Effects of tyrphostins on activity of casein kinase II from rat liver
Abstract
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.
Keywords:
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.