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The p38‐MAPK inhibitor, SB203580, inhibits cardiac stress‐activated protein kinases/c‐Jun N‐terminal kinases (SAPKs/JNKs)
Author(s) -
Clerk Angela,
Sugden Peter H
Publication year - 1998
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/s0014-5793(98)00324-x
Subject(s) - p38 mitogen activated protein kinases , kinase , chemistry , mapk/erk pathway , stimulation , gene isoform , immunoprecipitation , mitogen activated protein kinase , protein kinase a , microbiology and biotechnology , biophysics , biochemistry , biology , gene , endocrinology
SB203580 is a recognised inhibitor of p38‐MAPKs. Here, we investigated the effects of SB203580 on cardiac SAPKs/JNKs. The IC 50 for inhibition of p38‐MAPK stimulation of MAPKAPK2 was approximately 0.07 μM, whereas that for total SAPK/JNK activity was 3–10 μM. 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 μM) 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.