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The cGAS-STING pathway is a cellular DNA sensor that’s involved in innate immunity. It senses the DNA of invading microorganisms and releases a messenger molecule (cGAMP) which stimulates the cell to respond. One practical application is in cancer immunotherapy.


STING (Stimulator of Interferon Genes) is an endoplasmic reticulum-associated transmembrane protein that is essential for activation of the innate immune system in response to the sensing of cytosolic DNA.1,2,3 It controls the transcription of numerous defenses including type I interferons and pro-inflammatory cytokines. In addition to detecting pathogenic DNA, it may react to self-DNA resulting in autoinflammatory diseases and inflammation-associated cancers.4,5 Conversely, STING agonists are potential cancer immunotherapy enhancers.6

DMXAA - 10-2676

STING (Stimulator of Interferon Genes) agonist selective for mouse STING. 7,8 Intratumoural administration of DMXAA resulted in tumour regression and complete rejection in mouse xenografts. 9

2', 3' -cGAMP - 10-1639

Endogenous STING (Stimulator of Interferon Genes) agonist. 10 Produced from ATP and GTP via the action of cGMP-AMP synthase (cGAS) which acts as a cytosolic DNA sensor. 11, 12 Induces autophagy which is a mechanism for clearance of DNA and viruses in the cytosol. 13 DNA damage stimulates 2', 3'- cGAMP which stimulates an inflammatory response. 14

H-151 - 10-4132

H-151 is an inhibitor of the signalling molecule STING in mouse and human cells. 15 It covalently binds to Cys91 of STING preventing activation via blockade of palmitoylation at Cys91. It reduced systemic cytokine response in mice treated with the STING agonist 10-carboxymethyl-9-acridanone and showed efficacy in Trex-/- mice.

C-176 - 10-4130

C-176 is an inhibitor of STING in mouse cells. 15 Treatment of Trex-/-mice with C-176 resulted in a significant reduction in serum levels of Type I Interferons and amelioration of systemic inflammation.

C-178 - 10-4131

C-178 is an inhibitor of the signalling molecule STING in mouse cells. 15