产品描述:
CC-930 is an orally bioavailable and potent inhibitor of JNKs (IC50s = 61, 7, and 6 nM for JNK1, JNK2, and JNK3, respectively).{39372} It is selective for MAP kinases over a panel of 240 kinases, showing greater than 50% inhibition at only one non-MAP kinase target, EGFR (IC50 = 380 nM). Within the MAPK family, it is selective for JNKs having IC50 values of 3,400 and 480 nM for p38α and ERK1, respectively. CC-930 inhibits JNK in a cell lysate assay with an IC50 value of 200 nM and blocks the phosphorylation of c-Jun in stimulated human peripheral blood mononuclear cells (PBMCs). In rats, CC-930 (10 and 30 mg/kg) inhibits TNF-α production induced by LPS. It also reduces lung fibrosis in a dose-dependent manner in a mouse pulmonary fibrosis model.