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

TGF-β Receptor

Transforming growth factor beta receptors

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-145855
    J-1063
    Inhibitor
    J-1063 is a potent, selective and orally active ALK5 inhibitor with an IC50 of 0.039 µM. J-1063 shows anti-fibrotic effect by the inhibition of inflammatory infiltration, collagen deposition, and hepatocytes necrosis. J-1063 has the potential for the research of liver fibrosis.
    J-1063
  • HY-N17821
    Butrin
    Inhibitor
    Butrin is a compound found in Butea monosperma flowers. Butrin reduces expression of SIRT1, AURKB, cyclin D1, pAKT, GSK-3β, β-catenin, and TGF-3β expression, enhances apoptosis and ROS production in cancer cells. Butrin downregulates Wnt and NF-κB signaling, mitigates oxidative stress, reduces proinflammatory cytokine (TNF-α, IL-6 and IL-8) production and suppresses neuroinflammation. Butrin inhibits IKK enzyme activity. Butrin can be used for the researches of colorectal cancer, Alzheimer’s disease, and rheumatoid arthritis.
    Butrin
  • HY-P11227
    Compound 19A8.8
    Inhibitor
    Compound 19A8.8 is a cyclic peptide derived from a CD36 protein fragment. Compound 19A8.8 inhibits the TGF-β/Smad3 signaling pathway by suppressing the interaction between TSP1 and CD36. Compound 19A8.8 has no obvious cytotoxicity. Compound 19A8.8 can be used for research on colon injury and fibrosis.
    Compound 19A8.8
  • HY-139636
    MCA17-1
    Inhibitor
    MCA17-1 shows stronger bioactivity than the positive control obeticholic acid (OCA) against liver fibrosis.
    MCA17-1
  • HY-151275
    ALK5-IN-28
    Inhibitor
    ALK5-IN-28 (Compound Ex-05) is a selective ALK-5 inhibitor (IC50 ≤ 10 nM) that inhibits TGF-β-induced SMAD signaling. ALK5-IN-28 has the potential to inhibit tumor growth in vivo. ALK5-IN-28 can be used in the research of proliferative diseases such as cancer.
    ALK5-IN-28
  • HY-RS14446
    TGFBR1 Rat Pre-designed siRNA Set A
    Inhibitor

