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-10432A
    A 83-01 sodium
    		Inhibitor 98.03%
    A 83-01 sodium is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and 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 sodium
  • HY-13521
    SB-505124
    		Inhibitor 99.73%
    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
  • HY-P99590
    Sotatercept
    		99.94%
    Sotatercept (ACE-011) is a soluble activin receptor 2A (ACVR2A) type IgG Fc fusion protein. Sotatercept combines activin and growth differentiation factor to try to restore the balance between growth promotion and growth inhibition signal pathways. Sotatercept has potential application in pulmonary arterial hypertension, anemia, bone loss, erythropoiesis, multiple myeloma (MM) osteolytic lesions.
    Sotatercept
  • HY-13462
    LY-364947
    		Inhibitor 99.23%
    LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II.
    LY-364947
  • HY-10431G
    SB-431542 (GMP)
    		Inhibitor
    SB-431542 (GMP) is SB-431542 (HY-10431) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SB-431542 is a TGF-β receptor kinase inhibitor (TRKI) in SMAD signaling.
    SB-431542 (GMP)
  • HY-100113
    Buloxibutid
    		Inhibitor 98.94%
    Buloxibutid (AT2 receptor agonist C21) 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
  • HY-16712
    LDN-214117
    		Inhibitor 99.54%
    LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) .
    LDN-214117
  • HY-A0183
    Phosphatidylserine
    		Inducer ≥98.0%
    Phosphatidylserine (Phospholipids) is a well-conserved anti-inflammatory and immunosuppressive signal. Phosphatidylserine is involved in membrane translocation and the activation of protein kinase C, participating in Akt signaling through its interaction with PIP3. The local exposure of Phosphatidylserine can interact with complement and other proteins, promoting microglial phagocytosis during critical periods of synaptic refinement. Phosphatidylserine can promote blood coagulation in the extracellular environment and acts as a "eat me" signal to clear out apoptotic cells. Phosphatidylserine can suppress inflammation in tissues by inducing TGF-β secretion and inhibiting immune responses.
    Phosphatidylserine
  • HY-12278
    K02288
    		Inhibitor 99.95%
    K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC50s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC50s of of 5-34 nM.
    K02288
  • HY-13227
    SD-208
    		Inhibitor 99.87%
    SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.
    SD-208
  • HY-P99632
    Garetosmab
    		Inhibitor 99.57%
    Garetosmab (REGN 2477) is a fully human IgG4 monoclonal antibody that specifically inhibits activin A. Garetosmab can be used for fibrodysplasia ossificans progressiva (FOP) research.
    Garetosmab
  • HY-P99590A
    Sotatercept (mIgG2a)
    		Inhibitor 99.93%
    Sotatercept (mIgG2a) (RAP-011), the murine homolog of Sotatercept (ACE-011) (HY-P99590), is a soluble activin receptor type IIA (ActRIIA) ligand trap. Sotatercept (mIgG2a) inhibits the binding of activin A and other members of the TGF-β superfamily (such as Activin A/B, GDF11 and BMP9/10) to their receptors by combining and neutralizing them, thereby regulating cell proliferation and differentiation. Sotatercept (mIgG2a) mainly inhibits the SMAD2/3 signaling pathway, and can be used in various diseases such as chronic kidney disease. Sotatercept (mIgG2a) reduces the expression of erythropoietic hepcidin (ERFE), regulates iron metabolism, and promotes red blood cell production. Sotatercept (mIgG2a) has a dual effect of promoting bone formation (anabolic) and inhibiting bone resorption (catabolic).
    Sotatercept (mIgG2a)
  • HY-11103
    Sitaxsentan sodium
    		Activator 98.83%
    Sitaxsentan sodium (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 sodium exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan sodium is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan sodium can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension.
    Sitaxsentan sodium
  • HY-10326
    GW788388
    		Inhibitor 99.92%
    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
  • HY-13012G
    RepSox (GMP)
    		Inhibitor
    RepSox (E-616452) (GMP) is a RepSox (HY-13012) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RepSox is a potent and selective TGF-β-RI/ALK5 inhibitor.
    RepSox (GMP)
  • HY-157442
    GLPG3312
    		Antagonist 98.63%
    GLPG3312 (Compound 28) is an orally active SIK inhibitor with IC50 values of 2.0 nM, 0.7 nM and 0.6 nM for SIK1, SIK2 and SIK3, respectively. GLPG3312 exhibits anti-inflammatory and immunomodulatory activity in vitro on human primary myeloid cells and in vivo in mouse models. GLPG3312 has good oral bioavailability and can be used for research on inflammatory and immune diseases.
    GLPG3312
  • HY-P3970A
    KRFK TFA
    		Agonist 99.76%
    KRFK TFA, a peptide derived from TSP-1, can activate TGF-β. KRFK TFA promotes TGF-β-mediated signaling and its downstream role, independent of thrombospondin (TSP) receptors such as CD47 and CD36. KRFK TFA can be used for chronic ocular surface inflammatory disorders reseach.
    KRFK TFA
  • HY-12704
    ITD-1
    		Inhibitor 99.73%
    ITD-1 is the first selective TGFβ receptor inhibitor with an IC50 of 460 nM.
    ITD-1
  • HY-136244
    PF-06952229
    		Inhibitor 99.92%
    PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction.?PF-06952229 is a promising antineoplastic?agent for the study solid tumors, especifically metastatic breast cancer.
    PF-06952229
  • HY-15897
    LDN-212854
    		Inhibitor 99.62%
    LDN-212854 is a bone morphogenetic protein (BMP) inhibitor that potently inhibits ALK2 (IC50: 1.3 nM). LDN-212854 also inhibits ALK1 (IC50: 2.40 nM). LDN-212854 can be used in the research of fibrodysplasia ossificans progressive and cancers, such as hepatocellular carcinoma (HCC).
    LDN-212854
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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