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-148246
    MU1700
    		Inhibitor
    MU1700 is an orally active and potent ALK1/2 inhibitor with IC50s of 13 nM and 6 nM, respectively. MU1700 shows cell membrane permeability and high brain permeability.
    MU1700
  • HY-161398
    TGFβRII-IN-3
    		Degrader
    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-151273
    ALK5-IN-27
    		Inhibitor
    ALK5-IN-27 (Compound EX-04) is a potent ALK-5 inhibitor with an IC50 ≤10 nM. ALK5-IN-27 also inhibits ALK-2 (selectivity ALK2/ALK5 ≤10).
    ALK5-IN-27
  • 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-P99818
    Ramatercept
    		Antagonist
    Ramatercept (ACE-031) is a soluble ActRIIB receptor and can be used as a soluble activin receptor 2 (ACVR2) antagonist. Ramatercept inhibits the signal pathway of muscle growth inhibition and has potential application in muscle atrophy.
    Ramatercept
  • 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-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-155939
    M4K2163 dihydrochloride
    		Inhibitor
    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-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-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-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-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-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-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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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