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-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-177657A
    Pixofisiran sodium
    		Inhibitor
    Pixofisiran sodium is a siRNA in STP705. It targets to TGF‐β1. STP705 is composed of 2 siRNA oligonucleotides (Pixofisiran and Lixadesiran) that individually target TGF-β1 and COX-2 mRNA.
    Pixofisiran sodium
  • HY-121025
    BUR1
    		Inhibitor 99.65%
    BUR1 is a BMP upregulator (EC50: 98 nM) and activates BMPRII signalling. BUR1 induces BMP2 and PTGS2 expression. BUR1 reversed pulmonary arterial pressure in Monocrotaline (HY-N0750) induced rats.
    BUR1
  • HY-177657
    Pixofisiran
    		Inhibitor
    Pixofisiran is a siRNA in STP705. It targets to TGF‐β1. STP705 is composed of 2 siRNA oligonucleotides (Pixofisiran and Lixadesiran) that individually target TGF-β1 and COX-2 mRNA.
    Pixofisiran
  • HY-N4019
    Maohuoside A
    		98.94%
    Maohuoside A, a single compound isolated from the E. koreanum that potently promotes osteogenesis. Maohuoside A enhances the osteogenesis of bone marrow-derived mesenchymal stem cells via bone morphogenetic protein (BMP) and MAPK signaling pathways.
    Maohuoside A
  • HY-145855
    J-1063
    		Inhibitor
    J-1063 is a potent, selective and orally active ALK5 inhibitor with an IC50 of 0.039 µM. J-1063 shows anti-fibrotic effect by the inhibition of inflammatory infiltration, collagen deposition, and hepatocytes necrosis. J-1063 has the potential for the research of liver fibrosis.
    J-1063
  • HY-139636
    MCA17-1
    		Inhibitor
    MCA17-1 shows stronger bioactivity than the positive control obeticholic acid (OCA) against liver fibrosis.
    MCA17-1
  • HY-151275
    ALK5-IN-28
    		Inhibitor
    ALK5-IN-28 (compound Ex-05) is a selective ALK-5 inhibitor (IC50≤10 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-28 has the potential to inhibit growth of tumour in vivo. ALK5-IN-28 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis.
    ALK5-IN-28
  • HY-RS14446
    TGFBR1 Rat Pre-designed siRNA Set A
    		Inhibitor

    TGFBR1 Rat Pre-designed siRNA Set A contains three designed siRNAs for TGFBR1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    TGFBR1 Rat Pre-designed siRNA Set A
  • HY-151282
    ALK5-IN-32
    		Inhibitor
    ALK5-IN-32 (compound EX-09) is a selective ALK-5 inhibitor (10 nM<IC50<100 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-32 has the potential to inhibit growth of tumour in vivo. ALK5-IN-32 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis.
    ALK5-IN-32
  • HY-161377
    M4K2306
    		Inhibitor
    M4K2306 is a selective inhibitor for activin receptor-like kinase-2 (ALK2) with an IC50 of 7 nM. M4K2306 is blood brain permeable with a brain to plasma ratio of 75.6.
    M4K2306
  • HY-170227
    Autotaxin-IN-7
    		Inhibitor
    Autotaxin-IN-7 (45), a pyridine-2-carboxylic derivative, demonstrates subnanomolar ATX inhibition (IC50 = 0.086 nM), with a favorable heart safety profile (hERG > 30 μM) and minimal fibroblast toxicity. Autotaxin-IN-7 (45) suppresses the TGF-β/Smad signaling pathway, downregulating α-smooth muscle actin (α-SMA) and extracellular matrix components (ECM). Autotaxin-IN-7 (45) is used in the research for pulmonary fibrosis.
    Autotaxin-IN-7
  • 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-E70867
    TGFβR2 Recombinant Human Active Protein Kinase
    TGF-β is a pleiotropic multifunctional cytokine that regulates many cellular processes, such as cell growth, differentiation, apoptosis and cellular homeostasis. Before exerting the biological effects within cells, TGF-β first requires extracellular activation, namely binds to its type II receptor (TGFβR2) and promotes the phosphorylation. TGFβR1 plays an important role in TGF-β signaling transduction and serves as a tumor suppressor. TGFβR2 Recombinant Human Active Protein Kinase is a recombinant TGFβR2 protein that can be used to study TGFβR2-related functions.
    TGFβR2 Recombinant Human Active Protein Kinase
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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