Chemical Structure : GHN105
货号: PC-24093Not For Human Use, Lab Use Only.
GHN105 is a specific, orally bioavailable, covalent STING inhibitor, selectively targets the membrane-proximal Cys91 residue of STING, inhibits IFN-β levels in culture supernatants of THP1 macrophages with IC50 of 4.4 uM.
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GHN105 is a specific, orally bioavailable, covalent STING inhibitor, selectively targets the membrane-proximal Cys91 residue of STING, inhibits IFN-β levels in culture supernatants of THP1 macrophages with IC50 of 4.4 uM.
GHN105 dose-dependently inhibits cGAS-STING signaling and type I interferon responses in cells and in vivo.
GHN105 strongly reduced dsDNA-induced phosphorylation of STING, TANK-binding kinase 1 (TBK1), and IFN regulatory factor 3 (IRF3) in murine NIH3T3 cells.
GHN105 suppressed host antiviral responses in human mesenchymal stem cells.
GHN105 exhibited on-target engagement in vivo and markedly reversed key pathological features in a delayed treatment of the acute colitis mouse model.
GHN105 has efficacy against the most common hSTING allele as well as the pathogenic variant causing STING-associated vasculopathy in infants (SAVI).
分子量 | 800.90 | |
分子式 | C41H56N2O14 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Niu GH, et al. J Med Chem. 2025 Feb 27. doi: 10.1021/acs.jmedchem.4c02665.
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