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Effects of tyrphostins on activity of casein kinase II from rat liver
1Department of Medical Biochemistry, Guangdong Medical College, Zhanjiang, China.
Aim:
To investigate the effects of tyrphostins, (AG213, AG1394, AG114, AG1109, AG555) on the activity of casein kinase (CK) II.
Methods:
CK II was partially purified from rat livers by sequential DE52 and heparin-Sepharose chromatography. CK II activity was assayed by incubating CK II with dephosphorylated casein and [gamma-32 P]ATP.
Results:
AG213 inhibited the activity of CK II with IC50 44.7 mumol.L-1 (41.5-47.9 mumol.L-1), and AG1394 (144 mumol.L-1) strongly inhibited the activity of CK II with an inhibitory ratio of 89%. AG114 (174 mumol.L-1) and AG1109 (126 mumol.L-1) had inhibitory effects on the activity of CK II (p < 0.01). AG555 (136 mumol.L-1) had little effect on CK II activity.
Conclusion:
Some tyrphostins are potent inhibitors of CK II.