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-N0353R
    Curdione (Standard)
    Curdione (Standard) is the analytical standard of Curdione. This product is intended for research and analytical applications. Curdione ((+)-Curdione) is an orally active sesquiterpenoid. Curdione inhibits platelet aggregation. Curdione induces ferroptosis in colorectal cancer via m6A methylation mediated by METTL14 and YTHDF2. Curdione inhibits ferroptosis in Isoproterenol (HY-B0468)-induced myocardial infarction by regulating the Keap1/Trx1/GPX4 signaling pathway, suppressing oxidative stress (ROS) and apoptosis. Curdione ameliorates Doxorubicin (HY-15142)-induced cardiotoxicity by inhibiting oxidative stress (ROS) and activating the Nrf2/HO-1 pathway. Curdione ameliorates sepsis-induced lung injury by inhibiting platelet-mediated neutrophil extracellular trap formation. Curdione ameliorates Bleomycin (HY-17565A)-induced pulmonary fibrosis by inhibiting TGF-β-induced fibroblast-to-myofibroblast differentiation. Curdione exhibits neuroprotective effects against focal cerebral ischemia-reperfusion injury in rats. Curdione exerts antiproliferative effects against human uterine leiomyosarcoma by targeting IDO1. Curdione protects vascular endothelial cells and atherosclerosis by regulating DNMT1-mediated ERBB4 promoter methylation. Curdione inhibits inducible prostaglandin E2 production (IC50 = 1.1 μM) and cyclooxygenase 2 expression.
    Curdione (Standard)
  • HY-178191
    SGC stimulator 1
    		Inhibitor
    sGC stimulator 1 is a carbonyl sulfide (COS)/H2S-donor hybrid soluble guanylyl cyclase (sGC) stimulator (EC50 = 496 nM). sGC stimulator 1 exhibits a well-characterized H2S-releasing property. sGC stimulator 1 reduces fibrosis in TGF-β1-treated cardiac fibroblasts by increasing cGMP and H2S levels. sGC stimulator 1 can exert anti-fibrotic effects by activating sGC and increasing H2S. sGC stimulator 1 can be used for the study of heart failure (HF).
    SGC stimulator 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-P11354
    THR-123
    		Agonist
    THR-123 is an orally active ALK3 peptide agonist. THR-123 has a relatively weak binding to ALK2, but does not bind to ALK6. THR-123 suppresses inflammation, apoptosis and the epithelial-to-mesenchymal transition program and reverses established fibrosis in five mouse models of acute and chronic renal injury. THR-123 can be used for the study of kidney fibrosis.
    THR-123
  • HY-171878
    BI-4659
    		Inhibitor
    BI-4659 (Compound 47i) is a TGF-β type I receptor (TGF-βRI) (Alk5) inhibitor with an IC50 of 19  nM. BI-4659 also inhibits <PDGFRα> (IC50: 99 nM) and significantly blocks TGFβRI-mediated phosphorylation of Smad2/3 with low cross-reactivities within the human kinome. BI-4659 can be used for fibrotic diseases like idiopathic pulmonary fibrosis (IPF) and cancers research.
    BI-4659
  • HY-178477
    LIFR/GPBAR1 modulator 1
    		Inhibitor
    LIFR/GPBAR1 modulator 1 is an orally active, potent GPBAR1 agonist (EC50 = 0.2 μM) and LIFR inhibitor (IC50 = 7.9 μM). LIFR/GPBAR1 modulator 1 upregulates leukaemia inhibitory factor (LIF)-mediated mRNA expression of LIFR and GPBAR1 and significantly reduces the expression of pro-fibrosis markers (COL1A1, ASMA, and TGFβ), and reduces TIMP1 expression and increases MMP9 expression. LIFR/GPBAR1 modulator 1 can be used for the study of human fibrotic disorders.
    LIFR/GPBAR1 modulator 1
  • 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-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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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