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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References |
1. Domizio JD, Gulen MF, Saidoune F, Thacker VV, Yatim A, Sharma K, Nass T, Guenova E, Schaller M, Conrad C et al.. (2022)
The cGAS-STING pathway drives type I IFN immunopathology in COVID-19. Nature, 603 (7899): 145-151. [PMID:35045565] |
2. Haag SM, Gulen MF, Reymond L, Gibelin A, Abrami L, Decout A, Heymann M, van der Goot FG, Turcatti G, Behrendt R et al.. (2018)
Targeting STING with covalent small-molecule inhibitors. Nature, 559 (7713): 269-273. [PMID:29973723] |