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首页-小分子抑制剂&激动剂-Immunology/Inflammation-STING-GHN105
GHN105

Chemical Structure : GHN105

CAS No.:

GHN105 (GHN-105)

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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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).

物理化学性质&存储条件

分子量 800.90
分子式 C41H56N2O14
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2aS,6S,7R,7aR,8S,10S,11R,11aS,12S,12aS,13aR,E)-6-(butyryloxy)-7a,11,13a-trimethyl-1-oxo-10-((3-(piperidin-1-yl)propanoyl)oxy)-4-((E)-((prop-2-yn-1-yloxy)imino)methyl)-1,2a,5,7,7a,8,9,10,11,11a,12,13a-dodecahydro-6H-benzo[4,5]cyclodeca[1,2-b]oxireno[2,3-c]furan-7,8,12-triyl triacetate

参考文献

1. Niu GH, et al. J Med Chem. 2025 Feb 27. doi: 10.1021/acs.jmedchem.4c02665.

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