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 (Item No. 14159) 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

WARNING This product is not for human or veterinary use.

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 inhibitor. Cell 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 vitro. PLoS One 8(12), e83467 (2013).

3. Holcakova, J., Tomasec, P., Bugert, J.J., et al. The inhibitor of cyclin-dependent kinases, olomoucine II, exhibits potent antiviral properties. Antivir. Chem. Chemother. 20(3), 133-142 (2010).