tcsc1544 CC-930 (Tanzisertib)

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

IC50 & Target: IC50: 61 nM (JNK1), 7 nM (JNK2), 6 nM (JNK3)^[1]

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].