 3283.
- Related Categories Cell Biology, Cell Signaling and Neuroscience, Cyclin-Dependent Kinase (CDK), Kinase/Phosphatase Biology, Serine/Threonine Kinase Biology, Serine/Threonine Kinase Inhibitors More... Quality Level