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-155705
    BMP agonist 1
    		Agonist
    BMP agonist 1 (compound 2 b) is a small-molecule agonist of bone morphogenic protein (BMP). BMP induces C2C12 cell differentiation with BMP and highly depends on active BMP signaling. BMP agonist 1 inhibits GSK3β, increases β-catenin signaling and synergistically regulates Id2and Id3 expression. BMP agonist 1 is used in diseases and defects of the skeleton research.
    BMP agonist 1
  • HY-154970
    BMPR2-IN-1
    		Inhibitor
    BMPR2-IN-1 (Compound 8a) is a BMPR2 inhibitor with an IC50 of 506 nM and a KD of 83.5 nM. BMPR2-IN-1 can be used for research of pulmonary arterial hypertension, Alzheimer’s disease and cancer.
    BMPR2-IN-1
  • HY-118810
    BIO-013077-01
    		Inhibitor 99.63%
    BIO-013077-01 is a pyrazole TGF-β inhibitor.
    BIO-013077-01
  • HY-163121
    PST3.1a
    PST3.1a is an orally active and brain-penetrant N-acetylglucosamine glycosyltransferase (MGAT5) inhibitor with a human IC50 of 2 µM. PST3.1a inhibits TGFβR and FAK signaling pathway activity. PST3.1a alters β1,6-GlcNAc N-glycans and microtubule/microfilament integrity, increases OLIG2 expression, and inhibits proliferation, migration, invasiveness, and clonogenic capacities of glioblastoma initiating cells. PST3.1a reduces invasive and proliferative capacity of glioblastoma initiating cells in orthotopic graft models, increases overall survival of orthotopic graft model mice. PST3.1a blunts MGAT5 overexpression, decreases renal fibrosis via collagen 1, collagen 4, and galectin 3 downregulation in a rat chronic kidney disease model. PST3.1a can be used for the research of glioblastoma multiforme and chronic kidney disease.
    PST3.1a
  • HY-W028145
    TGF-βRI inhibitor 2
    		Inhibitor 98.32%
    TGF-βRI inhibitor 2 (compound 13) is a TGF-βRI inhibitor. TGF-βRI inhibitor 2 can be used in cancer research.
    TGF-βRI inhibitor 2
  • HY-161398
    TGFβRII-IN-3
    		Degrader 99.51%
    TGFβRII-IN-3 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) (IC50 = 4.1 μM). TGFβRII-IN-3 inhibits TGFβ signaling by promoting the proteolytic degradation of TGFβ RII. TGFβRII-IN-3 can block endothelial-to-mesenchymal transition and cell migration. TGFβRII-IN-3 can be used in cancer research.
    TGFβRII-IN-3
  • HY-173149
    CDD-2789
    		Inhibitor
    CDD-2789 is a potent and selective ALK2 inhibitor with an IC50 0.54 μM and a Kd of 2.1 nM, respectively. CDD-2789 exhibits >120-fold selectivity over ALK3/5/6. CDD-2789 reduces activin A- and BMP2-induced SMAD1/5 phosphorylation in fibroblasts. CDD-2789 can be used for ALK2-related cancer research.
    CDD-2789
  • HY-19628A
    OD36 hydrochloride
    		Inhibitor
    OD36hydrochloride is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 hydrochloride is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 hydrochloride shows ALK2-directed activity with KDs of 37 nM.
    OD36 hydrochloride
  • 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-P99841
    Dalutrafusp alfa
    		Inhibitor
    Dalutrafusp alfa (AGEN-1423; GS-1423) is a specific bifunctional antibody against CD73 and TGF-β, which is involved in the immunosuppressive pathway.
    Dalutrafusp alfa
  • 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-B1829
    Dexamethasone phosphate
    		Inhibitor 98.89%
    Dexamethasone phosphate (Dexamethasone 21-phosphate) is a prodrug form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone phosphate is prepared by introducing a phosphate ester group to the hydroxyl group at position 21 of the Dexamethasone molecule. Dexamethasone phosphate inhibits LPS (HY-D1056)-induced degradation of IRAK-1 and IRAK-4, and blocks LPS-induced activation of TRAF6, p-TAK1 and p-JNK. Dexamethasone phosphate inhibits the secretion of RANTES, TGF-β1 and NO, promotes the production of MIP-1α and IL-10, and blocks microglial migration. Dexamethasone phosphate is almost completely converted to Dexamethasone in rat blood, and supports transdermal delivery via iontophoresis. Dexamethasone phosphate can be used in research related to steroid-dependent ulcerative colitis, chemotherapy-induced vomiting, allergic asthma and acute colitis (inflammatory bowel disease).
    Dexamethasone phosphate
  • HY-13226R
    Galunisertib (Standard)
    		Inhibitor
    Galunisertib (Standard) is the analytical standard of Galunisertib. This product is intended for research and analytical applications. Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
    Galunisertib (Standard)
  • HY-P990454
    Anti-INHBB/Activin B Antibody
    The Anti-INHBB/Activin B Antibody is a human antibody expressed in CHO, targeting INHBB/Activin B. The Anti-INHBB/Activin B Antibody has a huIgG1 type heavy chain and a huκ type light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for the Anti-INHBB/Activin B Antibody can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-INHBB/Activin B Antibody
  • 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-162404
    (14S,15R)-14-Deoxyoxacyclododecindione
    (14S,15R)-14-Deoxyoxacyclododecindione (Compound 3) acts as an inhibitor of TGF-β-dependent Smad2/3 and IL-4-dependent STAT6, with IC50 values of 90 nM and 20 nM, respectively. (14S,15R)-14-deoxyoxacyclododecindione is a potent IL-4 inhibitor with an IC50
    value of 20 nM. (14S,15R)-14-Deoxyoxacyclododecindione is applicable to the research of chronic inflammation and fibrotic diseases.
    (14S,15R)-14-Deoxyoxacyclododecindione
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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