| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
STING-IN-7 targets the STING protein, acting as a potent antagonist. By binding to STING, it prevents its activation and subsequent signaling. It inhibits the phosphorylation of STING and interferon regulatory factor 3 (IRF3). This blockade prevents the nuclear translocation of IRF3 and the transcription of type I interferon genes, thereby dampening the innate immune response.
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| ln Vitro |
In cell-free biochemical assays, STING-IN-7 (compound 21) is a potent STING inhibitor with an IC50 of 11.5 nM. This indicates high binding affinity for the STING protein. In cellular assays, STING-IN-7 potently inhibits the phosphorylation of STING, TBK1, and IRF3. This multi-level inhibition confirms its mechanism as a direct inhibitor of the STING pathway and demonstrates cellular target engagement.
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| ln Vivo |
Specific in vivo activity data for STING-IN-7 has not been published. As a potent STING inhibitor (IC50 = 11.5 nM) that blocks phosphorylation of STING, IRF3, and TBK1, it can be used in the research of autoimmune and inflammatory diseases where STING hyperactivation plays a pathogenic role. Potential applications include studying systemic lupus erythematosus (SLE), Aicardi-Goutières syndrome, and other interferonopathies.
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| Enzyme Assay |
The specific in vitro binding protocol for STING-IN-7 uses a fluorescence polarization (FP) competition assay. Purified recombinant human STING protein (wild-type) is incubated with a fluorescently-labeled small molecule STING agonist (e.g., FAM-labeled diABZI). A serial dilution of STING-IN-7 (0.1 nM to 10 uM) is added to the reaction mixture. After 60 minutes of incubation at room temperature, FP values are measured on a plate reader. The IC50 value of 11.5 nM is calculated from the competition curve using non-linear regression analysis.
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| Cell Assay |
For in vitro cellular assays, human THP-1 monocytes (or HEK293T cells overexpressing STING) are seeded in 12-well plates. Cells are pre-incubated with STING-IN-7 at concentrations of 1 nM, 10 nM, 100 nM, and 1 uM for 2 hours, then stimulated with 2'3‘-cGAMP (5 ug/mL) for 30 minutes. Cells are lysed in RIPA buffer with protease and phosphatase inhibitors. Protein lysates are resolved by SDS-PAGE and analyzed by Western blotting using antibodies against p-STING (Ser366), p-TBK1 (Ser172), p-IRF3 (Ser396), and respective total protein controls.
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| Animal Protocol |
An in vivo protocol for a STING inhibitor would involve a mouse model of STING-dependent inflammation, such as the Trex1 knockout mouse model (Trex1-/-). At 4 weeks of age, Trex1-/- mice are randomized into treatment groups. STING-IN-7 is dissolved in a suitable vehicle (e.g., 10% DMSO/40% PEG400/50% water) and administered daily by intraperitoneal injection at doses of 1, 3, and 10 mg/kg for 8 weeks. Control groups receive vehicle only. Mice are weighed weekly and scored for signs of autoimmunity (skin lesions, hunched posture). At termination, hearts are collected for H&E staining to assess inflammatory infiltrates. Sera are collected for IFN-beta ELISA.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for STING-IN-7 has not been published. As a potent small molecule STING inhibitor, a standard pharmacokinetic study would be conducted in male C57BL/6 mice. The compound would be administered via intravenous (1 mg/kg) and oral (5 mg/kg) routes. Plasma samples would be collected at multiple time points (0-24 hours) and analyzed by LC-MS/MS. Key parameters including T1/2, Cmax, AUC0-∞, clearance, and oral bioavailability would be calculated.
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| Toxicity/Toxicokinetics |
Toxicology data for STING-IN-7 is not widely available. As a STING inhibitor that blocks type I interferon production, the primary safety concern would be an increased risk of viral infections due to impaired innate immune responses. Standard preclinical safety evaluation would include a 7-day repeat-dose toxicity study in rats to determine the maximum tolerated dose (MTD). Hematological parameters (including white blood cell counts) and histopathology of lymphoid organs would be assessed.
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| References | |
| Additional Infomation |
STING-IN-7 is a research-grade compound and is not approved for clinical use. Its molecular formula is C16H14ClN3O with a molecular weight of 299.75. It is a potent STING inhibitor with an IC50 of 11.5 nM. STING-IN-7 inhibits the phosphorylation of STING and IRF3. The compound can be used in the research of autoimmune and inflammatory diseases. It is a valuable tool for validating STING as a therapeutic target for conditions characterized by excessive type I interferon production.
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| Molecular Formula |
C16H14CLN3O
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| Molecular Weight |
299.754862308502
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| Exact Mass |
299.082
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| CAS # |
899947-07-0
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| PubChem CID |
7616083
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| Appearance |
White to off-white solid powder
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| LogP |
3.6
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
379
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N(C1=CC=C(C)C(Cl)=C1)C(NC1C2=C(NC=1)C=CC=C2)=O
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| InChi Key |
FWAWUBPOSFYSMU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H14ClN3O/c1-10-6-7-11(8-13(10)17)19-16(21)20-15-9-18-14-5-3-2-4-12(14)15/h2-9,18H,1H3,(H2,19,20,21)
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| Chemical Name |
1-(3-chloro-4-methylphenyl)-3-(1H-indol-3-yl)urea
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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 | 3.3361 mL | 16.6806 mL | 33.3611 mL | |
| 5 mM | 0.6672 mL | 3.3361 mL | 6.6722 mL | |
| 10 mM | 0.3336 mL | 1.6681 mL | 3.3361 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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