Background:

CC-401 is a specific inhibitor of JNK with Ki values of 25-50nM [1].

CC-401 is a second generation ATP-competitive inhibitor of all three forms of JNK. It is selective against JNK over other kinases such as p38, ERK, IKK2 and ZAP70. CC-401 potently inhibits JNK in cell-based assay with concentration of 1 to 5μM. The activation of JNK signaling is identified in many immune-mediated kidney disease models. Thus, as the JNK inhibitor, CC-401 is found to be effective in these renal injury models. In the acute anti-GBM disease, CC-401 inhibits JNK activation and causes 50%-70% reduction of proteinuria. In addition, CC-401 is also used in liver injury models [1, 2 and 3].

参考文献:
[1] Ma F Y, Flanc R S, Tesch G H, et al.  A pathogenic role for c-Jun amino-terminal kinase signaling in renal fibrosis and tubular cell apoptosis. Journal of the American Society of Nephrology, 2007, 18(2): 472-484.
[2] Flanc R S, Ma F Y, Tesch G H, et al.  A pathogenic role for JNK signaling in experimental anti-GBM glomerulonephritis. Kidney international, 2007, 72(6): 698-708.
[3] Bogoyevitch M A, Arthur P G.  Inhibitors of c-Jun N-terminal kinases—JuNK no more Biochimica et Biophysica Acta (BBA)-Proteins and Proteomics, 2008, 1784(1): 76-93.