1. Signaling Pathways
  2. TGF-beta/Smad
  3. TGF-β Receptor

TGF-β Receptor

Transforming growth factor beta receptors

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P5832
    BMP2-derived peptide
    Ligand 98.48%
    BMP2-derived peptide is a functional motif from positions 73 to 92 of the amino acid sequence of BMP-2. BMP2-derived peptide promotes osteogenic differentiation of bone marrow stromal cells (BMSCs) and enhances bone regeneration.
    BMP2-derived peptide
  • HY-13521A
    SB-505124 hydrochloride
    Inhibitor 99.34%
    SB-505124 hydrochloride is a selective inhibitor of?TGF-β Receptor type I receptor (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 hydrochloride
  • HY-136773
    KER047
    Inhibitor 99.35%
    ALK2-IN-4 is a potent ALK2 inhibitor extracted from patent WO2020086963A1, compound Formula I free base.
    KER047
  • HY-P99746
    Murlentamab
    Inhibitor
    Murlentamab (3C23K; GM102) is a humanized anti-AMHRII antibody. AMHRII is the anti-Müllerian hormone receptor. Murlentama significantly promotes macrophage-mediated antibody-dependent cell-mediated cytotoxicity (ADCC). Murlentama stimulates pro-inflammatory and anti-tumor internal environment, recruits and activates T cells. Murlentama suppresses tumors growth by inducing naïve macrophage orientation and promoting tumor-associated macrophage (TAM) reprogramming.
    Murlentamab
  • HY-P10388
    TAX2 peptide
    Antagonist 98.70%
    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-10327
    GW-6604
    Inhibitor ≥98.0%
    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
  • HY-109179A
    Itacnosertib (hydrocholide)
    Inhibitor 99.43%
    Itacnosertib hydrocholide is an inhibitor of JAK2, ACVR1 (ALK2) and ALK5.
    Itacnosertib (hydrocholide)
  • HY-P2294A
    pm26TGF-β1 peptide TFA
    99.68%
    pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.
    pm26TGF-β1 peptide TFA
  • 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-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-W107024
    BMS-986260
    Inhibitor 98.03%
    BMS-986260, an immuno-oncology agent, is a potent, selective, and orally active TGFβR1 inhibitor (IC50=1.6 nM). BMS-986260 displays exquisite selectivity for TGFβR1 over its isozyme TGFβR2, as well as in a panel of more than 200 kinases examined. BMS-986260 inhibits TGFβ mediated nuclear translocation of pSMAD2/3 in MINK and NHLF cells lines with an IC50 of 350 nM and 190 nM, respectively.
    BMS-986260
  • HY-P4651
    H-Tyr-Ile-Gly-Ser-Arg-NH2
    Inhibitor 98.92%
    H-Tyr-Ile-Gly-Ser-Arg-NH2 is a hexapeptide that is an essential fragment of laminin responsible for efficient cell adhesion and receptor binding. H-Tyr-Ile-Gly-Ser-Arg-NH2 promotes various epithelial cell adhesion activities.
    H-Tyr-Ile-Gly-Ser-Arg-NH2
  • HY-154970
    BMPR2-IN-1
    Inhibitor
    BMPR2-IN-1 (Compound 8a) is a BMPR2 inhibitor with an IC50 of 506 nM and a KD of 83.5 nM. BMPR2-IN-1 can be used for research of pulmonary arterial hypertension, Alzheimer’s disease and cancer.
    BMPR2-IN-1
  • HY-12273R
    DMH-1 (Standard)
    Inhibitor
    DMH-1 (Standard) is the analytical standard of DMH-1. DMH-1 is a potent and selective BMP inhibitor with IC50s of 27/107.9/<5/47.6 nM for ALK1/ALK2/ALK3/ALK6, respectively.
    DMH-1 (Standard)
  • HY-128437
    TGFβ-IN-5
    Inhibitor 98.03%
    TGFβ-IN-5(Compd 12) is a TGFβ inhibitor useful for the study of fibroproliferative diseases associated with TGF-β signaling.
    TGFβ-IN-5
  • 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-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-113604
    Pentabromopseudilin
    Inhibitor 98%
    Pentabromopseudilin (PBrP) is a marine antibiotic isolated from the marine bacteria Pseudomonas bromoutilis and Alteromonas luteoviolaceus. PBrP exhibits antimicrobial, anti-tumour and phytotoxic activities. PBrP is a reversible and allosteric inhibitor of myosin Va (MyoVa). PBrP also is a potent inhibitor of transforming growth factor-β (TGF-β) activity. PBrP can be used for the research of fibrotic diseases and cancer.
    Pentabromopseudilin
  • 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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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