Synonyms: H 151 | H151
Compound class:
Synthetic organic
Comment: H-151 is a small molecule covalent STING antagonist [2]. Mechanistically it binds to Cys91 of the protein and prevents its palmitoylation. The non-modified STING protein is then unable to assemble the STING complexes that are essential to activate downstream processes (e.g. Type I interferon response). H-151 has been reported to reduce SARS-CoV-2-induced lung inflammation and to improve disease outcome in ACE2-humanised mice [1].
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Bioactivity Comments |
H-151 inhibits IFNβ luciferase reporter activation in HEK293 cells expressing human STING [2]. The authors (Haag et al., 2018) show direct interaction of H-151 and STING, and STING functional inhibition by H-151 using various methodologies but no inhibitory constant value is provided in the article. From Figure 5b it looks as though half-maximal inhibition in the IFNβ reporter assay occurs in the 50-100 nM range. |
Selectivity at other protein targets | ||||||||||||||||||||||||||||||||||
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