Selonsertib

Selonsertib is an inhibitor of apoptosis signal-regulating kinase 1 (ASK1; IC₅₀ = 5.01 nM).¹ It decreases apoptosis and stellate cell activation in an in vitro 3D-human liver microtissue model of non-alcoholic steatohepatitis (NASH) induced by palmitic acid (Item No. 10006627) when used at a concentration of 1 µM.² Selonsertib (10 µM) sensitizes KB-C2 epidermoid carcinoma cells, which endogenously express ATP-binding cassette family B member 1 (ABCB1), to doxorubicin (Item No. 15007) and paclitaxel (Item No. 10461).³ It reduces hepatic necrosis and increases in serum TNF-α, IL-6, and chemokine (C-C motif) ligand 2 (CCL2) levels in a mouse model of LPS/D-galactosamine-induced acute liver failure when administered at doses of 15, 30, or 60 mg/kg.⁴

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1. Lanier, M., Pickens, J., Bigi, S.V., et al. Structure-based design of ASK1 inhibitors as potential agents for heart failure. ACS Med. Chem. Lett. 8(3), 316-320 (2017).

2. Mukherjee, S., Zhelnin, L., Sanfiz, A., et al. Development and validation of an in vitro 3D model of NASH with severe fibrotic phenotype. Am. J. Transl. Res. 11(3), 1531-1540 (2019).

3. Ji, N., Yang, Y., Cai, C.-Y., et al. Selonsertib (GS-4997), an ASK1 inhibitor, antagonizes multidrug resistance in ABCB1- and ABCG2-overexpressing cancer cells. Cancer Lett. 440-441, 82-93 (2018).

4. Lou, G., Li, A., Cen, Y., et al. Selonsertib, a potential drug for liver failure therapy by rescuing the mitochondrial dysfunction of macrophage via ASK1-JNK-DRP1 pathway. Cell Biosci. 11(1), 9 (2021).