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-12273G
    DMH-1 (GMP)
    		Inhibitor
    DMH-1 (GMP) is a GMP-grade version of DMH-1 (HY-12273). Small molecules of GMP grade can be used as adjuvant reagents in cell therapy. DMH-1 (GMP) promotes cardiac differentiation in mouse embryonic stem cells. DMH-1 (GMP) promotes neurogenesis of hiPSCs. DMH-1 is a potent and selective BMP inhibitor.
    DMH-1 (GMP)
  • HY-13012R
    RepSox (Standard)
    		Inhibitor
    RepSox (Standard) is the analytical standard of RepSox. This product is intended for research and analytical applications. RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes.
    RepSox (Standard)
  • HY-171247
    CDD-1281
    		Inhibitor
    CDD-1281 is a highly potent and selective BMPR2 kinase inhibitor with an IC50 of 1.2 nM. CDD-1281 can effectively inhibit BMP-mediated gene expression.
    CDD-1281
  • HY-12075R
    LY2109761 (Standard)
    		Inhibitor
    LY2109761 (Standard) is the analytical standard of LY2109761. This product is intended for research and analytical applications. LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.
    LY2109761 (Standard)
  • 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-162902
    ALK5-IN-82
    		Inhibitor
    ALK5-IN-82 is a potent and selective inhibitor against activin receptor-like kinase 5 (ALK5) with an IC50 value of 9.1 nM. ALK5-IN-82 inhibits the protein expression of α-smooth muscle actin (α-SMA), collagen I and tissue inhibitor of metalloproteinase 1 (TIMP-1)/matrix metalloproteinase 13 (MMP-13) in transforming growth factor-β-induced human umbilical vein endothelial cells. ALK5-IN-82 is promising for research of cardiac fibrosis.
    ALK5-IN-82
  • HY-W928653
    L-Seryl-L-leucyl-L-leucyl-L-lysine
    		Control
    L-Seryl-L-leucyl-L-leucyl-L-lysine (SLLK) is the control peptide for LSKL (HY-P0299).
    L-Seryl-L-leucyl-L-leucyl-L-lysine
  • HY-103388
    NCX 466
    		Inhibitor
    NCX 466 is an orally active COX-1 and COX-2 inhibitor that exhibits anti-inflammatory and analgesic effects. Additionally, NCX 466 acts as a NO donor, exerting anti-inflammatory and antioxidant effects by improving microcirculation. NCX 466 significantly reduces the levels of transforming growth factor-β (TGF-β) and oxidative stress markers (such as thiobarbituric acid reactive substances (TBARS) and 8-hydroxy-2'-deoxyguanosine (8-OHdG)), and it decreases leukocyte recruitment during inflammation by reducing myeloperoxidase (MPO) activity, thereby preventing bleomycin (HY-108345)-induced pulmonary fibrosis in mice.
    NCX 466
  • HY-12071BR
    LDN-193189 dihydrochloride (Standard)
    		Inhibitor
    LDN-193189 (dihydrochloride) (Standard) is the analytical standard of LDN-193189 (dihydrochloride). This product is intended for research and analytical applications. LDN-193189 (dihydrochloride) is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.
    LDN-193189 dihydrochloride (Standard)
  • HY-13227R
    SD-208 (Standard)
    		Inhibitor
    SD-208 (Standard) is the analytical standard of SD-208. This product is intended for research and analytical applications. SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.
    SD-208 (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-W684904
    LY550410
    		Inhibitor
    LY550410 is a small-molecule ATP-competitive inhibitor against type I TGF-β receptor kinase, which contains heteroaryl rings for potent binding to the kinase-domain active site. LY550410 modulates TGF-β signalling, thereby regulates gene expression and ultimately cell growth. LY550410 is promising for research of cancers.
    LY550410
  • HY-123409
    Nicousamide
    		Inhibitor
    Nicousamide is a potent inhibitor of TGF-β RII phosphorylation. Nicousamide can be used to study renal fibrosis in animal models of diabetic nephropathy.
    Nicousamide
  • 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-18758R
    IN-1130 (Standard)
    		Inhibitor
    IN-1130 (Standard) is the analytical standard of IN-1130. This product is intended for research and analytical applications. IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis.
    IN-1130 (Standard)
  • HY-13521AR
    SB-505124 hydrochloride (Standard)
    		Inhibitor
    SB-505124 (hydrochloride) (Standard) is the analytical standard of SB-505124 (hydrochloride). This product is intended for research and analytical applications. SB-505124 hydrochloride is a selective inhibitor of TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
    SB-505124 hydrochloride (Standard)
  • HY-13521R
    SB-505124 (Standard)
    		Inhibitor
    SB-505124 (Standard) is the analytical standard of SB-505124. This product is intended for research and analytical applications. SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
    SB-505124 (Standard)
  • HY-12071AR
    LDN193189 Tetrahydrochloride (Standard)
    		Inhibitor
    LDN193189 (Tetrahydrochloride) (Standard) is the analytical standard of LDN193189 (Tetrahydrochloride). This product is intended for research and analytical applications. LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM).
    LDN193189 Tetrahydrochloride (Standard)
  • HY-13418R
    Dorsomorphin dihydrochloride (Standard)
    		Inhibitor
    Dorsomorphin (dihydrochloride) (Standard) is the analytical standard of Dorsomorphin (dihydrochloride). This product is intended for research and analytical applications. Dorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).
    Dorsomorphin dihydrochloride (Standard)
  • HY-P0301
    SLLK, Control Peptide for TSP1 Inhibitor
    		Control
    SLLK, Control Peptide for TSP1 Inhibitor is a control peptide for LSKL (leucine-serine-lysine-leucine).
    SLLK, Control Peptide for TSP1 Inhibitor
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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