CC-401 dihydrochloride

CC-401 dihydrochloride has at least 40-fold selectivity for JNK compared with other related kinases, including p38, extracellular signal-regulated kinase (ERK), inhibitor of κB kinase (IKK2), protein kinase C, Lck, zeta-associated protein of 70 kDa (ZAP70). In cell-based assays, 1 to 5 μM CC-401 dihydrochloride provides specific JNK inhibition. CC-401 dihydrochloride, a small molecule that is a specific inhibitor of all three JNK isoforms. CC-401 dihydrochloride competitively binds the ATP binding site in JNK, resulting in inhibition of the phosphorylation of the N-terminal activation domain of the transcription factor c-Jun. The specificity of this inhibitor is tested in vitro using osmotic stress of the HK-2 human tubular epithelial cell line. CC-401 dihydrochloride inhibits sorbitol-induced phosphorylation of c-Jun in a dosage-dependent manner. However, CC-401 dihydrochloride does not prevent sorbitol-induced phosphorylation of JNK, p38, or ERK^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.