TGFβ-IN-2
Based on 1 publication(s) in Google Scholar
TGFβ-IN-2 is an orally active TGF-β inhibitor. TGFβ-IN-2 suppresses the TGF-β-induced protein expression of COL1A1, α-SMA, and p-Smad3 in vitro. TGFβ-IN-2 demonstrates excellent anti-fibrotic efficacy in Bleomycin (HY-108345)-induced pulmonary fibrosis model. TGFβ-IN-2 can be used for the study of pulmonary fibrosis.
For research use only. We do not sell to patients.
- Purity : 99.37%
- CAS No.: 2387678-02-4
- Formula: C22H22N2O4
- Molecular Weight:378.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) TGFβ-IN-2
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| NRK-49F | IC50 |
4.31 μM
Compound: 9d
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Inhibition of TGF-beta-induced collagen accumulation in rat NRK-49F cells incubated for 2 days by PSR staining based microscopic analysis
Inhibition of TGF-beta-induced collagen accumulation in rat NRK-49F cells incubated for 2 days by PSR staining based microscopic analysis
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[PMID: 31699535] |
In Vitro
TGFβ-IN-2 (Compound 9d) (10 μM, 72 h) shows 85.14% inhibition at 10 μM of TGF-β-induced total collagen accumulation in NRK-49F cells with a 93.62% cell survival rate[1].
TGFβ-IN-2 (10 μM) inhibits TGF-β-induced total collagen accumulation in NRK-49F cells with an IC50 of 4.31 μM[1].
TGFβ-IN-2 (1 μM, 24 h) exhibits the most potent inhibition on fibroblasts-driven macrophage migration in vitro compared to other compounds[1].
TGFβ-IN-2 (20-40 μM) suppresses TGF-β1-induced protein expression of COL1A1, α-SMA, and p-Smad3 in NRK-49F cells, indicating inhibition of the TGF-β/Smad3 pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Bleomycin (HY-108345) (2 U/kg) was intratracheally instilled into 7-8-week-old male C57BL/6 mice to induce pulmonary fibrosis model[1].
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Dosage:50, 100 mg/kg
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Administration:p.o. daily for 4 weeks
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Result:Reduced hydroxyproline content in lung tissues.
Alleviated alveolar structure destruction.
Decreased inflammatory cell infiltration in lung tissue and bronchoalveolar lavage fluid (BALF).
Improved survival rate to about 90% in bleomycin-induced pulmonary fibrosis model.
Did not inhibit fibrosis50 mg/kg.
Chemical Information
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CAS No. 2387678-02-4
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Appearance Solid
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Molecular Weight 378.42
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Formula C22H22N2O4
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Color White to off-white
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SMILES
O=C(NC1=CC=C(C=C1)OC2=CC(OC3=CC=CC=C32)=O)CN4CCCCC4
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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 (1)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Highly Bioadaptable Hybrid Conduits with Spatially Bidirectional Structure for Precision Nerve Fiber Regeneration via Gene Therapy. [Abstract]2024 May;11(19):e2309306. PMID: 38483934
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (264.26 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: ≥ 5 mg/mL (13.21 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (13.21 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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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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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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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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 Protein Expression And Purification
Recombinant protein expression in Escherichia coli followed by purification of a His-tagged soluble protein by immobilized metal affinity chromatography (IMAC), with optional MBP fusion and TEV tag removal when the construct includes these elements. The biological readout is production of the encoded target protein, detected as an inducible band at the expected molecular mass by SDS-PAGE and quantified by total protein assay or chromatographic absorbance; the purification readout is enrichment of the target protein in elution fractions after selective binding of polyhistidine residues to immobilized Ni2+/metal-chelate resin and elution by imidazole-containing buffer. Expression is driven by an inducible bacterial expression system, commonly T7/lac-based, in which IPTG or lactose/auto-induction activates transcription and translation of the cloned gene; lower induction temperature, lower inducer concentration, induction timing, and solubility-enhancing fusion tags can influence the frac
Purity & Documentation
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Data Sheet (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 | 2.6426 mL | 13.2128 mL | 26.4257 mL | 66.0642 mL |
| 5 mM | 0.5285 mL | 2.6426 mL | 5.2851 mL | 13.2128 mL | |
| 10 mM | 0.2643 mL | 1.3213 mL | 2.6426 mL | 6.6064 mL | |
| 15 mM | 0.1762 mL | 0.8809 mL | 1.7617 mL | 4.4043 mL | |
| 20 mM | 0.1321 mL | 0.6606 mL | 1.3213 mL | 3.3032 mL | |
| 25 mM | 0.1057 mL | 0.5285 mL | 1.0570 mL | 2.6426 mL | |
| 30 mM | 0.0881 mL | 0.4404 mL | 0.8809 mL | 2.2021 mL | |
| 40 mM | 0.0661 mL | 0.3303 mL | 0.6606 mL | 1.6516 mL | |
| 50 mM | 0.0529 mL | 0.2643 mL | 0.5285 mL | 1.3213 mL | |
| 60 mM | 0.0440 mL | 0.2202 mL | 0.4404 mL | 1.1011 mL | |
| 80 mM | 0.0330 mL | 0.1652 mL | 0.3303 mL | 0.8258 mL | |
| 100 mM | 0.0264 mL | 0.1321 mL | 0.2643 mL | 0.6606 mL |
TGFβ-IN-2 Related Classifications
HY-146434 Related Classifications
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