MSA-2 (Synonyms: 5,6-dimethoxy-γ-oxo-benzobthiophene-2-Butanoic Acid) |
Catalog No.GC61092
One-Click Copy Product Info
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MSA-2 is an orally available non-nucleotide interferon gene stimulator (STING) agonist, with EC50 values of 8.3μM and 24μM for human STING subtypes WT and HAQ, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 129425-81-6
Sample solution is provided at 25 µL, 10mM.
MSA-2 is an orally available non-nucleotide interferon gene stimulator (STING) agonist, with EC50 values of 8.3μM and 24μM for human STING subtypes WT and HAQ, respectively[1]. MSA-2 exhibits higher potency in the acidic tumor microenvironment, where the small molecule undergoes non-covalent dimerization to form a bioactive ligand[2]. MSA-2 in solution exists as monomers and noncovalent dimers in an equilibrium that holds a strong tendency towards the monomeric state[3].
In vitro, MSA-2 (20-50 μM) treatment of porcine PK-15 cells infected with Seneca Valley virus (SVV) for 24 hours dose-dependently inhibited SVV replication in the cells, activated the STING signaling pathway, and induced the expression of cytokines IFN-β, IL-6, and TNF-α[4]. MSA-2 (10, 50 μM) treatment of RAW264.7 cells for 24 hours increased intracellular IFN-β levels[5]. MSA-2 (25μM) treatment of human monocytes for 20 hours eliminated LPS-induced IL-10 and IL-19 production, while IL-1β and TNF-α were not inhibited[6].
In vivo, MSA-2 (p.o. 60 mg/kg or s.c. 50 mg/kg) treatment of mice with colon cancer models effectively inhibited tumor growth and increased levels of cytokines IFN-β, IL-6, and TNF-α in tumor cells[1]. MSA-2 (150 μg) administered intrathecally to mice with colon cancer and melanoma models significantly inhibited tumor growth, improved survival rates, enhanced the infiltration and activity of cytotoxic T cells in tumors, and contributed to tumor regression[5].
References:
[1] Pan B S, Perera S A, Piesvaux J A, et al. An orally available non-nucleotide STING agonist with antitumor activity[J]. Science, 2020, 369(6506): eaba6098.
[2] Liu J, Huang X, Ding J. Identification of MSA-2: An oral antitumor non-nucleotide STING agonist[J]. Signal Transduction and Targeted Therapy, 2021, 6(1): 18.
[3] Yang J, Luo Z, Ma J, et al. A next-generation STING agonist MSA-2: From mechanism to application[J]. Journal of Controlled Release, 2024, 371: 273-287.
[4] Lin H, Zhang R, Xiang H, et al. A Non-Nucleotide STING Agonist MSA-2 Synergized with Manganese in Enhancing STING Activation to Elicit Potent Anti-RNA Virus Activity in the Cells[J]. Viruses, 2023, 15(11): 2138.
[5] Wang M, Cai Y, He T, et al. Antitumor Effect of Platinum-Modified STING Agonist MSA-2[J]. ACS omega, 2024, 9(2): 2650-2656.
Kabelitz D, Zarobkiewicz M, Heib M, et al. Signal strength of STING activation determines cytokine plasticity and cell death in human monocytes[J]. Scientific Reports, 2022, 12(1): 17827.
Cell experiment [1]: | |
Cell lines | PK-15 cells |
Preparation method | PK-15 cells were infected with SVV at a multiplicity of infection (MOI) of 10, incubated for 1 h to wash away unbound virus, and then treated with MSA-2 at concentrations of 20, 30, 40, and 50 μM for 24 h. |
Reaction Conditions | 20-50μM; 24 h |
Applications | The level of viral RNA was significantly decreased in MSA-2-treated cells in a dose-dependent manner. |
Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation method | MC38 cells were injected subcutaneously into 6-week old female C57BL/6 mice to establish tumor models. When the tumor volumes reached about 100mm3, the mice were randomly divided into 3 groups: control, MSA-2, and MSA-2-Pt. The mice were intratumor (i.t.) injected with control, 150μg of MSA-2, and 150μg of MSA-2-Pt for three doses |
Dosage form | 150μg; i.t. |
Applications | Treatment with MSA-2-Pt and MSA-2 significantly reduced tumor growth and increased survival when compared to the control group. |
References: [1] Lin H, Zhang R, Xiang H, et al. A Non-Nucleotide STING Agonist MSA-2 Synergized with Manganese in Enhancing STING Activation to Elicit Potent Anti-RNA Virus Activity in the Cells[J]. Viruses, 2023, 15(11): 2138. [2] Wang M, Cai Y, He T, et al. Antitumor Effect of Platinum-Modified STING Agonist MSA-2[J]. ACS omega, 2024, 9(2): 2650-2656. | |
| Cas No. | 129425-81-6 | SDF | |
| Synonyms | 5,6-dimethoxy-γ-oxo-benzobthiophene-2-Butanoic Acid | ||
| Canonical SMILES | O=C(C1=CC(C(S1)=C2)=CC(OC)=C2OC)CCC(O)=O | ||
| Formula | C14H14O5S | M.Wt | 294.32 |
| Solubility | DMSO: 125 mg/mL (424.71 mM) | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3977 mL | 16.9883 mL | 33.9766 mL |
| 5 mM | 679.5 μL | 3.3977 mL | 6.7953 mL |
| 10 mM | 339.8 μL | 1.6988 mL | 3.3977 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)