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-178231
    ALK5-IN-85
    Inhibitor
    ALK5-IN-85 (Compound 19) is a TGFβRI (ALK5) inhibitor with an IC50 < 100 ?nM. ALK5-IN-85 can be used for respiratory diseases including idiopathic pulmonary fibrosis, asthma, COPD and lumg cancer, and dermal and ocular fibrotic conditions research.
    ALK5-IN-85
  • HY-P3970C
    KQFK
    Control
    KQFK is an inactive control of KRFK (HY-P3970). KRFK is a peptide derived from TSP-1 that can activate TGF-β.
    KQFK
  • HY-P991880
    Anti-BMP6 Antibody
    Anti-BMP6 Antibody is an antibody against human BMP6. Recommend Isotype Controls:?Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-BMP6 Antibody
  • HY-151270
    ALK5-IN-25
    Inhibitor
    ALK5-IN-25 (compound EX-02) is a potent ALK-5 inhibitor with an IC50 ≤10 nM.ALK5-IN-25 also inhibits ALK-2 (selectivity ALK2/ALK5≤10). ALK5-IN-25 can be used for the research of cancer.
    ALK5-IN-25
  • HY-P991881
    KY1070
    Inhibitor
    KY1070 is a fully human anti-BMP6 antibody with a Kd of 0.00014 μM against the human BMP6. It exhibits high specificity for BMP6, showing no cross-reactivity with other members of the BMP family, and effectively inhibits BMP6-induced BMP receptor heterodimerization and hepcidin expression. KY1070 modulates Ferroportin expression on erythroid progenitor cells and accelerates erythropoiesis. In rodent anemia models, KY1070 reduces the required dose of erythropoietin (EPO) when used in combination with EPO and enhances the responsiveness of mice with chronic kidney disease (CKD)-associated anemia to EPO treatment. KY1070 is applicable for research on anemia of chronic disease [1] [2].
    KY1070
  • HY-167864
    M4K2308
    Inhibitor
    M4K2308 is a selective ether-linked inhibitor of ALK2 with an IC50 of 2 nM. M4K2308 exhibits exceptional selectivity for ALK2 over ALK5 (IC50 of 224 nM). M4K2308 has the potential for the study of diffuse intrinsic pontine glioma (DIPG) research.
    M4K2308
  • HY-P991882
    Anti-BMPR1B Antibody
    Anti-BMPR1B Antibody is an antibody against human BMPR1B. Recommend Isotype Controls:?Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-BMPR1B Antibody
  • HY-148246
    MU1700
    Inhibitor
    MU1700, a chemical probe, is an orally active and potent ALK1/2 inhibitor with IC50s of 13 nM and 6 nM, respectively. MU1700 shows cell membrane permeability and high brain permeability.
    MU1700
  • HY-13012S
    RepSox-d5
    RepSox-d5 (E-616452-d5) is the deuterium labeled RepSox (HY-13012). RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes.
    RepSox-d<sub>5</sub>
  • HY-P991382
    SAR-439459
    Inhibitor
    SAR-439459 is a human monoclonal antibody (mAb) targeting TGFB1/TGFβ-1. SAR-439459 blocks TGFβ-mediated pSMAD signaling, and suppression of T cells and NK cells. SAR-439459 has anti-tumor activity .
    SAR-439459
  • HY-149196
    TGFβ-IN-3
    Inhibitor
    TGFβ-IN-3 (Compound 8) is a long-acting tumor-activating prodrug of TGFβR1 inhibitor. TGFβ-IN-3 can achieve selective drug release in tumors, and the tumor/blood ratio is increased by 2.2 times. TGFβ-IN-3 can be used for the study of colon cancer.
    TGFβ-IN-3
  • HY-180336
    LM9
    Inhibitor
    LM9 is a potent, orally active MyD88 inhibitor. LM9 blocks TLR4/MyD88 binding, MyD88 homodimer formation, and TLR4/MyD88/NF-κB signaling pathway activation. LM9 prevents atherosclerosis by regulating inflammatory responses and oxidative stress in macrophages. LM9 efficiently mitigates inflammatory responses and fibrosis in obesity-induced cardiomyopathy. LM9 can be used for fibrosis and atherosclerosis research.
    LM9
  • HY-151273
    ALK5-IN-27
    Inhibitor
    ALK5-IN-27 (Compound EX-04) is a potent ALK-5 inhibitor with an IC50 ≤10 nM. ALK5-IN-27 also inhibits ALK-2 (selectivity ALK2/ALK5 ≤10).
    ALK5-IN-27
  • HY-118970
    LG190155
    Activator
    LG190155 is a nonsteroidal vitamin D receptor (VDR) agonist. LG190155 activates VDR in mesenchymal stem cells, thereby upregulating the BMP6-IL6 autocrine axis. Pretreatment of mesenchymal stem cells with LG190155 significantly enhances their ability to induce differentiation of acute myeloid leukemia cells, without inducing hypercalcemia. LG190155 is applicable to research related to acute myeloid leukemia (AML).
    LG190155
  • HY-177657A
    Pixofisiran sodium
    Inhibitor
    Pixofisiran sodium is a siRNA in STP705. It targets to TGF‐β1. STP705 is composed of 2 siRNA oligonucleotides (Pixofisiran and Lixadesiran) that individually target TGF-β1 and COX-2 mRNA.
    Pixofisiran sodium
  • HY-185430
    HM-279
    Inhibitor
    HM-279 is a potent and orally active ALK5 inhibitor with an IC50 of 4.7 nM. HM-279 shows cross-reactivity with ALK7 (IC50 = 6.8 nM), but HM-279 has fair to good selectivity against other TGF-β receptor family kinases, with 4.5-693-fold selectivity. HM-279 demonstrates antitumor activity in vivo through CD8+ T cell immunity. HM-279 can be used for the research of colon cancer.
    HM-279
  • HY-121025
    BUR1
    Inhibitor 99.65%
    BUR1 is a BMP upregulator (EC50: 98 nM) and activates BMPRII signalling. BUR1 induces BMP2 and PTGS2 expression. BUR1 reversed pulmonary arterial pressure in Monocrotaline (HY-N0750) induced rats.
    BUR1
  • HY-177657
    Pixofisiran
    Inhibitor
    Pixofisiran is a siRNA in STP705. It targets to TGF‐β1. STP705 is composed of 2 siRNA oligonucleotides (Pixofisiran and Lixadesiran) that individually target TGF-β1 and COX-2 mRNA.
    Pixofisiran
  • HY-N4019
    Maohuoside A
    99.47%
    Maohuoside A, a single compound isolated from the E. koreanum that potently promotes osteogenesis. Maohuoside A enhances the osteogenesis of bone marrow-derived mesenchymal stem cells via bone morphogenetic protein (BMP) and MAPK signaling pathways.
    Maohuoside A
  • HY-145855
    J-1063
    Inhibitor
    J-1063 is a potent, selective and orally active ALK5 inhibitor with an IC50 of 0.039 µM. J-1063 shows anti-fibrotic effect by the inhibition of inflammatory infiltration, collagen deposition, and hepatocytes necrosis. J-1063 has the potential for the research of liver fibrosis.
    J-1063
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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