Olomoucine II

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).¹ It 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).^1,2 Olomoucine 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

1.Kryštof, 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) 2.Cihalova, D., Hofman, J., Ceckova, M., et al.Purvalanol A, olomoucine II and roscovitine inhibit ABCB1 transporter and synergistically potentiate cytotoxic effects of daunorubicin in vitroPLoS One8(12)e83467(2013) 3.Holcakova, J., Tomasec, P., Bugert, J.J., et al.The inhibitor of cyclin-dependent kinases, olomoucine II, exhibits potent antiviral propertiesAntivir. Chem. Chemother.20(3)133-142(2010)