sting agonist4

STING agonist-4 is an agonist of stimulator of Interferon Genes (STING) receptor(IC50 of 20 nM).

STINGagonist-42 (compound 8a) is a potent STING agonist. It activates STING in THP1 and RAW 264.7 cells, with EC50 values of 0.06 μM and 14.15 μM, respectively.

STINGagonist-44 (Compound 4) is a potent and selective STING agonist with an EC50 value of 5.68 μM in THP1 cells and 2.212 μM in RAW cells for inducing IRF. It activates the STING pathway, leading to the production of type I interferons and pro-inflammatory cytokines (e.g., CXCL10, TNFα). STINGagonist-44 holds promise for cancer research.

STINGagonist-43 (Compound 67) is a selective STING agonist with an EC50 of 20.53 μM. It selectively enhances the cGAMP-dependent STING pathway activation by modulating STING oligomerization. STINGagonist-43 demonstrates antitumor activity in a B16.F10 mouse melanoma model and can be utilized in cancer immunotherapy research.

PPARα agonist4 (compound BH400) is a PPARα agonist with an EC50 of 1.2 μM. In addition to its primary activity, PPARα agonist4 inhibits STING with an IC50 of 8.1 μM. It also reduces reactive oxygen species production induced by CoCl2 and decreases IL-6 secretion prompted by LPS. Further, PPARα agonist4 restores the decreased expression of PCG1α caused by LPS.