| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
STING-IN-16 (compound 5c) (1 μM, 24 h) inhibited STING activation, with IC50 values of 44 nM (THP1-Blue-ISG cells) and 32 nM (RAW-Lucia-ISG cells), respectively [1]. STING-IN-16 (0.3-3 μM, 3-6 h) inhibited the STING signaling pathway activated by STING activators and significantly improved the thermostability of STING in THP1 cells, BMDM cells, MEF cells and RAW264.7 mouse macrophages [1]. STING-IN-16 (1 μM, 6 h) inhibited the activation of the cGAS-STING axis triggered by cisplatin-induced DNA damage, thereby reducing ROS accumulation and apoptosis in HK2 cells [1].
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| ln Vivo |
STING-IN-16 (compound 5c) (10 mg/kg, intraperitoneal injection, once daily for 3 days) reduced cisplatin-induced inflammation in mice [1]. STING-IN-16 (10 mg/kg, intraperitoneal injection, single dose) showed anti-inflammatory efficacy in an MSA-2-induced mouse inflammation model [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: THP1 cells, BMDM cells, HK2 cells Tested Concentrations: 0.3, 1, 3 μM Incubation Duration: 6 hours Experimental Results: In THP1 cells, the inhibition of MSA-2 ( )-stimulated phosphorylation of STING, TBK1, and IRF3 was superior to that of H151 ( ). In BMDM cells, the inhibition of Vadimezan (DMXAA) ( )-stimulated phosphorylation of STING, TBK1, and IRF3 was superior to that of H151. In HK2 cells, the inhibition of cisplatin-stimulated phosphorylation of STING, TBK1, IRF3, and P65 was more potent than that of H151. It reduced the expression of apoptosis markers (such as cleaved caspase 3 and cleaved caspase 8) and DNA damage markers (γ-H2A.X and p-CHK1). Real-time quantitative PCR[1] Cell Types: THP1 cells, BMDM cells, HK2 cells Tested Concentrations: 0.3, 1, 3 μM Incubation Duration: 3, 6 h Experimental Results: In THP1 cells, the expression of MSA-2-induced cytokines (ISG15, ISG56, IFNβ, CXCL10, and CCL5) was inhibited in a dose-dependent manner. In BMDM cells, the expression of DMXAA-induced cytokines (ISG15, ISG56, IFNβ, CXCL10, and CCL5) was inhibited in a dose-dependent manner. The expression of diABZI STING agonist-1, cGAMP, and HTDNA-triggered cytokines (IFNβ, IL6, CXCL10, and ISG15) was inhibited in both THP1 and BMDM cells. It reduced the gene expression of cisplatin-induced inflammatory cytokines (such as IL6, TNFA, IL8 and CXCL10) in HK2 cells. ELISA detection [1] Cell Types: THP1 cells, BMDM cells Tested Concentrations: 0.3, 1, 3 μM Incubation Duration: 6 hours Experimental Results: In THP1 cells, MSA-2 induced a decrease in the secretion of IFN-β, CXCL10, and IL-6, with significantly higher efficacy than H151. In BMDM cells, DMXAA induced a decrease in the secretion of IFN-β, CXCL10, and IL-6, with significantly higher efficacy than H151.
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| Animal Protocol |
Animal/Disease Models:Cisplatin-induced kidney injury in male C57BL/6 mice (8 weeks old) [1]
Doses: 10 mg/kg< Route of Administration:Intraperitoneal injection, once daily for 3 consecutive days Experimental Experimental Results:Inhibited the expression of Ifnb, Il6 and Tnfa. Reduced cisplatin-induced blood urea nitrogen (BUN) elevation. Alleviated cisplatin-induced pathological changes (severe tubular dilatation, tubular necrosis and cast formation). Reduced cisplatin-induced plasma IL-6 elevation, with better effect than H151. Restored the expression of mitochondrial encoding genes (mt-CO1, mt-CO2, mt-CO3, mt-ATP6, mt-ND2 and mt-ND4). Animal/Disease Models:MSA-2-induced inflammation in male C57BL/6 mice (8 weeks old) [1] Doses: 10 mg/kg Route of Administration: Single intraperitoneal injection Experimental Results: MSA-2-induced cytokine secretion was reduced in serum, including IFN-β, CXCL10, and IL-6. MSA-2-induced expression of Ifnb and Il6 was decreased in kidney tissue. MSA-2-stimulated expression of Ifnb, Il6, and Ccl5 was decreased in heart tissue. |
| References |
| Molecular Formula |
C25H22CLN3O2
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|---|---|
| Molecular Weight |
431.91
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| CAS # |
2982807-58-7
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C(N1CCC2=C(C1)C=CC(C3=CC=C(C=C3)OC)=C2)NC4=CNC5=C4C=C(C=C5)Cl
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3153 mL | 11.5765 mL | 23.1530 mL | |
| 5 mM | 0.4631 mL | 2.3153 mL | 4.6306 mL | |
| 10 mM | 0.2315 mL | 1.1576 mL | 2.3153 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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