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

TGF-β Receptor

Transforming growth factor beta receptors

TGF-β Receptor

Related Products

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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-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-137918
    TGF-βRI inhibitor 3
    		Inhibitor
    TGF-βRI inhibitor 3 (Compound 9ac) is a selective TGF-β inhibitor. TGF-βRI inhibitor 3 can effectively inhibit the TGF-β signaling pathway. TGF-βRI inhibitor 3 has IC50 values of 13 μM and 0.63 μM for c-Src kinase and ALK5 kinase, respectively.
    TGF-βRI inhibitor 3
  • HY-P990326
    Anti-ACVR2A Antibody (Ab-14E1)
    		Inhibitor
    Anti-ACVR2A Antibody (Ab-14E1) is a CHO-expressed human antibody that targets ACVR2A. Anti-ACVR2A Antibody (Ab-14E1) features an IgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for Anti-ACVR2A Antibody (Ab-14E1) can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-ACVR2A Antibody (Ab-14E1)
  • 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-168990
    Ontunisertib
    		Inhibitor
    Ontunisertib (Example 26) is an inhibitor of TGFβ receptor I/ALK5 (TGFβRI/ALK5), with IC50 values ranging from 100 to 500 nM for TGFβRI and an IC50 value of ≤100 nM for ALK5. Ontunisertib can be used in research on gastrointestinal diseases, as well as diseases and cancers related to fibrotic conditions in the skin and eyes.
    Ontunisertib
  • 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-108464
    Phenamil
    		Activator
    Phenamil is a compound that promotes bone repair and regulates stem cell differentiation. It can activate the bone morphogenetic protein signaling pathway to promote bone repair, but it also induces adipogenesis. A specific 3D scaffold strategy can improve its induced osteogenic differentiation and reduce adipogenesis.
    Phenamil
  • 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-P990454
    Anti-INHBB/Activin B Antibody
    The Anti-INHBB/Activin B Antibody is a human antibody expressed in CHO, targeting INHBB/Activin B. The Anti-INHBB/Activin B Antibody has a huIgG1 type heavy chain and a huκ type light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for the Anti-INHBB/Activin B Antibody can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-INHBB/Activin B Antibody
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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