1. TGF-beta/Smad Stem Cell/Wnt
  2. TGF-β Receptor TGF-beta/Smad
  3. TGFβRII-IN-3

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.

TGFβRII-IN-3 Chemical Structure

TGFβRII-IN-3 Chemical Structure

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Description

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[1].

IC50 & Target[1]

TGF-βR2

4.1 μM (IC50)

In Vitro

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.

Western Blot Analysis[1]

Cell Line: A549 cell
Concentration: 5;10;15 μM
Incubation Time: 24h
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.
Molecular Weight

454.48

Formula

C26H25F3N2O2

Unlabeled Cas

SMILES

FC(F)(F)C1=CC=C(C2=CC=CC(CN(C)C(C3=CNC4=C3C(CC(C)(C)C4)=O)=O)=C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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TGFβRII-IN-3 Related Classifications

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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.

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Product Name:
TGFβRII-IN-3
Cat. No.:
HY-161398
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