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-155939
    M4K2163 dihydrochloride
    Inhibitor 98.30%
    M4K2163 dihydrochloride is a potent, selective, blood-brain barrier (BBB) permeable activin receptor-like kinase-2 (ALK2) inhibitor, with an IC50 of 19 nM. M4K2163 dihydrochloride can be used in the research of diffuse intrinsic pontine glioma (DIPG).
    M4K2163 dihydrochloride
  • HY-P99748
    Nadecnemab
    Inhibitor
    Nadecnemab is an IgG4κ antibody targeting to GFRA3, glial cell derived neurotrophic factor family receptor alpha 3. Nadecnemab can be used for research of osteoarthritis of the knee/pain.
    Nadecnemab
  • HY-143891
    Chromenone 1
    Activator 99.78%
    Chromenone 1 is a potent osteogenic bone morphogenetic protein (BMP) potentiator. Chromenone 1 exhibits a unique mode of action as it induces a pronounced, kinase-independent, negative TGFβ feedback that enhances nuclear BMP-Smad signaling outputs.
    Chromenone 1
  • HY-114192
    TGFβRI-IN-1
    Inhibitor
    TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively .
    TGFβRI-IN-1
  • HY-139858
    TGFβR-IN-1
    Inhibitor
    TGFβR-IN-1 is a long-acting tumor-activated proagent of a TGFβR inhibitor.
    TGFβR-IN-1
  • HY-P990974
    Bezeotermin alfa
    HY-P990974 is an BMP-6-targeting Fusion Protein.
    Bezeotermin alfa
  • HY-13226A
    Galunisertib monohydrate
    Inhibitor
    Galunisertib monohydrate is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
    Galunisertib monohydrate
  • HY-RS14445
    Tgfbr1 Mouse Pre-designed siRNA Set A
    Inhibitor

    Tgfbr1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Tgfbr1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Tgfbr1 Mouse Pre-designed siRNA Set A
  • HY-P3972
    H-ILE-ARG-VAL-VAL-MET-OH
    H-ILE-ARG-VAL-VAL-MET-OH is a pentapeptide from C7 with a domain that supports cell attachment. H-ILE-ARG-VAL-VAL-MET-OH is also the sequence fragment that binds to the thrombospondin-1 (TS1) receptor.
    H-ILE-ARG-VAL-VAL-MET-OH
  • HY-100167
    TAK-778
    Agonist
    TAK-778 is a derivative of ipriflavone and has been shown to induce bone growth in in vitro and in vivo models.
    TAK-778
  • HY-112864
    TGFβRI-IN-6
    Inhibitor
    TGFβRI-IN-6 (compound 22) is a potent TGFβRI inhibitor with an IC50 value of 0.55 nM. TGFβRI-IN-6 has the potential to enhance anti-tumor immunity.
    TGFβRI-IN-6
  • HY-151233
    ALK5-IN-10
    Inhibitor
    ALK5-IN-10 (Compound 5d) is a TGF-β type I receptor kinase ALK5 inhibitor, with IC50s of 0.007 and 1.98 μM for ALK5 and p38α, respectively. ALK5-IN-10 can be used for the research of cancer.
    ALK5-IN-10
  • HY-RS14444
    TGFBR1 Human Pre-designed siRNA Set A
    Inhibitor

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

    TGFBR1 Human Pre-designed siRNA Set A
  • HY-P2294
    pm26TGF-β1 peptide
    pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.
    pm26TGF-β1 peptide
  • 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-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-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-137918
    TGF-βRI inhibitor 3
    Inhibitor 99.16%
    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)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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