STING-Inducer-1 has enhanced binding affinity to STING and activate all known human STING alleles. STING-Inducer-1 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, STING-Inducer-1 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%.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||Water ≥ 10 mg/mL|
Direct Activation of STING in the Tumor Microenvironment Leads to Potent and Systemic Tumor Regression and Immunity.
Corrales L, et al. Cell Rep. 2015 May 19;11(7):1018-30. PMID: 25959818.
|Related STING Products|
c-di-AMP (Cyclic diadenylate) is a STING agonist, it binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway.
H-151 is a highly potent, selective and covalent antagonist of STING, reduces TBK1 phosphorylation and suppresses human STING palmitoylation.
C-178 is a covalent inhibitor of STING, binds to Cys91 on STING to block its palmitoylation.
SR-717 is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively.
C-176 is a potent small-molecule inhibitor of STING.
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