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BI-78D3 is a substrate competitive inhibitor of JNK inhibitor [2].

JNK is a member of the MAPK family. JNK is a stress-activated protein kinase that modulates pathways implicated in a variety of disease states. Non-motoric JNK functions may differ between cell types and organs. The JNK is involved in a1-adrenoceptor-mediated contraction of prostate smooth muscle. For non-malignant, epithelial human prostate cells, JNK activation not only has the function of pro-apoptotic and antiproliferative but also related with JNK-dependent survival.[1]

BI-78D3 is competitive with ATF2 for binding to JNK1 with an apparent Ki value of 200 nM. In addition, it has been reported that BI-78D3 does not inhibit the phosphorylation of a short peptide substrate lacking a D-domain. This confirms that BI-78D3 is substrate competitive.[2]

BI-78D3 inhibits both noradrenaline- and phenylephrine-induced contractions. Then it prevents α1-adrenoceptor-mediated contraction of prostate tissue. As an effective JNK inhibitor, BI-78D3 has the ability of abrogating ConA-induced liver damage and restoring insulin sensitivity. [1,2]

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