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-P3972
    H-ILE-ARG-VAL-VAL-MET-OH
    H-ILE-ARG-VAL-VAL-MET-OH is a pentapeptide from C7 with a domain that supports cell attachment. H-ILE-ARG-VAL-VAL-MET-OH is also the sequence fragment that binds to the thrombospondin-1 (TS1) receptor.
    H-ILE-ARG-VAL-VAL-MET-OH
  • HY-100167
    TAK-778
    		Agonist
    TAK-778 is a derivative of ipriflavone and has been shown to induce bone growth in in vitro and in vivo models.
    TAK-778
  • HY-P992393
    JMT203
    JMT203 is a monoclonal antibody against GFRAL and a body weight gain inducer. JMT203 induces early-onset, sustained and progressive body weight gain in cancer cachexia. JMT203 can be used for research related to cancer cachexia.
    JMT203
  • HY-112864
    TGFβRI-IN-6
    		Inhibitor
    TGFβRI-IN-6 (compound 22) is a potent TGFβRI inhibitor with an IC50 value of 0.55 nM. TGFβRI-IN-6 has the potential to enhance anti-tumor immunity.
    TGFβRI-IN-6
  • HY-151233
    ALK5-IN-10
    		Inhibitor
    ALK5-IN-10 (Compound 5d) is a TGF-β type I receptor kinase ALK5 inhibitor, with IC50s of 0.007 and 1.98 μM for ALK5 and p38α, respectively. ALK5-IN-10 can be used for the research of cancer.
    ALK5-IN-10
  • HY-182611
    SRI-31277
    SRI-31277 is a thrombospondin 1 (TSP-1) inhibitor with a human target pIC50 of 8.28 nM and in vivo activity, and exhibits a very short plasma half-life with intravenous administration.SRI-31277 inhibits interaction between TSP-1 and the latency-associated peptide (LAP) of latent TGF-β, blocking TSP-1-mediated TGF-β activation.SRI-31277 can be used for the research of multiple myeloma and fibrotic conditions.
    SRI-31277
  • HY-RS14444
    TGFBR1 Human Pre-designed siRNA Set A
    		Inhibitor

    TGFBR1 Human Pre-designed siRNA Set A contains three designed siRNAs for TGFBR1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    TGFBR1 Human Pre-designed siRNA Set A
  • HY-P991254
    VPI-2690B
    		Inhibitor
    VPI-2690B is a human monoclonal antibody (mAb) targeting Integrin aVb3. VPI-2690B inhibits TGF-β signaling. VPI-2690B can be used in Diabetic nephropathies research.
    VPI-2690B
  • HY-13227G
    SD-208 (GMP)
    		Inhibitor
    SD-208 (GMP) is SD-208 (HY-13227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.
    SD-208 (GMP)
  • HY-P2294
    pm26TGF-β1 peptide
    pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.
    pm26TGF-β1 peptide
  • HY-N17383
    Ligusticum cycloprolactam
    		Inhibitor
    Ligusticum cycloprolactam is a potent, orally active, and CNS-penetrant TLR4/NF-κB inhibitor, exhibiting anti-inflammatory and neuroprotective activity. Ligusticum cycloprolactam reduces FPR1 expression, inhibits NLRP3 inflammasome, TLR4/NF-κB, hepatic MAPK and TGF-β signaling, and selectively activates hepatic FXR. Ligusticum cycloprolactam attenuates pro-inflammatory mediator production, enhances anti-inflammatory cytokine secretion, regulates renal uric acid transporters, and preserves intestinal microbiota composition. Ligusticum cycloprolactam can be used for the research of ischemic stroke, hyperuricemic nephropathy, neuroinflammation, and metabolic dysfunction-associated fatty liver disease.
    Ligusticum cycloprolactam
  • HY-15472A
    PRX-08066 maleate
    		Inhibitor
    PRX-08066 maleate is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki of 3.4 nM. PRX-08066 maleate inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 maleate inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 maleate inhibits pulmonary vascular remodeling. PRX-08066 maleate can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET).
    PRX-08066 maleate
  • HY-112877
    ALK-5-IN-1
    		Inhibitor
    ALK-5-IN-1 is an ALK-5 inhibitor. ALK-5-IN-1 can be used for the research of cancer, and conditions involving fibrosis.
