Biological Activity
Tanzisertib (CC-930) is a potent JNK1/2/3 inhibitor with IC50s of 61/7/6 nM, respectively.
In Vitro
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]. 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) blocks the JNK pathway that is activated by pro-fibrotic cytokines in systemic sclerosis[3].
In Vivo
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, but can also induce the regression of pre-existing fibrosis[3].
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.