Bioactivity | 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]. | |||||||||
Invitro | 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]. | |||||||||
In Vivo | 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]. | |||||||||
Name | CC-90001 | |||||||||
CAS | 1403859-14-2 | |||||||||
Formula | C16H27N5O2 | |||||||||
Molar Mass | 321.42 | |||||||||
Appearance | Solid | |||||||||
Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
Storage |
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Reference | [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. |