Tanzisertib 是有效的JNK1/2/3抑制剂，IC50分别为61、7 和 6 nM。

Tanzisertib (CC-930) is a potent inhibitor of JNK1/2/3 with IC50s of 61/7/6 nM, respectively, with potential antifibrotic activity.

Tanzisertib (CC-930) inhibits the formation of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin (IC50=1 μM)[1] and it blocks the JNK pathway that is activated by pro-fibrotic cytokines in systemic sclerosis[3]. Tanzisertib (CC-930) (1-2 μM) substantially reduces hepatocyte apoptosis and necrosis, abrogates apoptosis and necrosis in FC-loaded WT hepatocytes[2].

Tanzisertib (CC-930) (10 and 30 mg/kg, p.o.) inhibits the production of TNFa by 23% and 77% in the acute rat LPS-induced TNFa production PK-PD model[1]. Tanzisertib (CC-930) (150 mg/kg) prevents the development of fibrosis in different models. However, it can also induce the regression of pre-existing fibrosis[3].

899805-25-5

C21H23F3N6O2

448.44

CC-930

DMSO:33 mg/mL (73.59 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years