2. Signaling Pathways
  3. TGF-beta/Smad
  4. TGF-β Receptor

TGF-β Receptor

Transforming growth factor beta receptors

TGF-β Receptor

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TGF-β receptors (Transforming growth factor-β receptors) are single pass serine/threonine kinase receptors. Transforming growth factor beta (TGF-beta) is a member of a large family of pleiotropic cytokines that are involved in many biological processes, including growth control, differentiation, migration, cell survival, adhesion, and specification of developmental fate, in both normal and diseased states. TGF-beta superfamily members signal through a receptor complex comprising a type II and type I receptor, both serine/threonine kinases.

The type I receptors, referred to as activin receptor-like kinases (ALK), lie at the epicenter of the signaling cascade as they transduce TGF-beta signals to intracellular regulators of transcription known as Smad proteins. ALKs possess an extracellular binding domain, a transmembrane domain, a GS domain that serves as the site of activation by type II receptors, and a kinase domain that activates downstream signaling molecules. ALKs mediate the effect of TGF-beta superfamily on a variety of cellular processes such as proliferation, differentiation, apoptosis, adhesion and migration, and therefore play important roles in many biological processes. Some ALKs have been implicated in several disorders, including tumorigenesis and immune diseases, suggesting that these receptors can be used as drug targets.

TGF-β Receptor Isoform Specific Products:

