Uses
Olomoucine II is a potent CDK inhibitor with IC50 values of 0.06, 0.1, 0.45, 7.6, 19.8 μM for CDK9/cyclin T, CDK2/cyclin E, CDK7/cyclin H, CDK1/cyclin B, CDK4/cyclin D1, respectively. Olomoucine II shows antiproliferative activity[1].
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 IC
50 of 20 nM and displays increased potency over purvalanol A (Cat. No.
540500; IC
50 = 50 nM), Roscovitine (Cat. No.
557360; IC
50 = 450 nM), Bohemine (Cat. No.
203600; IC
50 = 1.1 μM) and Olomoucine (Cat. No.
495620; IC
50 = 7.0 μM). Further, exerts greater
in vitro cytotoxicity in various cancer cell lines (IC
50 = 3.0 μM, 5.3 μM, 6.3 μM, 6.3 μM and 11.1 μM for CEM, MCF7, HOS, G631 and K562, respectively).
IC 50
CDK9/cycT: 0.06 μM (IC
50); CDK2/cyclinE: 0.1 μM (IC
50); CDK7/cyclin H: 0.45 μM (IC
50); Cdk1/cyclin B: 7.6 μM (IC
50); CDK4/cyclinD1: 19.8 μM (IC
50)
References
[1] Krystof V, et al. Antiproliferative activity of olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor. Cell Mol Life Sci. 2005 Aug;62(15):1763-71. DOI:
10.1007/s00018-005-5185-1
