2. Immunology/Inflammation Apoptosis
  3. STING IFNAR TNF Receptor Interleukin Related
  4. STING-IN-15

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.

For research use only. We do not sell to patients.

STING-IN-15

STING-IN-15 Chemical Structure

CAS No. : 2912492-05-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

STING-IN-15 Related Antibodies

Top Publications Citing Use of Products

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

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.

STING-IN-15 Related Antibodies

RT-PCR[1]

Cell Line: THP1-Dual cells
Concentration: 0.3, 1, 3 μM+ MSA-2 (HY-136927) (10 μM)/cGAMP (HY-12512) (10 μM)
Incubation Time: 1 h
Result: Reduced the mRNA expression of IFNB and IP-10.

Western Blot Analysis[1]

Cell Line: THP1-Dual cells
Concentration: 0.3, 1, 3 μM+ MSA-2 (10 μM)/cGAMP (10 μM)/HT-DNA (2 μM)
Incubation Time: 1 h
Result: Inhibited TBK1/IRF3 phosphorylation.
Parmacokinetics
Species Dose Route AUC0-∞ T1/2 MRT0-∞ Bioavailability Vz CL
Rat[1] 1 mg/kg i.v. 196 ng·h/mL 0.33 h 0.38 h / 2382 mL/kg 88.1 mL/min/kg
Mice[1] 3 mg/kg p.o. 74.8 ng·h/mL 3.27 h 7.66 h 12.7 % / /
In Vivo

STING-IN-15 (10 mg/kg, i.p., single administration) effectively alleviates systemic and renal inflammation induced by MSA-2 in C57BL/6 mice by inhibiting the expression of downstream cytokines and interferon-stimulated genes[1].
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.

Animal Model: C57BL/6 (8-week-old male)[1]
Dosage: 10 mg/kg
Administration: i.p.; single dose (1 hour prior to MSA-2 stimulation)
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.
Animal Model: C57BL/6J (8-week-old male); STING-KO C57BL/6 (8-week-old male)[1]
Dosage: 5 mg/kg
Administration: i.p.; daily; 3 consecutive days (first dose 1 hour prior to cisplatin injection)
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.
Animal Model: TREX1 D18N; wild-type control[1]
Dosage: 10 mg/kg
Administration: i.p.; daily; 14 consecutive days
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.
Molecular Weight

396.35

Formula

C20H14F2N4O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CNC2=C1C=C(C=C2)/C=C/CC#N)NC3=CC4=C(C=C3)OC(F)(F)O4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5230 mL 12.6151 mL 25.2302 mL
5 mM 0.5046 mL 2.5230 mL 5.0460 mL
View the 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.

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  • Dilution Calculator

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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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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
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STING-IN-15 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

STING-IN-152912492-05-6STINGIFNARTNF ReceptorInterleukin RelatedStimulator of Interferon GenesTMEM173MITAERISMPYSInterferon-α/β receptorInterferon-alpha/beta receptor Tumor Necrosis Factor ReceptorTNFRILC57BL/6 miceBMDMsacute kidney injuryTHP1-Dual cellsRAW264.7 cellshuman STINGRAW-Lucia cellsHEK293T cellsmouse STINGInhibitorinhibitorinhibit

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