Cdk5 inhibitor 25-106 is a potent, brain-penetrant inhibitor of Cdk5/p35 activity with IC50 of 178 nM.
Cdk5 inhibitor 25-106 demonstrated similar inhibition against highly homologous Cdk2/Cyclin E (IC50=149 nM), and weak inhibition against CDK9/Cyclin T1 (IC50=5710 nM) in in vitro selectivity assays.
25-106 significantly reduced phospho-Ser549 synapsin I levels in the striatum 2 h after I.V. injection.
25-106 inhibits Cdk5 activity in vivo and displays high potency for inhibition in vitro.
25-106 (50 mg/kg) displayed an increased latency to suspend immobility and displayed a reduction in total immobility time as compared to vehicle-injected mice, modulated behavioral phenotypes linked to Cdk5 through previous characterizations of conditional knockout mice.
