General description
A purine derivative that acts as a potent, reversible and selective inhibitor of p34cdk1/cyclin B (IC50 = 7 µM) and related kinases including p33cdk2/cyclin A (IC50 = 7 µM), p33cdk2/cyclin E (IC50 = 7 µM), p33cdk5/p35 (IC50 = 3 µM), and p44 MAP kinase (IC50 = 25 µM). Acts by competing for the ATP binding domain of the kinase. Exhibits reduced sensitivity towards related kinases, p34cdk4/cyclin D (IC50 >1 mM), and p40cdk6/cyclin D3 (IC50 >250 µM). Does not significantly affect the activity of other protein kinases at 1 mM. Known to inhibit DNA synthesis in interleukin-2-stimulated T lymphocytes and trigger G1 arrest similar to that observed in interleukin-2-deprived cells. Also used to synchronize cells in G1. A 50 mM (5 mg/336 µl) solution of Olomoucine (Cat. No. 495624) in DMSOis also available.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
p34cdk1/cyclin B
Product competes with ATP.
Reversible: yes
Target IC50: 7 µM, 7 µM, 7 µM, 3 µM, 25 µM against p34cdk1/cyclin B, p33cdk2/cyclin A, p33cdk2/cyclin E, p33cdk5/p35, and p44 MAP kinase, respectively
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 6 months at -20°C.
Other Notes
Abraham, R.T., et al. 1995. Biol. Cell 83, 105.
Mistelli, T., and Warren, G. 1995. J. Cell Sci. 108, 2715.
Glab, N., et al. 1994. FEBS Lett. 353, 207.
Veselý, J., et al. 1994. Eur. J. Biochem.224, 771.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥98% (TLC) |
| form | crystalline solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze |
| solubility | DMSO: soluble |
| shipped in | ambient |
| storage temp. | −20°C |
| SMILES string | [n]1(c2nc(nc(c2nc1)NCc3ccccc3)NCCO)C |
| InChI | 1S/C15H18N6O/c1-21-10-18-12-13(17-9-11-5-3-2-4-6-11)19-15(16-7-8-22)20-14(12)21/h2-6,10,22H,7-9H2,1H3,(H2,16,17,19,20) |
| InChI key | GTVPOLSIJWJJNY-UHFFFAOYSA-N |
