c-Jun N-Terminal Kinase (JNK) Inhibitor

No.175(October 2017)

A2548: SP600125 (1)

SP600125 (1) is an inhibitor for JNK1, JNK2, and JNK3 with IC₅₀ of 40 nM, 40 nM, and 90 nM respectively.¹⁾ Inhibitory constants of 1 for these JNKs are Ki = 0.19 μM. The inhibitory mechanism of 1 to the JNKs is ATP-competitive.

The selectivity of 1 was determined by crystal structural analysis using the ternary complex, JNK1-peptide fragment JIP1-1.²⁾ JIP1 is a member of the JNK-interacting protein (JIP) family and contains a JNK binding domain (JBD), an SRC homology (SH3) domain, and a phosphotyrosine-binding (PTB) domain.^3,4) JBD possesses the consensus sequence, R/KXXXXLXL.⁵⁾ The sequence of peptide fragment JIP1 used in the research described above is RPKRPTTLNLF.²⁾

The product is for research purpose only.

References

1)SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase
- B. L. Bennett, D. T. Sasaki, B. W. Murray, E. C. O’Leary, S. T. Sakata, W. Xu, J. C. Leisten, A. Motiwala, S. Pierce, Y. Satoh, S. S. Bhagwat, A. M. Manning, D. W. Anderson, Proc. Natl. Acad. Sci. USA 2001, 98, 13681.
2)Structural basis for the selective inhibition of JNK1 by the scaffolding protein JIP1 and SP600125
- Y.-S. Heo, S.-K. Kim, C. I. Seo, Y. K. Kim, B.-J. Sung, H. S. Lee, J. I. Lee, S. Y. Park, J. H. Kim, K. Y. Hwang, Y.-L. Hyun, Y. H. Jeon, S. Ro, J. M. Cho, T. G. Lee, C.-H. Yang, EMBO J. 2004, 23, 2185.
3)A mammalian scaffold complex that selectively mediates MAP kinase activation
- A. J. Whitmarsh, J. Cavanagh, C. Tournier, J. Yasuda, R. J. Davis, Science 1998, 281, 1671.
4)Scaffold proteins of MAP-kinase modules
- D. N. Dhanasekaran, K. Kashef, C. M. Lee, H. Xu, E. P. Reddy, Oncogene 2007, 26, 3185.
5)Differential targeting of MAP kinases to the ETS-domain transcription factor Elk-1
- S.-H. Yang, A. J. Whitmarsh, R. J. Davis, A. D. Sharrocks, EMBO J. 1998, 17, 1740.

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c-Jun N-Terminal Kinase (JNK) Inhibitor

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