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-19628
    OD36
    		Inhibitor 98.70%
    OD36 is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 shows ALK2-directed activity with KDs of 37 nM.
    OD36
  • 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-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-132290
    TGFβRI-IN-3
    		Inhibitor 98.04%
    TGFβRI-IN-3 inhibits TGFβR1 at an IC50 of 0.79 nM with 2000-fold selectivity against MAP4K4. TGFβRI-IN-3 represents a highly selective TGFβR1 inhibitor that has potential applications in immuno-oncology.
    TGFβRI-IN-3
  • HY-150793
    SY-LB-57
    		Agonist 99.26%
    SY-LB-57 is a highly potent bone morphogenetic protein (BMP) receptor signaling agonist. SY-LB-57 can be used in studies of diseases such as fractures and pulmonary arterial hypertension.
    SY-LB-57
  • HY-146693
    CJJ300
    		Inhibitor 99.77%
    CJJ300 is a transforming growth factor-β (TGF-β) inhibitor with an IC50 of 5.3 µM. CJJ300 inhibits TGF-β signaling by disrupting the formation of the TGF-β-TβR-I-TβR-II signaling complex.
    CJJ300
  • HY-18766
    EW-7195
    		Inhibitor 99.20%
    EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung.
    EW-7195
  • HY-115669
    Pentachloropseudilin
    		Inhibitor 98.88%
    Pentachloropseudilin (Antibiotic A 15104 Y; PClP) is a reversible and allosteric potent inhibitor of Myo1s (class 1 myosins) with IC50s range from 1 to 5 μM for mammalian class-1 myosins and greater than 90 μM for class-2 and class-5 myosins. Pentachloropseudilin is a potent inhibitor of transforming growth factor-β (TGF-β)-stimulated signaling, with an IC50 of 0.1 to 0.2 μM for TGF-β.
    Pentachloropseudilin
  • HY-144043
    ALK5-IN-8
    		Inhibitor 98.06%
    ALK5-IN-8 is a potent inhibitor of TGFβRI (ALK5). ALK5-IN-8 Inhibits the phosphorylation of ALK5 on its downstream signaling proteins (Smad2 or Smad3) by blocking the binding of TGFβRI to ligands, thereby affecting or blocking TGF-β signaling. ALK5-IN-8 has the potential for the research of various ALK5-mediated related diseases (extracted from patent WO2021190425A1, compound 1).
    ALK5-IN-8
  • HY-78349
    A 77-01
    		Inhibitor 99.68%
    A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM.
    A 77-01
  • HY-122856
    AZ12601011
    		Inhibitor 99.88%
    AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
    AZ12601011
  • HY-109179
    Itacnosertib
    		Inhibitor 99.77%
    Itacnosertib (TP-0184) is both inhibitor to JAK2, ACVR1 (ALK2) and ALK5 as described in WO2014151871.
    Itacnosertib
  • HY-118528A
    TP0427736 hydrochloride
    		Inhibitor 99.22%
    TP0427736 hydrochloride is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50=836 nM). TP0427736 hydrochloride also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. TP0427736 hydrochloride can be used for the research of androgenic alopecia (AGA).
    TP0427736 hydrochloride
  • HY-151427
    TGFβ1-IN-1
    		Inhibitor 99.89%
    TGFβ1-IN-1 (compound 42) is a potent, orally active TGF-β1 inhibitor. TGFβ1-IN-1 inhibits the upregulation of TGF-β1-induced fibrosis markers (α-SMA and fibronectin) and can be used in liver fibrosis disease studies.
    TGFβ1-IN-1
  • 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-P99632
    Garetosmab
    		Inhibitor
    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-123900
    AZ12799734
    		Inhibitor 98.07%
    AZ12799734 is a selective, orally active TGFBR1 kinase inhibitor with an IC50 of 47 nM. AZ12799734 is also a pan BMP and TGFβ inhibitor.
    AZ12799734
  • HY-100434
    PD-161570
    		Inhibitor 99.04%
    PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.
    PD-161570
  • HY-136773A
    KER047 succinate
    		Inhibitor 98.93%
    ALK2-IN-4 succinate is a potent ALK2 inhibitor extracted from patent WO2020086963A1, compound Formula I free base.
    KER047 succinate
  • HY-145608
    Zilurgisertib
    		Inhibitor 99.77%
    Zilurgisertib (INCB-000928; NBU-928) is a selective ALK 2 inhibitor for researching diseases such as cancer.
    Zilurgisertib
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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