Olomoucine II

Description: Olomoucine II is an inhibitor of cyclin-dependent kinases (CDKs, IC50s = 7.6, 0.1, 19.8, 0.45, and 0.06 µM for Cdk1, -2, -4, -7, and -9, respectively).1It is selective for CDKs over 10 additional kinases (IC50s = >100 µM for all) but does inhibit ERK2 (IC50= 32 µM) and the ATP-binding cassette transporter B1 (ABCB1, IC50= 6.4 µM).1,2Olomoucine II inhibits proliferation of a variety of cancer cells, including those expressing wild-type p53 or mutant p53 (mean IC50s = 7.4 and 10.1 µM, respectively), and it acts synergistically with daunorubicin to inhibit proliferation of HCT-8 cells that endogenously express ABCB1. Olomoucine also inhibits replication of herpes simplex virus 1 (HSV-1), HSV-2, vaccinia virus, human adenovirus type 4 (Ad4), and human CMV (IC50s = 5, 4.7, 3.8, 2.4, and 3.2 µM, respectively) but not measles virus or influenza virus (IC50s = >20 µM for both).3. Target: Others. Smiles: C(C)(C)N1C=2C(=C(NCC3=C(O)C=CC=C3)N=C(N[C@H](CC)CO)N2)N=C1. References: Kry?tof, V., McNae, I.W., Walkinshaw, M.D., et al.Antiproliferative activity of olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitorCell Mol. Life Sci.62(15)1763-1771(2005)