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.

STINGagonist-45 is a selective STING agonist (EC50= 0.28 μM) that activates the innate immune response through the cGAS-STING pathway, increasing key markers such as p-TBK1 and IRF3. This compound exhibits potent STING activation in human peripheral blood mononuclear cells (PBMC), inducing type I interferons like IFN-β and downstream cytokines such as TNF-α and IL-6. In mouse models, STINGagonist-45 enhances anti-tumor immunity, inhibits tumor growth, and increases CD8+ T cell infiltration. It is applicable for research on STING-associated diseases.

STINGagonist-46 is an orally active STING agonist that activates the STING signaling pathway, leading to the phosphorylation of TBK1 and IRF3, and enhances the secretion of IFN-β and IP-10. It directly binds to STING, increasing its thermal stability. In B16F10, CT26, and 4T1 mouse models, STINGagonist-46 demonstrates potent antitumor efficacy. This compound can be utilized for research in cancer immunotherapy.

STINGagonist-47 is a STING agonist with an EC50 of 0.72 μM and a Kd of 176 nM. It is a dimer of MSA-2 and is applicable in cancer research, including studies on breast cancer.

STINGagonist-49 (Compound 1) is a STING agonist that serves as a payload for ADCs. It is applicable in lung cancer research.

STINGagonist-49-PAB-Ala-Val-CO-C2-mal is a peptide-cSTING linker-payload, used as a Drug-Linker Conjugate for ADC (Antibody-Drug Conjugate). It serves as a component for ADC synthesis.

STINGagonist-49-β-D-Glu-benzylalcohol-di(amide-C2)-mal (compound gluc-cSTING linker-payload) is a drug-linker conjugate used in antibody-drug conjugates (ADC). STINGagonist-49-PAB-Ala-Val-CO-C2-mal is applicable for ADC synthesis.

STINGagonist-49-CO-C2-mal-Cys (compound 2) is a derivative of STINGagonist-49-CO-C2-mal, resulting from the metabolism and payload release of an ADC, and exhibits antitumor activity in vivo.

STINGagonist-49-CO-C2-mal (compound ncSTING linker-payload) is a non-cleavable Drug-Linker Conjugate for ADC (Antibody-Drug Conjugates). This compound is used in the synthesis of ADCs.

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.