Biological Activity:GS143 is selective β-TrCP1 ligase inhibitor, inhibits IκBα ubiquitination with IC50 ~5.2 μM without affecting proteasome activity. It blocks LPS-induced expression of inflammatory cytokines in human myelomonocytic cells. It suppresses antigen-induced NFκB expression, inflammation and mucus production in airways of OVA-sensitized mice.
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