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ADU-S100 (MIW815; ML RR-S2 CDA) has enhanced binding affinity to STING and activate all known human STING alleles. 2’3’-c-di-AM(PS)2 (Rp,Rp) (ADU-S100) induces the highest expression of IFN-β and the pro-inflammatory cytokines TNF-α, IL-6, and MCP-1 on a molar equivalent basis, as compared to endogenous ML cGAMP and the TLR3 agonist poly I:C. ML RR-S2 CDA is also found to induce aggregation of STING and induce phosphorylation of TBK1 and IRF3 in mouse bone marrow macrophage (BMM). ML RR-S2 CDA induces significantly higher levels of IFN-α when compared to ML cGAMP.
In vivo, 2’3’-c-di-AM(PS)2 (Rp,Rp) (ADU-S100) shows higher anti-tumor control than the endogenous ML cGAMP. A dose response of the ML RR-S2 CDA compound is performed in B16 tumor-bearing mice, which identifies an optimal antitumor dose level that also elicites maximum tumor antigen-specific CD8+ T cell responses, and improves long-term survival to 50%.
| Molecular Weight | 690.54 |
| Formula | C20H24N10O10P2S2 |
| CAS Number | 1638241-89-0 |
| Solubility (25°C) | Water ≥ 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related STING Products |
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| Vadimezan
Vadimezan (DMXAA; ASA-404) acts as a tumor vascular disrupting agent (tumor-VDA), is also a murine agonist of the stimulator of interferon genes (STING) and also a potent inducer of type I IFNs and other cytokines. |
| G10
G10 is a activator of STING-dependent signaling. |
| 3′3′-cGAMP
3',3'-cGAMP is an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. 3',3'-cGAMP activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators. |
| diABZI (tautomerism)
diABZI (STING agonist 1; Tautomerism) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively. |
| C-176
C-176 is a potent, selective and blood-brain barrier permeable inhibitor of STING. C-176 covalently targets transmembrane cysteine residue 91 and thereby blocking activation-induced palmitoylation of STING. |
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