C-178 is a potent and selective covalent inhibitor of STING. C-178 binds to Cys91 and suppresses the STING responses elicited by distinct bona fide activators in mouse but not human.
体外研究
C-178 targets the poorly characterized N-terminal portion of mmSTING that includes the transmembrane domains. Moreover, C-178 interferes with this process by inhibiting the palmitoylation of STING. C-178 does not appreciably affect STING responses in human cells. C-178 (0-1 μM; 1 hour) alone does not appreciably affect the gene expression profile of BMDMs. In addition, it inhibits the CMA-induced phosphorylation of TBK1. C-178 (1 μM; 1 hour) decreases cdG, dsDNA, CMA and LPS-induced Ifnb1 expression in mouse bone marrow-derived macrophages. C-178 (1 μM; 0.5-4 hours) inhibits the CMA-induced p-TBK1 and sting protein expression as a time-dependent manner in mouse embryonic fibroblasts.
Western Blot Analysis
Cell Line:
Mouse bone marrow-derived macrophages (BMDMs)
Concentration:
0 μM; 0.125 μM; 0.25 μM; 0.5 μM; 1 μM
Incubation Time:
1 hour
Result:
Inhibited CMA-induced p-TBK1 expression as a does dependent manner.
RT-PCR
Cell Line:
Mouse bone marrow-derived macrophages (BMDMs)
Concentration:
1 μM
Incubation Time:
1 hour
Result:
Downregulated Ifnb1 expression in BMDMs.
分子式
C17H10N2O5
分子量
322.27
CAS号
329198-87-0
运输条件
Room temperature in continental US; may vary elsewhere.