STAT3-IN-15
Based on 2 publication(s) in Google Scholar
STAT3-IN-15 is a potent and orally active STAT3 inhibitor against idiopathic pulmonary fibrosis (IPF). STAT3-IN-15 inhibits STAT3 phosphorylation. STAT3-IN-15 also inhibits the migration and deformation of epithelial cells induced by TGF-β1 and inhibit epithelial-mesenchymal transition (EMT).
For research use only. We do not sell to patients.
- Purity : 98.99%
- CAS No.: 3037596-35-0
- Formula: C20H17F3N2O3S
- Molecular Weight:422.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) STAT3-IN-15
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Biological Activity
Description
IC50 & Target
[1]|
STAT3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NIH3T3 | IC50 |
0.47 μM
Compound: 10K
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Antiproliferative activity against mouse NIH3T3 cells assessed as cell growth inhibition incubated for 24 to 72 hrs by CCK-8 assay
Antiproliferative activity against mouse NIH3T3 cells assessed as cell growth inhibition incubated for 24 to 72 hrs by CCK-8 assay
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[PMID: 36463728] |
In Vitro
STAT3-IN-15 (compound 10k) inhibits NIH-3T3 cell proliferation with an IC50 of 0.47 μM[1].
STAT3-IN-15 forms hydrogen bonds with Lys591 and Ser636, occupying the pY subpocket of STAT3[1].
STAT3-IN-15 (0-100 nM, 72 h) inhibits fibroblast activation and proliferation[1].
STAT3-IN-15 (50 nM, 24 h) inhibited TGF-β1 (5 ng/mL)-induced activation of NIH-3T3 cells[1].
STAT3-IN-15 (200 nM, 24 h) blocks TGF-β1 induced EMT process in A549 cells, determined by morphological changes[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:NIH-3T3 cells
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Concentration:0, 6.25, 12.5, 25, 50, 100 nM
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Incubation Time:72 h
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Result:Inhibited NIH-3T3 cell viability dose-dependently.
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Cell Line:NIH-3T3 cells
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Concentration:Inhibited NIH-3T3 cell viability dose-dependently.
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Incubation Time:24 h
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Result:Inhibited the expression of α-SMA and collagen I and the phosphorylation of STAT3.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BLM-induced pulmonary fibrosis mouse model[1]
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Dosage:30 and 60 mg/kg
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Administration:Intragastric administration
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Result:Recovered the lung structure and reduced the hydroxyproline content.
Reduced the expression of the p-Stat3Ty705 protein in the lung tissue.
Improved BLM-induced imbalance of immune microenvironment.
Chemical Information
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CAS No. 3037596-35-0
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Appearance Solid
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Molecular Weight 422.42
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Formula C20H17F3N2O3S
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Color Off-white to light yellow
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SMILES
O=C(N1CCN(CC1)CC2=CC(F)=C(C=C2F)F)C3=CC4=CC=CC=C4S3(=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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iScience
Roquin-1 resolves sepsis-associated acute liver injury by regulating inflammatory profiles via miRNA cargo in extracellular vesicles. [Abstract]2023 Jul 12;26(8):107295. PMID: 37554446
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (236.73 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.
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.
Protocols
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Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
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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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Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
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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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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
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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.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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 | 2.3673 mL | 11.8366 mL | 23.6731 mL | 59.1828 mL |
| 5 mM | 0.4735 mL | 2.3673 mL | 4.7346 mL | 11.8366 mL | |
| 10 mM | 0.2367 mL | 1.1837 mL | 2.3673 mL | 5.9183 mL | |
| 15 mM | 0.1578 mL | 0.7891 mL | 1.5782 mL | 3.9455 mL | |
| 20 mM | 0.1184 mL | 0.5918 mL | 1.1837 mL | 2.9591 mL | |
| 25 mM | 0.0947 mL | 0.4735 mL | 0.9469 mL | 2.3673 mL | |
| 30 mM | 0.0789 mL | 0.3946 mL | 0.7891 mL | 1.9728 mL | |
| 40 mM | 0.0592 mL | 0.2959 mL | 0.5918 mL | 1.4796 mL | |
| 50 mM | 0.0473 mL | 0.2367 mL | 0.4735 mL | 1.1837 mL | |
| 60 mM | 0.0395 mL | 0.1973 mL | 0.3946 mL | 0.9864 mL | |
| 80 mM | 0.0296 mL | 0.1480 mL | 0.2959 mL | 0.7398 mL | |
| 100 mM | 0.0237 mL | 0.1184 mL | 0.2367 mL | 0.5918 mL |