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-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-116428
    L-744832
    		Modulator
    L-744832 is a farnesyl transferase inhibitor. L-744832 effectively inhibits the farnesylation of H-Ras and N-Ras, but has little effect on K-Ras treatment. L-744832 not only directly targets the oncogenic pathway by inhibiting Ras farnesylation, but also enhances radiosensitivity by restoring TGF-β signaling through epigenetic reprogramming. L-744832 can induce cell cycle arrest and apoptosis. L-744832 can be used in combination therapy studies for Ras-driven tumors such as pancreatic cancer.
    L-744832
  • 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-W1142093
    ActRIIB-IN-4
    ActRIIB-IN-4 (Compound 10) is an ActRIIB inhibitor with an IC50 of 4.0 nM. ActRIIB-IN-4 enhances muscle grip strength in tumor cachexia mice.
    ActRIIB-IN-4
  • 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-P991855
    RKER-216
    		Inhibitor
    RKER-216 is a human monoclonal IgG antibody inhibitor targeting ALK2 with a KD of 58.7 pM. RKER-216 reduces hepcidin transcription in Hep3B.RKER-216 competes with BMP ligands for binding to the extracellular domain of ALK2, thereby inhibiting BMP-SMAD signal. RKER-216 mobilizes tissue iron effectively in inflammatory conditions. RKER-216 improves microcytic anemia in a dose-dependent manner by inhibiting SMAD signaling to reduce hepcidin and promote iron absorption and utilization in vivo. RKER-216 can be used for research on anemia of inflammation.
    RKER-216
  • 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-183005
    ActRIIB-IN-1
    ActRIIB-IN-1, 7-azaindole compound is an orally active activin type II receptor B (ActRIIB) inhibitor with an IC50 of 1.8 nM. ActRIIB-IN-1 can alleviate weight loss, muscle atrophy and decreased muscle strength caused by tumor cachexia, as well as improve appetite. ActRIIB-IN-1 can be used for the research of cancer cachexia.
    ActRIIB-IN-1
  • HY-E70866
    TGFβR1 Recombinant Human Active Protein Kinase
    TGFβR1 plays an important role in TGF-β signaling transduction and serves as a tumor suppressor. TGFβR1 Recombinant Human Active Protein Kinase is a recombinant TGFβR1 protein that can be used to study TGFβR1-related functions.
    TGFβR1 Recombinant Human Active Protein Kinase
  • HY-183504
    ActRIIB-IN-3
    		Inhibitor
    ActRIIB-IN-3 is a ActRIIB inhibitor. ActRIIB-IN-3 inhibits the ActRIIB protein in the MSTN pathway and induces the reversal of skeletal muscle atrophy associated with cancer cachexia. ActRIIB-IN-3 is applicable for the research of cancer cachexia.
    ActRIIB-IN-3
  • 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
  • HY-W1142089
    ActRIIB-IN-2
    		Inhibitor
    ActRIIB-IN-2 is an ActRIIB inhibitor with an IC50 of 1.1 nM. ActRIIB-IN-2 can be used for the research of cancer cachexia.
    ActRIIB-IN-2
  • 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-N16527
    7-O-Galloyl-D-sedoheptulose
    		Inhibitor
    7-O-Galloyl-D-sedoheptulose is an orally effective polyphenolic compound. 7-O-Galloyl-D-sedoheptulose lowers the serum levels of glucose, leptin, insulin, C-peptide, resistin, TNF-α, IL-6, and increases the serum level of adiponectin. 7-O-Galloyl-D-sedoheptulose significantly reduces the levels of ROS and lipid peroxidation products (TBARS) by down-regulating the protein expression of NADPH oxidase subunit Nox-4 and p22phox. 7-O-Galloyl-D-sedoheptulose down-regulates NF-κB and related pro-inflammatory factors (COX-2, iNOS), inhibits the phosphorylation of JNK and the activity of its downstream AP-1. 7-O-Galloyl-D-sedoheptulose reduces the expression of TGF-β1 and fibronectin, indicating its potential in anti-tissue fibrosis. 7-O-Galloyl-D-sedoheptulose can be used for the study of type 2 diabetes and its hepatic and pancreatic complications.
    7-O-Galloyl-D-sedoheptulose
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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