GS143

GS143 is a selective, cell-permeable small-molecule inhibitor of the E3 ubiquitin ligase complex SCF^βTrCP1 (specifically targeting β-TrCP, also known as BTRC or FBXW11). It prevents the ubiquitination and subsequent proteasomal degradation of phosphorylated IκBα (IC₅₀ = 5.2 μM) without directly inhibiting IκB kinase (IKK) phosphorylation or proteasome activity. By blocking IκBα degradation, GS143 suppresses NF-κB activation and the transcription of downstream inflammatory genes. It has been investigated in preclinical models for its potential therapeutic applications in inflammatory diseases such as asthma and rheumatoid arthritis, as well as its role as a latency-reversing agent in HIV-1 infection.

Other names

4-(3-Benzyl-4-(5-(2-fluoro-phenyl)-furan-2-ylmethylene)-5-oxo-4,5-dihydropyrazol-1-yl)-benzoic acid4-[4-[[5-(2-Fluorophenyl)-2-furanyl]methylene]-4,5-dihydro-5-oxo-3-(phenylmethyl)-1H-pyrazol-1-yl]benzoic acid