C-178 is a covalent inhibitor of STING, binds to Cys91 on STING to block its palmitoylation. C-178 targets the poorly characterized N-terminal portion of mmSTING that includes the transmembrane domains. C-178 decreases cdG, dsDNA, CMA and LPS-induced Ifnb1 expression in mouse bone marrow-derived macrophages.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥ 35 mg/mL|
Targeting STING with covalent small-molecule inhibitors
Simone M Haag, et al. Nature. 2018 Jul;559(7713):269-273. PMID: 29973723.
|Related STING Products|
c-di-AMP (Cyclic diadenylate) is a STING agonist, it binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway.
H-151 is a highly potent, selective and covalent antagonist of STING, reduces TBK1 phosphorylation and suppresses human STING palmitoylation.
SR-717 is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively.
C-176 is a potent small-molecule inhibitor of STING.
|diABZI STING agonist 1 (compound 3)
diABZI STING agonist-1 (compound 3) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.
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