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 32p of [γ-32P]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 IC50 of 1.37 μmol·L-1, Kinetic studies of SQMS on recombinant human CK2 showed the inhibition was competitive with ATP and noncompetitive with casein. CONCLUSION: SQMS is an inhibitor of protein kinase CK2, and the inhibitory action of SQMS on CK2 is competitive with ATP and noncompetitive with casein.