    TGFBR1 Rat Pre-designed siRNA Set A contains three designed siRNAs for TGFBR1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    TGFBR1 Rat Pre-designed siRNA Set A
  • HY-151282
    ALK5-IN-32
    Inhibitor
    ALK5-IN-32 (compound EX-09) is a selective ALK-5 inhibitor (10 nM<IC50<100 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-32 has the potential to inhibit growth of tumour in vivo. ALK5-IN-32 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis.
    ALK5-IN-32
  • HY-182612
    SRI-35241
    Antagonist
    SRI-35241 is a thrombospondin TSP-1 inhibitor with a pIC50 of 8.12 nM against human targets. SRI-35241 inhibits the binding of TSP-1 to latent transforming growth factor-β-associated peptide (LAP) and blocks the activation of TGF-β. SRI-35241 shows a certain time-dependent property, with a plasma half-life of 1.8 h after intravenous administration. SRI-35241 can be used for the research of multiple myeloma and fibrotic diseases.
    SRI-35241
  • HY-P991879
    Anti-BMP-4 Antibody
    Anti-BMP-4 Antibody is an antibody against human BMP-4. Recommend Isotype Controls:?Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-BMP-4 Antibody
  • HY-N17639
    Regiafuran C
    Inhibitor
    Regiafuran C is a compound with both TGF-βRI inhibitory and anti-fibrotic activities. Regiafuran C effectively inhibits renal fibrosis by binding to TGF-βRI and interfering with the TGF-β/Smad and Wnt/β-catenin signaling pathways. Regiafuran C also exhibits free radical scavenging activity, but shows no anti-inflammatory activity in PGE2 competitive enzyme immunoassays. The ability of Regiafuran C to specifically block the Smad3-TGF-βRII interaction and inhibit fibrotic processes allows its use in renal fibrosis research.
    Regiafuran C
  • HY-161377
    M4K2306
    Inhibitor
    M4K2306 is a selective inhibitor for activin receptor-like kinase-2 (ALK2) with an IC50 of 7 nM. M4K2306 is blood brain permeable with a brain to plasma ratio of 75.6.
    M4K2306
  • HY-170227
    Autotaxin-IN-7
    Inhibitor
    Autotaxin-IN-7 (45), a pyridine-2-carboxylic derivative, demonstrates subnanomolar ATX inhibition (IC50 = 0.086 nM), with a favorable heart safety profile (hERG > 30 μM) and minimal fibroblast toxicity. Autotaxin-IN-7 (45) suppresses the TGF-β/Smad signaling pathway, downregulating α-smooth muscle actin (α-SMA) and extracellular matrix components (ECM). Autotaxin-IN-7 (45) is used in the research for pulmonary fibrosis.
    Autotaxin-IN-7
  • HY-176941
    ALK2-IN-6
    Inhibitor
    ALK2-IN-6 (Compound 14a) is a selective ALK2 inhibitor, with an IC50 of 9 nM. ALK2-IN-6 can be used in the research of diffuse intrinsic pontine glioma.
    ALK2-IN-6
  • HY-161925
    sTGFBR3 antagonist 1
    Antagonist
    sTGFBR3 antagonist 1 (Compound p24) is an antagonist for soluble transforming growth factor beta receptor 3 (sTGFBR3), thus activates TGF-β signaling pathway, and inhibits IκBα/NF-κB signaling pathway. sTGFBR3 antagonist 1 inhibits NO-release in LPS (HY-D1056) -induced BV2 cells with an IC50 of 0.52 μM. sTGFBR3 antagonist 1 exhibits anti-inflammatory and neuroprotective activities with blood brain barrier (BBB) permeability. sTGFBR3 antagonist 1 can be used in Alzheimer’s Disease research.
    sTGFBR3 antagonist 1
  • HY-E70867
    TGFβR2 Recombinant Human Active Protein Kinase
    TGF-β is a pleiotropic multifunctional cytokine that regulates many cellular processes, such as cell growth, differentiation, apoptosis and cellular homeostasis. Before exerting the biological effects within cells, TGF-β first requires extracellular activation, namely binds to its type II receptor (TGFβR2) and promotes the phosphorylation. TGFβR1 plays an important role in TGF-β signaling transduction and serves as a tumor suppressor. TGFβR2 Recombinant Human Active Protein Kinase is a recombinant TGFβR2 protein that can be used to study TGFβR2-related functions.
    TGFβR2 Recombinant Human Active Protein Kinase
  • HY-142967
    TGFβ-IN-1
    TGFβ-IN-1 is an antitumor growth and metastasis agent through inhibiting the transforming growth factor‑β signaling pathway.
    TGFβ-IN-1
  • HY-178850
    TJN-331
    Inhibitor
    TJN-331 is a potent and orally active TGF-β1 Inhibitor. TJN-331 ameliorates anti-glomerular basement membrane (GBM) nephritis in rats by inhibitng TGF-β1 production, thereby reducing extracapillary proliferation in glomeruli. TJN-331 inhibits mesangial expansion in experimental IgA nephropathy in ddY mice. TJN-331 can be used for the research of nephritis and IgA nephropathy.
    TJN-331
  • HY-142950
    ALK5-IN-6
    Inhibitor
    ALK5-IN-6 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-6 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 1).
    ALK5-IN-6
  • HY-146780
    TGFβRI-IN-4
    Inhibitor
    TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC50s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model.
    TGFβRI-IN-4
  • HY-P992188
    Anti-ALK7 Antibody
    Anti-ALK7 Antibody is a monoclonal antibody that targets ALK7. It can be used in ELISA, FACS, and functional assays. For isotype controls of Anti-ALK7 Antibody, please refer to Human IgG1 (L234A/L235A) kappa, Isotype Control (HY-P991207).
    Anti-ALK7 Antibody
Cat. No. Product Name / Synonyms Species Source
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