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GHN105

Chemical Structure : GHN105

CAS No.:

GHN105 (GHN-105)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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).

Physicochemical Properties

M.Wt 800.90
Formula C41H56N2O14
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

References

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