    ALK-5-IN-1
  • HY-N0353R
    Curdione (Standard)
    Curdione (Standard) is the analytical standard of Curdione. This product is intended for research and analytical applications. Curdione ((+)-Curdione) is an orally active sesquiterpenoid. Curdione inhibits platelet aggregation. Curdione induces ferroptosis in colorectal cancer via m6A methylation mediated by METTL14 and YTHDF2. Curdione inhibits ferroptosis in Isoproterenol (HY-B0468)-induced myocardial infarction by regulating the Keap1/Trx1/GPX4 signaling pathway, suppressing oxidative stress (ROS) and apoptosis. Curdione ameliorates Doxorubicin (HY-15142)-induced cardiotoxicity by inhibiting oxidative stress (ROS) and activating the Nrf2/HO-1 pathway. Curdione ameliorates sepsis-induced lung injury by inhibiting platelet-mediated neutrophil extracellular trap formation. Curdione ameliorates Bleomycin (HY-17565A)-induced pulmonary fibrosis by inhibiting TGF-β-induced fibroblast-to-myofibroblast differentiation. Curdione exhibits neuroprotective effects against focal cerebral ischemia-reperfusion injury in rats. Curdione exerts antiproliferative effects against human uterine leiomyosarcoma by targeting IDO1. Curdione protects vascular endothelial cells and atherosclerosis by regulating DNMT1-mediated ERBB4 promoter methylation. Curdione inhibits inducible prostaglandin E2 production (IC50 = 1.1 μM) and cyclooxygenase 2 expression.
    Curdione (Standard)
  • HY-N17650
    Salviamarinic acid A
    		Inhibitor
    Salviamarinic acid A is a water-soluble phenolic acid that can be extracted from Salvia miltiorrhiza with potent anti-pulmonary fibrosis activity. Salviamarinic acid A significantly increases cell viability, cell index, cell motility and E-cadherin expression, and reduces TGF-β1, α-SMA and Collagen I levels. Salviamarinic acid A can be used for pulmonary fibrosis research.
    Salviamarinic acid A
  • HY-178191
    SGC stimulator 1
    		Inhibitor
    sGC stimulator 1 is a carbonyl sulfide (COS)/H2S-donor hybrid soluble guanylyl cyclase (sGC) stimulator (EC50 = 496 nM). sGC stimulator 1 exhibits a well-characterized H2S-releasing property. sGC stimulator 1 reduces fibrosis in TGF-β1-treated cardiac fibroblasts by increasing cGMP and H2S levels. sGC stimulator 1 can exert anti-fibrotic effects by activating sGC and increasing H2S. sGC stimulator 1 can be used for the study of heart failure (HF).
    SGC stimulator 1
  • HY-161376
    M4K2281
    		Inhibitor
    M4K2281 is a selecitve inhibitor for activin receptor-like kinase-2 (ALK2) with an IC50 of 2 nM. M4K2281 exhibits a moderate blood brain permeability with a brain to plasma ratio of 3.7 at 4h.
    M4K2281
  • HY-P11354
    THR-123
    		Agonist
    THR-123 is an orally active ALK3 peptide agonist. THR-123 has a relatively weak binding to ALK2, but does not bind to ALK6. THR-123 suppresses inflammation, apoptosis and the epithelial-to-mesenchymal transition program and reverses established fibrosis in five mouse models of acute and chronic renal injury. THR-123 can be used for the study of kidney fibrosis.
    THR-123
  • HY-178477
    LIFR/GPBAR1 modulator 1
    		Inhibitor
    LIFR/GPBAR1 modulator 1 is an orally active, potent GPBAR1 agonist (EC50 = 0.2 μM) and LIFR inhibitor (IC50 = 7.9 μM). LIFR/GPBAR1 modulator 1 upregulates leukaemia inhibitory factor (LIF)-mediated mRNA expression of LIFR and GPBAR1 and significantly reduces the expression of pro-fibrosis markers (COL1A1, ASMA, and TGFβ), and reduces TIMP1 expression and increases MMP9 expression. LIFR/GPBAR1 modulator 1 can be used for the study of human fibrotic disorders.
    LIFR/GPBAR1 modulator 1
  • HY-144437
    ALK5-IN-9
    		Inhibitor
    ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC50 values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease.
    ALK5-IN-9
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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