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-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-P990022
    Prafnosbart
    		Inhibitor
    Prafnosbart (DS-6016A) is an IgG1-kappa, anti-ACVR1 (activin A receptor type 1, ACVRLK2, ALK2, ACVR1A, SKR1) humanized monoclonal antibody. Prafnosbart can be used for bone metabolism disorders research.
    Prafnosbart
  • HY-10432R
    A 83-01 (Standard)
    		Inhibitor
    A 83-01 (Standard) is the analytical standard of A 83-01 (HY-10432). This product is intended for research and analytical applications. A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
    A 83-01 (Standard)
  • 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-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-118528
    TP0427736
    		Inhibitor
    TP0427736 is a selective inhibitor of ALK5 with an IC50 of 2.72 nM. TP0427736 inhibits Smad2/3 phosphorylation in A549 cells. TP0427736 decreases the growth inhibition of human outer root sheath cells.
    TP0427736
  • HY-Z8643
    HCTZ-CH2-HCTZ
    		Control
    HCTZ-CH2-HCTZ is an isomer of HCTZ (HY-B0252). Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway.
    HCTZ-CH2-HCTZ
  • HY-137063
    (+)-ITD-1
    		Degrader
    (+)-ITD-1 is an inhibitor for TGF-β, that inhibits the TGF-β2 with an IC50 of 0.46 μM. (+)-ITD-1 promotes the degradation of TGF-b type II receptor (TGFBR2) and the differentiation of cardiomyocyte, and inhibits the mesoderm formation in the early differentiation stage of mouse embryonic stem cells (mESCs).
    (+)-ITD-1
  • 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-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-160215A
    TGF-βRI inhibitor 1 methylbenzenesulfonate
    		Inhibitor
    TGF-βRI inhibitor 1 (compoimd i) methylbenzenesulfonate is a TGF-βRI inhibitor. TGF-βRI inhibitor 1 methylbenzenesulfonate can be used for cancer research.
    TGF-βRI inhibitor 1 methylbenzenesulfonate
  • 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.
    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-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-160215
    TGF-βRI inhibitor 1
    		Inhibitor
    TGF-βRI inhibitor 1 (compoimd i) is a TGF-βRI inhibitor. TGF-βRI inhibitor 1 can be used for cancer research.
    TGF-βRI inhibitor 1
  • 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-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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