TGFβRII-IN-3
Based on 1 Customer Validation
TGFβRII-IN-3 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) (IC50 = 4.1 μM). TGFβRII-IN-3 inhibits TGFβ signaling by promoting the proteolytic degradation of TGFβ RII. TGFβRII-IN-3 can block endothelial-to-mesenchymal transition and cell migration. TGFβRII-IN-3 can be used in cancer research.
For research use only. We do not sell to patients.
- Purity: 99.51%
- CAS No.: 2351149-20-5
- Formula: C27H27F3N2O2
- Molecular Weight:468.51
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Storage:Powder -20°C, 3 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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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TGF-βR2 4.1 μM (IC50) |
TGFβRII-IN-3 (5-15 μM; 24 h) inhibits the activity of the TGFβ signaling pathway by reducing the phosphorylation levels of Smad2 in A549 cells and demonstrates selective degradation of TGFβ RII[1].
TGFβRII-IN-3 (2.5-10 μM; 48 h) effectively inhibits the loss of E-cadherin induced by TGFβ1, while suppressing the upregulation of Snail and N-cadherin[1].
TGFβRII-IN-3 (5 μM; 48h) inhibits cell migration and morphological changes by suppressing TGFβ signaling in A549 and H1299 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cell
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Concentration:5;10;15 μM
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Incubation Time:24h
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Result:Significantly and dose-dependently inhibited TGFβ1-induced phosphorylation of Smad2 in A549 cells.
Significantly reduced the steady-state levels of TβRII in a dose-dependent manner. At the same time, the levels of TGFβ type I receptor were not significantly affected.
Chemical Information
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CAS No. 2351149-20-5
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Appearance Powder
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Molecular Weight 468.51
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Formula C27H27F3N2O2
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Color White to off-white
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SMILES
O=C(N(CC1=CC=CC(C2=CC=C(C(F)(F)F)C=C2)=C1)C)C3=C(C)NC4=C3C(CC(C)(C4)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 4.17 mg/mL (8.90 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)
Purity & Documentation
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Data Sheet (275 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)
- 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 | 2.1344 mL | 10.6721 mL | 21.3443 mL | 53.3607 mL |
| 5 mM | 0.4269 mL | 2.1344 mL | 4.2689 mL | 10.6721 mL |
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