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-125851
    TP-008
    		Inhibitor 99.42%
    TP-008 is a potent, selective and orally active (Activin-Like Kinase 5) ALK5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose.
    TP-008
  • HY-151289
    ALK5-IN-34
    		Inhibitor 98.21%
    ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC50 value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer.
    ALK5-IN-34
  • HY-P5542
    Vicatertide
    		Inhibitor 98.43%
    Vicatertide is a TGF beta-1 inhibitor.
    Vicatertide
  • HY-13783
    BIBF0775
    		Inhibitor 99.53%
    BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.
    BIBF0775
  • HY-130437
    p-nitro-Pifithrin-α
    		Inhibitor
    p-nitro-Pifithrin-α, a cell-permeable analog of pifithrin-α, is a potent p53 inhibitor. p-nitro-Pifithrin-α suppresses p53-mediated TGF-β1 expression in HK-2 cells. p-nitro-Pifithrin-α inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice fed a high-fat diet [4]. non-alcoholic fatty liver disease.
    p-nitro-Pifithrin-α
  • HY-P99944
    SHR-1701
    		99.77%
    SHR-1701 (Retlirafusp alfa) is a bifunctional fusion protein targeting PD-L1 and TGF-β for cancer research.
    SHR-1701
  • HY-118810
    BIO-013077-01
    		Inhibitor 99.63%
    BIO-013077-01 is a pyrazole TGF-β inhibitor.
    BIO-013077-01
  • HY-N2589
    Isosaponarin
    		Activator 99.59%
    Isosaponarin is a flavone glycoside isolated from wasabi leaves. Isosaponarin increases collagen synthesis, caused by up-regulated TGF-β type II receptor (TβR-II) and prolyl 4-hydroxylase (P4H) proteins production.
    Isosaponarin
  • HY-P99748
    Nadecnemab
    		Inhibitor
    Nadecnemab is an IgG4κ antibody targeting to GFRA3, glial cell derived neurotrophic factor family receptor alpha 3. Nadecnemab can be used for research of osteoarthritis of the knee/pain.
    Nadecnemab
  • HY-143891
    Chromenone 1
    		Activator 99.78%
    Chromenone 1 is a potent osteogenic bone morphogenetic protein (BMP) potentiator. Chromenone 1 exhibits a unique mode of action as it induces a pronounced, kinase-independent, negative TGFβ feedback that enhances nuclear BMP-Smad signaling outputs.
    Chromenone 1
  • HY-12071G
    LDN193189 (GMP)
    		Inhibitor
    LDN193189 (DM-3189) (GMP) is LDN193189 (HY-12071) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. LDN193189 is selective BMP type I receptor inhibitor.
    LDN193189 (GMP)
  • HY-129171
    TGFBR1-IN-1
    		Inhibitor
    TGFBR1-IN-1 is an ALK5 inhibitor extracted from patent WO2018004290A1, Compound 33, has an IC50 of 10-100 nM.
    TGFBR1-IN-1
  • HY-139858
    TGFβR-IN-1
    		Inhibitor
    TGFβR-IN-1 is a long-acting tumor-activated proagent of a TGFβR inhibitor.
    TGFβR-IN-1
  • HY-114192
    TGFβRI-IN-1
    		Inhibitor
    TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively .
    TGFβRI-IN-1
  • HY-112864
    TGFβRI-IN-6
    		Inhibitor
    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-P10388
    TAX2 peptide
    		Antagonist
    TAX2 peptide is a dodecapeptide based on molecular docking and simulation design, derived from the cell surface receptor CD47 sequence. TAX2 peptide acts as a selective antagonist of TSP-1 (thromboxin-1) interacting with CD47. TAX2 peptide can promote the binding of TSP-1 to CD36, which leads to the destruction of VEGFR2/KDR/Flk-1 (vascular endothelial growth factor receptor 2) activation, thereby blocking downstream NO (nitric oxide) signaling, demonstrating anti-angiogenic properties. TAX2 peptide can be used to study angiogenesis and tumor cell interactions in the tumor microenvironment.
    TAX2 peptide
  • HY-164145
    CDD-1653
    CDD-1653 is a potent and selective BMPR2 inhibitor (IC50=2.8 nM). CDD-1653 reduces the ability of ATP to bind to the kinase domain of BMPR2, thereby affecting the phosphorylation of SMAD1/5/8 transcription factors, which play a key role in the BMP signaling pathway. CDD-1653 can be used to study diseases related to the BMP signaling pathway.
    CDD-1653
  • HY-160237
    HYL001
    		Inhibitor
    HYL001 (compund 338) is a potent inhibitor of TGFβ receptor 1 (ALK5) that is approximately 9 times more potent than the structurally related compound Galunisertib (HY-13226) and is able to eliminate liver metastases established in mice.
    HYL001
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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