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-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 GMP grade DMH-1 (HY-12273). DMH-1 (GMP) is a selective BMP inhibitor. DMH-1 (GMP) upregulates the expression of SOX1. DMH-1 (GMP) increases cardiomyocyte progenitor cells and promotes the differentiation of mouse embryonic stem cells into cardiomyocytes. DMH-1 (GMP) induces the differentiation of hiPSC-derived neural progenitor cells into β3-tubulin-positive neurons.
    DMH-1 (GMP)
  • HY-165339
    Lysyl-phenylalanyl-lysine
    Lysyl-phenylalanyl-lysine (Compound KFK) is a tripeptide and belongs to the peptide segments related to thrombospondin-1 (TSP-1) (HY-P0299). Lysyl-phenylalanyl-lysine can activate LAP-TGF-β1 and release active TGF-β1, thereby inhibiting abnormal expression of MMP. Lysyl-phenylalanyl-lysine can be used for research on skin aging-related diseases and poor wound healing.
    Lysyl-phenylalanyl-lysine
  • HY-76520
    Sitaxsentan
    		Activator
    Sitaxsentan (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension.
    Sitaxsentan
  • 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-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
    LDN193189 dihydrochloride (Standard)
    		Inhibitor
    LDN193189 (DM-3189) dihydrochloride (Standard) is the analytical standard of LDN193189 dihydrochloride (HY-12071B). This product is intended for research and analytical applications. LDN193189 (DM-3189) dihydrochloride is a potent selective BMP type I receptor (BMP I) inhibitor. LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.
    LDN193189 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-76520S
    Sitaxsentan-13C6
    		Activator
    Sitaxsentan-13C6 (IPI 1040-13C6) is 13C labeled Sitaxsentan (HY-76520). Sitaxsentan (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension.
    Sitaxsentan-<sup>13</sup>C<sub>6</sub>
  • HY-10327R
    GW-6604 (Standard)
    		Inhibitor
    GW-6604 (Standard) is the analytical standard of GW-6604 (HY-10327). This product is intended for research and analytical applications. GW-6604 is an ALK5 inhibitor with an IC50 value of 140 nM for inhibiting its autophosphorylation, and can be used in the study of liver fibrosis.
    GW-6604 (Standard)
  • HY-10326R
    GW788388 (Standard)
    		Inhibitor
    GW788388 (Standard) is the analytical standard of GW788388 (HY-10326). This product is intended for research and analytical applications. GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
    GW788388 (Standard)
  • 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-100113R
    Buloxibutid (Standard)
    		Inhibitor
    Buloxibutid (AT2 receptor agonist C21) (Standard) is the analytical standard of Buloxibutid (HY-100113). This product is intended for research and analytical applications. Buloxibutid is an orally active, selective angiotensin II type 2 receptor (AT2R) agonist, with a Ki value of 0.4 nM for porcine AT2R. Buloxibutid exerts effects such as vasodilation, anti-inflammation, anti-fibrosis (promoting the expression of collagenase MMP-13) and tissue repair mainly by activating the NO/cGMP pathway, inhibiting the pro-proliferative MAPK signaling, and suppressing the pro-fibrotic TGF-β/Smad pathway as well as the inflammatory NF-κB pathway. Buloxibutid can be used in research related to idiopathic pulmonary fibrosis, hypertension, and systemic sclerosis.
    Buloxibutid (Standard)
  • HY-103021R
    LY3200882 (Standard)
    		Inhibitor
    LY3200882 (Standard) is the analytical standard of LY3200882 (HY-103021). This product is intended for research and analytical applications. LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC50 of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent.
    LY3200882 (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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