Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression whose function/dysfunction has been implicated in cancer, a subset of human neurodegenerative diseases, and the reward response of addictive drugs via alteration of postsynaptic dopamine receptor signaling. Iso-olomoucine is an inactive stereoisomer of the Cdk5 inhibitor olomoucine. Because iso-olomoucine lacks activity at Cdk5 (IC50 ≥ 1 mM), it may have utility as a control compound for determining Cdk5 specificity. In a Cdk5-independent manner, iso-olomoucine has been shown to rapidly inhibit dopamine transporter activity in rat dorsal striatal synaptosomes with a potency similar to that of olomoucine (IC50 ~37 μM).
