CC-90001 是一种有效，选择性和具有口服活性的 c-Jun N 末端激酶 (JNK) 抑制剂。CC-90001 在基于细胞的模型中显示出对 JNK1 的选择性是 JNK2 的 12.9 倍。CC-90001 可用于特发性肺纤维化的研究。
CC-90001 is a potent, selective and orally active inhibitor of c-Jun N-terminal kinase (JNK). CC-90001 shows 12.9-fold selectivity for JNK1 over JNK2 in a cell-based model. CC-90001 can be used for the research of idiopathic pulmonary fibrosis[1][2].
CC-90001 blocks LPS-induced c-jun phosphorylation with an EC50 of 480 nM in cellular assays[1].CC-90001 is 12.9-fold more potent for JNK1 inhibition than JNK2 using JNK1 and JNK2 knockout fibroblasts[1].
CC-90001 (3 mg/kg b.i.d.) reduces the development of fibrosis, as evidenced by a 48% reduction in collagen and a 53% reduction in α-smooth muscle actin (α-SMA) in a steatohepatitis model[1].CC-90001 decreases multiple measures of lung collagen and reduces disease induced increases in α-SMA to nearly baseline levels in a house dust mite model of lung fibrosis[1].
[1]. Bennett B, et, al. CC-90001, a Second Generation Jun N-Terminal Kinase (JNK) Inhibitor for the Treatment of Idiopathic Pulmonary Fibrosis. American Journal of Respiratory and Critical Care Medicine 2017; 195:A5409.
[2]. Kolb M, et, al. Therapeutic targets in idiopathic pulmonary fibrosis. Respir Med. 2017 Oct;131:49-57.
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