STING-IN-15
Based on 1 publication(s) in Google Scholar
STING-IN-15 is an orally active STING inhibitor, with an IC50 of 116 nM against h-STING and an IC50 of 96.3 nM against m-STING. STING-IN-15 inhibits the STING signaling pathway in cells, reduces the secretion of IFN-β and IP-10, downregulates the expression of ISG15, ISG56 and TNF-α, and suppresses the phosphorylation of TBK1/IRF3. STING-IN-15 alleviates systemic and renal inflammation induced by STING agonists in mice, reduces tissue damage and the expression of interferon pathway genes, and inhibits spontaneous tissue inflammation in mice. STING-IN-15 can be used for the research of acute kidney injury and autoimmune/inflammatory diseases.
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- Pureté : 99.04%
- CAS No.: 2912492-05-6
- Formule: C20H14F2N4O3
- Masse moléculaire:396.35
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) STING-IN-15
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Activité biologique
Description
In Vitro
STING-IN-15 (Compound 66) (0.3-3 μM; 1 h pretreatment, 4-24 h stimulation) dose-dependently inhibits the STING signaling pathway in human THP1-Dual cells at concentrations of 0.3, 1, and 3 μM, reducing cytokine secretion, inflammatory gene expression, and downstream protein phosphorylation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:THP1-Dual cells
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Concentration:0.3, 1, 3 μM+ MSA-2 (HY-136927) (10 μM)/cGAMP (HY-12512) (10 μM)
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Incubation Time:1 h
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Result:Reduced the mRNA expression of IFNB and IP-10.
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Cell Line:THP1-Dual cells
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Concentration:0.3, 1, 3 μM+ MSA-2 (10 μM)/cGAMP (10 μM)/HT-DNA (2 μM)
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Incubation Time:1 h
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Result:Inhibited TBK1/IRF3 phosphorylation.
Parmacokinetics
In Vivo
STING-IN-15 (5 mg/kg; i.p.; once daily for 3 consecutive days) exerts STING-dependent protective effects in C57BL/6J mice, targeting Cisplatin (HY-1739)-induced acute kidney injury, and reduces tissue damage and the expression of interferon pathway genes[1].
STING-IN-15 (10 mg/kg; i.p.; once daily for 14 consecutive days) effectively suppresses spontaneous tissue inflammation in TREX1D18N mice and reduces the expression levels of inflammatory cytokines and interferon-stimulated genes in renal and cardiac tissues[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (8-week-old male)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose (1 hour prior to MSA-2 stimulation)
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Result:Significantly suppressed MSA-2-induced elevations in plasma IL-6 and IP-10 levels.
Significantly inhibited MSA-2-induced increases in renal mRNA expression of IL-6, Tnf-α, Cxcl-10, Isg15, and Isg56.
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Animal Model:C57BL/6J (8-week-old male); STING-KO C57BL/6 (8-week-old male)[1]
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Dosage:5 mg/kg
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Administration:i.p.; daily; 3 consecutive days (first dose 1 hour prior to cisplatin injection)
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Result:Largely prevented cisplatin-induced glomerular injury and interstitial vacuolation in wild-type mice.
Significantly reduced cisplatin-induced increases in renal mRNA expression of Ifn-β, Isg15, Isg56, and Cxcl-10 in wild-type mice.
No protective effects on kidney histology or gene expression were observed in STING-KO mice.
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Animal Model:TREX1 D18N; wild-type control[1]
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Dosage:10 mg/kg
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Administration:i.p.; daily; 14 consecutive days
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Result:Significantly reduced elevated renal mRNA expression of Il6, Cxcl10, Isg15, Isg56, Ifn-β, and Ccl5 in TREX1 D18N mice.
Significantly reduced elevated cardiac mRNA expression of Il6, Cxcl10, Isg15, Isg56, Ifn-β, and Ccl5 in TREX1 D18N mice.
Chemical Information
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CAS No. 2912492-05-6
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Appearance Solid
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Masse moléculaire 396.35
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Formule C20H14F2N4O3
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Color White to off-white
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SMILES
O=C(NC1=CNC2=C1C=C(C=C2)/C=C/CC#N)NC3=CC4=C(C=C3)OC(F)(F)O4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (252.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Nephrotoxicity Study
This protocol assesses nephrotoxicity by combining functional kidney injury readouts, urinary/tissue injury biomarkers, and renal histopathology. Serum creatinine and BUN reflect impaired kidney function, while KIM-1, NGAL, clusterin, osteopontin, IL-18, cystatin C, nephrin, Oat5, urinary protein, glucose, and alkaline phosphatase have been used to detect tubular injury in cisplatin-, gentamicin-, and acetaminophen-induced nephrotoxicity models.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureté et documentation
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Fiche technique (277 KB)
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SDS (251 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.5230 mL | 12.6151 mL | 25.2302 mL | 63.0756 mL |
| 5 mM | 0.5046 mL | 2.5230 mL | 5.0460 mL | 12.6151 mL | |
| 10 mM | 0.2523 mL | 1.2615 mL | 2.5230 mL | 6.3076 mL | |
| 15 mM | 0.1682 mL | 0.8410 mL | 1.6820 mL | 4.2050 mL | |
| 20 mM | 0.1262 mL | 0.6308 mL | 1.2615 mL | 3.1538 mL | |
| 25 mM | 0.1009 mL | 0.5046 mL | 1.0092 mL | 2.5230 mL | |
| 30 mM | 0.0841 mL | 0.4205 mL | 0.8410 mL | 2.1025 mL | |
| 40 mM | 0.0631 mL | 0.3154 mL | 0.6308 mL | 1.5769 mL | |
| 50 mM | 0.0505 mL | 0.2523 mL | 0.5046 mL | 1.2615 mL | |
| 60 mM | 0.0421 mL | 0.2103 mL | 0.4205 mL | 1.0513 mL | |
| 80 mM | 0.0315 mL | 0.1577 mL | 0.3154 mL | 0.7884 mL | |
| 100 mM | 0.0252 mL | 0.1262 mL | 0.2523 mL | 0.6308 mL |
STING-IN-15 Related Classifications
HY-173425 Related Classifications
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