TGF-β Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-112877
    ALK-5-IN-1
    		Inhibitor
    ALK-5-IN-1 is an ALK-5 inhibitor. ALK-5-IN-1 can be used for the research of cancer, and conditions involving fibrosis.
    ALK-5-IN-1
  • HY-113604
    Pentabromopseudilin
    		Inhibitor
    Pentabromopseudilin (PBrP) is a marine antibiotic isolated from the marine bacteria Pseudomonas bromoutilis and Alteromonas luteoviolaceus. PBrP exhibits antimicrobial, anti-tumour and phytotoxic activities. PBrP is a reversible and allosteric inhibitor of myosin Va (MyoVa). PBrP also is a potent inhibitor of transforming growth factor-β (TGF-β) activity. PBrP can be used for the research of fibrotic diseases and cancer.
    Pentabromopseudilin
  • HY-161376
    M4K2281
    		Inhibitor
    M4K2281 is a selecitve inhibitor for activin receptor-like kinase-2 (ALK2) with an IC50 of 2 nM. M4K2281 exhibits a moderate blood brain permeability with a brain to plasma ratio of 3.7 at 4h.
    M4K2281
  • HY-144437
    ALK5-IN-9
    		Inhibitor
    ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC50 values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease.
    ALK5-IN-9
  • HY-151283
    ALK5-IN-33
    		Inhibitor
    ALK5-IN-33 (Compound EX-10) is a selective, orally active ALK-5 inhibitor with an IC50 ≤10 nM.
    ALK5-IN-33
  • HY-162929
    TP-DEA2
    		Inhibitor
    TP-DEA2, a predictable-release Triptolide (HY-32735) prodrug, block Bleomycin-induced pulmonary fibrosis and inflammation. TP-DEA2 significantly inhibits α-SMA production.
    TP-DEA2
  • HY-161662
    ALK5-IN-80
    		Inhibitor
    ALK5-IN-80 (Compound 29b) is a selective ALK5 inhibitor with an IC50 value of 3.7 nM. ALK5-IN-80 can be used for cancer research.
    ALK5-IN-80
  • HY-P3970
    KRFK
    		Agonist
    KRFK, a peptide derived from TSP-1, can activate TGF-β. KRFK promotes TGF-β-mediated signaling and its downstream role, independent of thrombospondin (TSP) receptors such as CD47 and CD36. KRFK can be used for chronic ocular surface inflammatory disorders reseach.
    KRFK
  • HY-163429
    J-1149
    		Inhibitor
    J-1149 is a potent ALK5 inhibitor, with an IC50 value of 0.017 μM. J-1149 also shows weak p38α MAP kinase inhibitory activity, with an IC50 value of 0.435 μM. J-1149 can be used for liver fibrosis research.
    J-1149
  • HY-151281
    ALK5-IN-31
    		Inhibitor
    ALK5-IN-31 (compound Ex-08) is a selective ALK-5 inhibitor (IC50≤10 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-31 has the potential to inhibit growth of tumour in vivo. ALK5-IN-31 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis.
    ALK5-IN-31
  • HY-P10363
    Tiger17
    		Activator
    Tiger17 is an effective wound healing agent. Tiger17 is able to induce the secretion of TGF-β1 and acts through the Smad signaling pathway, specifically promoting wound healing by increasing the phosphorylation of Smad2 and Smad3.
    Tiger17
  • HY-147786
    TGFβRI-IN-5
    		Inhibitor
    TGFβRI-IN-5 (Compound 4b) is a potent inhibitor of TGFβRI with an IC50 of 0.08 μM. TGFβRI-IN-5 displays amazing anticancer activity 5–7 times that of reference agent against all the tested cell lines. TGFβRI-IN-5 enhances apoptosis and arrested G2/M phase of cell cycle.
    TGFβRI-IN-5
  • HY-151954
    TGFβ1-IN-2
    		Inhibitor
    TGFβ1-IN-2 is a diarylacylhydrazones derivative that effectively suppresses the activation and proliferation of fibroblasts. TGFβ1-IN-2 can be used for idiopathic pulmonary fibrosis (IPF) research.
    TGFβ1-IN-2
  • HY-151955
    TGFβ1-IN-3
    		Inhibitor
    TGFβ1-IN-3 is a diarylacylhydrazones derivative that effectively suppresses the activation and proliferation of fibroblasts. TGFβ1-IN-3 can be used for idiopathic pulmonary fibrosis (IPF) research.
    TGFβ1-IN-3
  • HY-142949
    ALK5-IN-7
    		Inhibitor
    ALK5-IN-7 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-7 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 4).
    ALK5-IN-7
  • HY-W028145
    TGF-βRI inhibitor 2
    		Inhibitor
    TGF-βRI inhibitor 2 (compound 13) is a TGF-βRI inhibitor. TGF-βRI inhibitor 2 can be used in cancer research.
    TGF-βRI inhibitor 2
  • HY-122179
    NUCC-555
    		Antagonist
    NUCC-555 is an activin antagonist. NUCC-555 interacts with Trp25, Trp28, Phe55, Tyr93, Lys103, and Asn107 in the Activin A binding pocket. NUCC-555 blocks Activin A-mediated hepatic stellate cells (HSCs) activation. NUCC-555 promotes liver regeneration and halts fibrosis progression in chronic liver disease models. NUCC-555 inhibits Activin A-mediated ovarian cell proliferation. NUCC-555 decreases FSH levels in ovariectomized mice.
    NUCC-555
  • HY-161400
    TGFβRII-IN-2
    		Inhibitor
    TGFβRII-IN-2 (Compound 3n) is an inhibitor for transforming growth factor-β type II receptor (TGFβRII) with IC50 of 2.4 μM, which blocks endothelial-to-mesenchymal transition and cell migration in different cancer cell lines without perturbing the microtubule network.
    TGFβRII-IN-2
  • HY-151270
    ALK5-IN-25
    		Inhibitor
    ALK5-IN-25 (compound EX-02) is a potent ALK-5 inhibitor with an IC50 ≤10 nM.ALK5-IN-25 also inhibits ALK-2 (selectivity ALK2/ALK5≤10). ALK5-IN-25 can be used for the research of cancer.
    ALK5-IN-25
  • HY-155705
    BMP agonist 1
    		Agonist
    BMP agonist 1 (compound 2 b) is a small-molecule agonist of bone morphogenic protein (BMP). BMP induces C2C12 cell differentiation with BMP and highly depends on active BMP signaling. BMP agonist 1 inhibits GSK3β, increases β-catenin signaling and synergistically regulates Id2and Id3 expression. BMP agonist 1 is used in diseases and defects of the skeleton research.
    BMP agonist 1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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