REVIEW CC-401 is a competitive inhibitor of the ATP binding site in the active, phosphorylated, form of JNK. This prevents JNK from phosphorylating its various target molecules, including the amino terminus of c-Jun. It is a potent inhibitor of all three forms of JNK (Ki of 25-50 nM), and has at least 40-fold selectivity for JNK compared with other related kinases, including: p38, ERK, IKK2, PKC, Lck, and ZAP70. CC-401 acts to inhibit JNK signaling by competitive binding to the adenosine triphosphate-binding site in the active, phosphorylated, form of JNK, resulting in inhibition of the phosphorylation of JNK targets, such as the amino-terminal activation domain of the transcription factor, c-Jun. In cell-based assays, 1-5 µmol/l CC-401 provides specific JNK inhibition.
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