[HTML][HTML] The p38-MAPK inhibitor, SB203580, inhibits cardiac stress-activated protein kinases/c-Jun N-terminal kinases (SAPKs/JNKs)

A Clerk, PH Sugden - FEBS letters, 1998 - Elsevier
A Clerk, PH Sugden
FEBS letters, 1998Elsevier
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 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) …
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 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.
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