Bioactivity | 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[1]. | ||||||||||||
Target | STING | ||||||||||||
Invitro | 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[1].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[1].C-178 (1 μM; 1 hour) decreases cdG, dsDNA, CMA and LPS-induced Ifnb1 expression in mouse bone marrow-derived macrophages[1].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[1]. Western Blot Analysis[1] Cell Line: | ||||||||||||
Name | C-178 | ||||||||||||
CAS | 329198-87-0 | ||||||||||||
Formula | C17H10N2O5 | ||||||||||||
Molar Mass | 322.27 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Haag SM, et al. Targeting STING with covalent small-molecule inhibitors. Nature. 2018 Jul;559(7713):269-273. |