CC-401 hydrochloride is a potent inhibitor of all three forms of JNK, with a Ki ranging from 25 to 50 nM. It demonstrates significant selectivity for JNK over other related kinases and provides specific JNK inhibition in cell-based assays. This compound achieves its effect by competitively binding to the ATP binding site in JNK, thereby inhibiting the phosphorylation of the N-terminal activation domain of c-Jun.
- Potent inhibitor of all three forms of JNK (Ki: 25-50 nM).
- Exhibits at least 40-fold selectivity for JNK compared to other related kinases.
- Provides specific JNK inhibition at concentrations of 1 to 5 μM in cell-based assays.
- Competitively binds the ATP binding site in JNK.
- Inhibits phosphorylation of the N-terminal activation domain of c-Jun.
- Inhibits sorbitol-induced phosphorylation of c-Jun in HK-2 human tubular epithelial cells.
- Slows progression of proteinuria and prevents renal impairment in animal models.