TGF-β Receptors

The transforming growth factor-β family of polypeptides (TGF-β1-3) are involved in the regulation of cellular processes, including division, differentiation, motility, adhesion and death. TGF-β signals by binding the type II receptor (TGF-βRII) which activates the type I receptor (TGF-βRI).

Products
Background
Literature
Pathways
Gene Data

Inhibitors

Cat No Product Name / Activity
2939 A 83-01
Selective inhibitor of TGF-βRI, ALK4 and ALK7
2902 D 4476
TGF-βRI inhibitor. Also inhibits CK1
3264 GW 788388
Potent and selective inhibitor of TGF-βRI
6016 IN 1130
Potent and selective inhibitor of TGF-βRI
2718 LY 364947
Selective inhibitor of TGF-βRI
5288 R 268712
Potent and selective inhibitor of TGF-βRI
3742 RepSox
Potent and selective inhibitor of TGF-βRI
1614 SB 431542
Potent, selective inhibitor of TGF-βRI, ALK4 and ALK7
3263 SB 505124
Selective inhibitor of TGF-βRI, ALK4 and ALK7
3211 SB 525334
Selective inhibitor of TGF-βRI
3269 SD 208
Potent ATP-competitive TGF-βRI inhibitor

Other

Cat No Product Name / Activity
5679 N-Acetylpuromycin
Downregulates SnoN and Ski protein expression; promotes TGF-β signaling
5068 ITD 1
Selective inhibitor of TGF-β signaling; induces cardiomyocyte differentiation in ESCs
5291 SIS3
Selective Smad3 inhibitor; inhibits TGF-βR1 signaling

The transforming growth factor-β family of polypeptides (TGF-β1, TGF-β2 and TGF-β3) are involved in the regulation of cellular processes, including cell division, differentiation, motility, adhesion and death. TGF-β signals by binding the TGF-β type II receptor (TGF-βRII) which transphosphorylates and activates the type I receptor (TGF-βRI). Activated TGF-βRI then phosphorylates a subset of SMAD proteins, Smad2 and Smad3, which translocate to the nucleus where they form transcription complexes with DNA binding factors and co-activators/co-repressors.

TGF-β functions as a tumor suppressor by inhibiting the cell cycle in the G1 phase. Administration of TGF-β is able to protect against mammary tumor development in transgenic mouse models in vivo. Disruption of the TGF-β/SMAD pathway has been implicated in a variety of human cancers, with the majority of colon and gastric cancers being caused by an inactivating mutation of TGF-βRII. Homozygous deletions of TGF-βRI and inactivating mutations of SMAD genes have also been found.

A pro-oncogenic role for TGF-β has also been proposed. Once cells lose their sensitivity to TGF-β1-mediated growth inhibition, autocrine TGF-β signaling can promote tumorigenesis. Elevated levels of TGF-β1 are often observed in advanced carcinomas, and have been correlated with increased tumor invasiveness and disease progression.

Literature for TGF-β Receptors

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Immunology

Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

  • Chemokine and Cytokine Signaling
  • Chemotaxis
  • Complement System
  • Immune Cell Signaling
  • Inflammation
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Stem Cells

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.

Pathways for TGF-β Receptors

TGF-β

TGF-β Signaling Pathway

The TGF-β signaling pathway is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis.

TGF-β Receptor Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
TGF-βRI Human TGFBR1 NM_004612 P36897
Mouse Tgfbr1 BC063260 Q64729
Rat Tgfbr1 NM_012775 P80204
TGF-βRII Human TGFBR2 NM_003242 P37173
Mouse Tgfbr2 NM_009371 Q62312
Rat Tgfbr2 NM_031132 P38438
TGF-βRIII Human TGFBR3 NM_003243 Q03167
Mouse Tgfbr3 NM_011578 O88393
Rat Tgfbr3 NM_017256 P26342