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-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-175257
    Theophylline-platinum(IV) prodrug-1
    		Inhibitor
    Theophylline-platinum(IV) prodrug-1 is a PARP-1 inhibitor. Theophylline-platinum(IV) prodrug-1 enhances DNA damage, ROS production, mitochondrial dysfunction, apoptosis and S-phase arrest, along with reducing invasion and metastasis in cells. Theophylline-platinum(IV) prodrug-1 exhibits superior antitumor activity in the xenograft SKOV3-BRCA1-KD tumor model. Theophylline-platinum(IV) prodrug-1 can be used for the study of ovarian cancer.
    Theophylline-platinum(IV) prodrug-1
  • HY-160215A
    GFH018 methylbenzenesulfonate
    		Inhibitor
    GFH018 methylbenzenesulfonate is a TGF-βRI inhibitor. GFH018 methylbenzenesulfonate can be used for cancer research.
    GFH018 methylbenzenesulfonate
  • 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-P991158
    Rinvatercept
    Rinvatercept, a fusion protein, is a glycyl (1)-chimeric N-terminal (1-108)-peptide (2-109) combined from the sequences of the extracellular domains of the human ACVR2A/B, and is fused via a G3 peptide linker (110-112) to an immunoglobulin G1 (IgG1) Fc fragment. Rinvatercept can be used for research of neuromuscular disease.
    Rinvatercept
  • 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 98.47%
    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-P991383
    LY2382770
    		Inhibitor
    LY2382770 is a human monoclonal antibody (mAb) targeting TGFB1. LY2382770 can be used in dabetic nephropathies research.
    LY2382770
  • HY-172108
    TGFβRI-IN-7
    		Inhibitor
    TGFβRI-IN-7 (compound 16W) is a potent inhibitor of TGFβRI. TGFβRI-IN-7 inhibits SMAD2/3 phosphorylation and H22 cell viability with IC50 values of 12 and 65 nM, respectively. TGFβRI-IN-7 shows anti-tumor efficacy in a xenograft model of H22 cells, with TGI of 79.6 %.
    TGFβRI-IN-7
  • 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-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-171249
    CDD-1431
    		Inhibitor
    CDD-1431 is a low-nanomolar selective kinase inhibitors of BMPR2, with Kiapp value of 20.6 nM. CDD-1431 suppresses BRE-reporter activity, with an IC50 of 4.87 μM. BMP controls cellular processes across many tissue types, including the kidney, skeletal muscle, heart, and reproductive organs. BMP induces ectopic bone formation.
    CDD-1431
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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