p38丝裂原活化蛋白激酶抑制剂SB203580可抑制心脏应激激活蛋白激酶/c-Jun氨基末端激酶（SAPKs/JNKs）。
The p38-MAPK inhibitor, SB203580, inhibits cardiac stress-activated protein kinases/c-Jun N-terminal kinases (SAPKs/JNKs).
作者信息
Clerk A, Sugden P H
机构信息
NHLI Division (Cardiac Medicine), Imperial College School of Medicine, London, UK.
出版信息
FEBS Lett. 1998 Apr 10;426(1):93-6. doi: 10.1016/s0014-5793(98)00324-x.
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 microM, whereas that for total SAPK/JNK activity was 3-10 microM. 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 microM) completely inhibited the 0.15 M NaCl activity and partially inhibited the 0.08 M NaCl activity. Since JNK1 antibodies immunoprecipitate the 46 kDa activity, this indicates that SB203580 selectively inhibits 52 and 54 kDa SAPKs/JNKs.
SB203580是一种公认的p38丝裂原活化蛋白激酶（p38-MAPKs）抑制剂。在此，我们研究了SB203580对心脏应激激活蛋白激酶/应激活化蛋白激酶（SAPKs/JNKs）的影响。抑制p38-MAPK刺激丝裂原活化蛋白激酶激活蛋白激酶2（MAPKAPK2）的半数抑制浓度（IC50）约为0.07微摩尔，而对总SAPK/JNK活性的IC50为3 - 10微摩尔。SB203580不抑制免疫沉淀的JNK1亚型。通过阴离子交换色谱分离出三个SAPK/JNK活性峰，分别在等度洗脱（44 kDa）、0.08 M氯化钠洗脱（46和52 kDa）以及0.15 M氯化钠洗脱（54 kDa）时出现。SB203580（10微摩尔）完全抑制了0.15 M氯化钠洗脱时的活性，并部分抑制了0.08 M氯化钠洗脱时的活性。由于JNK1抗体免疫沉淀46 kDa的活性，这表明SB203580选择性抑制52和54 kDa的SAPKs/JNKs。
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