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JNK-IN-7 is a selective JNK inhibitor with IC50 values of 1.54 nM, 1.99 nM, 0.75 nM to JNK1, JNK2, JNK3, respectively. It also inhibits phosphorylation of c-Jun, which is a direct substrate of JNK kinase.

JNK-IN-8, an analog of JNK-IN-7 with an extra flag methyl, dramatically improved in selectivity and eliminated binding to IRAK1, PIK3C3, PIP4K2C and PIP5K3, comparing to JNK-IN-7. JNK-IN-7 and JNK-IN-8 require Cys116 for JNK2 inhibition. JNK-IN-7 can indeed inhibit IRAK-1 dependent E3 ligase activity of pellino, which plays an role in the Toll receptor signaling pathway in cells at relative high compound concentrations (1–10 mM).

The IRAK1 inhibitor JNK-IN-7 inhibited the IL-1-stimulated activation of Pellino 1 in IL-1R cells, but not the Pam3CSK4-stimulated activation of Pellino 1 in RAW264.7 macrophages. JNK-IN-7 also suppressed the phosphorylation of c-Jun in Pam3CSK4-stimulated RAW macrophages, but in contrast with IL-1R cells it did not affect the activation of Pellino 1.

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