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c-Jun N-Terminal Kinase (JNK) Inhibitor

No.175(October 2017)
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.


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