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

TGF-β Receptor

Transforming growth factor beta receptors

TGF-β Receptor

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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-147786
    TGFβRI-IN-5
    		Inhibitor
    TGFβRI-IN-5 (Compound 4b) is a potent inhibitor of TGFβRI with an IC50 of 0.08 μM. TGFβRI-IN-5 displays amazing anticancer activity 5–7 times that of reference agent against all the tested cell lines. TGFβRI-IN-5 enhances apoptosis and arrested G2/M phase of cell cycle.
    TGFβRI-IN-5
  • HY-151954
    TGFβ1-IN-2
    		Inhibitor
    TGFβ1-IN-2 is a diarylacylhydrazones derivative that effectively suppresses the activation and proliferation of fibroblasts. TGFβ1-IN-2 can be used for idiopathic pulmonary fibrosis (IPF) research.
    TGFβ1-IN-2
  • HY-151955
    TGFβ1-IN-3
    		Inhibitor
    TGFβ1-IN-3 is a diarylacylhydrazones derivative that effectively suppresses the activation and proliferation of fibroblasts. TGFβ1-IN-3 can be used for idiopathic pulmonary fibrosis (IPF) research.
    TGFβ1-IN-3
  • HY-P991383
    LY2382770
    		Inhibitor
    LY2382770 is a human monoclonal antibody (mAb) targeting TGFB1. LY2382770 can be used in dabetic nephropathies research.
    LY2382770
  • HY-172108
    TGFβRI-IN-7
    		Inhibitor
    TGFβRI-IN-7 (compound 16W) is a potent inhibitor of TGFβRI. TGFβRI-IN-7 inhibits SMAD2/3 phosphorylation and H22 cell viability with IC50 values of 12 and 65 nM, respectively. TGFβRI-IN-7 shows anti-tumor efficacy in a xenograft model of H22 cells, with TGI of 79.6 %.
    TGFβRI-IN-7
  • HY-142949
    ALK5-IN-7
    		Inhibitor
    ALK5-IN-7 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-7 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 4).
    ALK5-IN-7
  • HY-E70866
    TGFβR1 Recombinant Human Active Protein Kinase
    TGFβR1 plays an important role in TGF-β signaling transduction and serves as a tumor suppressor. TGFβR1 Recombinant Human Active Protein Kinase is a recombinant TGFβR1 protein that can be used to study TGFβR1-related functions.
    TGFβR1 Recombinant Human Active Protein Kinase
  • HY-122179
    NUCC-555
    		Antagonist
    NUCC-555 is an activin antagonist. NUCC-555 interacts with Trp25, Trp28, Phe55, Tyr93, Lys103, and Asn107 in the Activin A binding pocket. NUCC-555 blocks Activin A-mediated hepatic stellate cells (HSCs) activation. NUCC-555 promotes liver regeneration and halts fibrosis progression in chronic liver disease models. NUCC-555 inhibits Activin A-mediated ovarian cell proliferation. NUCC-555 decreases FSH levels in ovariectomized mice.
    NUCC-555
  • HY-171249
    CDD-1431
    		Inhibitor
    CDD-1431 is a low-nanomolar selective kinase inhibitors of BMPR2, with Kiapp value of 20.6 nM. CDD-1431 suppresses BRE-reporter activity, with an IC50 of 4.87 μM. BMP controls cellular processes across many tissue types, including the kidney, skeletal muscle, heart, and reproductive organs. BMP induces ectopic bone formation.
    CDD-1431
  • HY-161400
    TGFβRII-IN-2
    		Inhibitor
    TGFβRII-IN-2 (Compound 3n) is an inhibitor for transforming growth factor-β type II receptor (TGFβRII) with IC50 of 2.4 μM, which blocks endothelial-to-mesenchymal transition and cell migration in different cancer cell lines without perturbing the microtubule network.
    TGFβRII-IN-2
  • 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-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-P990327
    Anti-ACVR2B Antibody
    		Inhibitor
    The Anti-ACVR2B Antibody is a human antibody expressed in CHO cells, targeting ACVR2B. The Anti-ACVR2B Antibody has huIgG1 heavy chain and huκ light chain, with a predicted molecular weight (MW) of 144.42 kDa. The isotype control for the Anti-ACVR2B Antibody can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-ACVR2B Antibody
  • 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-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-161398
    TGFβRII-IN-3
    		Degrader
    TGFβRII-IN-3 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) (IC50 = 4.1 μM). TGFβRII-IN-3 inhibits TGFβ signaling by promoting the proteolytic degradation of TGFβ RII. TGFβRII-IN-3 can block endothelial-to-mesenchymal transition and cell migration. TGFβRII-IN-3 can be used in cancer research.
    TGFβRII-IN-3
  • 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-173149
    CDD-2789
    		Inhibitor
    CDD-2789 is a highly selective small-molecule inhibitor targeting Activin receptor type 1 (ALK2, also known as ACVR1). It blocks the SMAD1/5 signaling pathway mediated by ALK2/ALK1, thereby effectively suppressing downstream phosphorylation events induced by BMP and activin A. In the NanoBRET cellular model, CDD-2789 exhibits an inhibitory IC50 of 0.54 µM against ALK2. CDD-2789 holds promise for research on ALK2-related diseases, including diffuse intrinsic pontine glioma (DIPG), ependymoma, endometrial cancer, melanoma, non–small cell lung cancer, colorectal cancer, and pancreatic cancer.
    CDD-2789
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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