Effects of sodium quercetin-7-sulfate on recombinant human protein kinase CK2 holoenzyme / 中国药理学通报

ABSTRACT

AIM To study the effects and kinetics of sodium quercetin 7 sulphate (SQMS) on recombinant human protein kinase CK2 holoenzyme. METHODS The recombinant human CK2 holoenzyme activity was assayed by detecting incorporation of 32 P of [? 32 P]ATP into the substrate at various conditions. RESULTS SQMS was shown to strongly inhibit the holoenzyme activity of recombinant human protein kinase CK2 with an IC 50 of 1 37 ?mol?L -1 , Kinetic studies of SQMS on recombinant human CK2 showed the inhibition was competitive with ATP and noncompetitive with casein. CONCLUSIONSQMS is an inhibitor of protein kinase CK2, and the inhibitory action of SQMS on CK2 is competitive with ATP and noncompetitive with casein.