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.

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TGFβRII-IN-3

TGFβRII-IN-3 Chemical Structure

CAS No. : 2351149-20-5

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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

468.51

Formula

C27H27F3N2O2

CAS No.
Appearance

Powder

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1344 mL 10.6721 mL 21.3443 mL
5 mM 0.4269 mL 2.1344 mL 4.2689 mL
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* 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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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 2.1344 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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  • 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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