The p38-MAPK inhibitor, SB203580, inhibits cardiac stress-activated protein kinases/c-Jun N-terminal kinases (SAPKs/JNKs)
The p38-MAPK inhibitor, SB203580, inhibits cardiac stress-activated protein kinases/c-Jun N-terminal kinases (SAPKs/JNKs)
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DOI：
10.1016/s0014-5793(98)00324-x
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发表时间：
1998-04-10
期刊：
影响因子：
3.5
通讯作者：
Sugden, PH
中科院分区：
文献类型：
--
作者：
Clerk, A;Sugden, PH
SB203580是一种公认的p38-MAPKs抑制剂。在这里，我们研究了SB203580对心脏SAPKs/JNKs的影响。抑制的IC50 p38-MAPK刺激MAPKAPK2大约是0.07μM,而总SAPK /物活动,是3 - 10μM . SB203580不抑制免疫沉淀反应JNK1亚型,三峰SAPK /物活动被阴离子交换色谱分离,洗脱的权力平等主义的洗(44 kDa),在0.08米(46岁和52 kDa)和0.15 M氯化钠(54 kDa), SB203580(10μM)完全抑制了0.15 M氯化钠活动和部分抑制0.08国际扶轮氯化钠的活动,由于JNK1抗体免疫沉淀46 kDa活性，这表明SB203580选择性抑制52和54 kDa SAPK/JNKs， (C) 1998 Federation of European Biochemical Societies。
SB203580 is a recognised inhibitor of p38-MAPKs. Here, we investigated the effects of SB203580 on cardiac SAPKs/JNKs. The IC50 for inhibition of p38-MAPK stimulation of MAPKAPK2 was approximately 0.07 mu M, whereas that for total SAPK/JNK activity, was 3-10 mu M. SB203580 did not inhibit immunoprecipitated JNK1 isoforms, Three peaks of SAPK/JNK activity were separated by anion exchange chromatography, eluting in the isocratic wash (44 kDa), and at 0.08 M (46 and 52 kDa) and 0.15 M NaCl (54 kDa), SB203580 (10 mu M) completely inhibited the 0.15 M NaCl activity and partially inhibited the 0.08 RI NaCl activity, Since JNK1 antibodies immunoprecipitate the 46 kDa activity, this indicates that SB203580 selectively inhibits 52 and 54 kDa SAPK/JNKs, (C) 1998 Federation of European Biochemical Societies.