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

FEBS Letters

Clerk, Angela¹  Sugden, Peter H¹ 

[1] NHLI Division (Cardiac Medicine), Imperial College School of Medicine, Dovehouse Street, London SW3 6LY, UK

关键词: Heart;    Protein kinase inhibitor;    SB203580;    Stress-activated protein kinase/c-Jun N-terminal kinase;    Mitogen-activated protein kinase-activated protein kinase 2;    ERK;    extracellularly responsive kinase;    FPLC;    fast protein liquid chromatography;    GST;    glutathione S-transferase;    JNK;    c-Jun N-terminal kinase;    MAPK;    mitogen-activated protein kinase;    MAPKAPK2;    MAPK-activated protein kinase 2;    SAPK;    stress-activated protein kinase;   

DOI  :  10.1016/S0014-5793(98)00324-X

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

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.

【 授权许可】

Unknown