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-175257
    Theophylline-platinum(IV) prodrug-1
    		Inhibitor
    Theophylline-platinum(IV) prodrug-1 is a PARP-1 inhibitor. Theophylline-platinum(IV) prodrug-1 enhances DNA damage, ROS production, mitochondrial dysfunction, apoptosis and S-phase arrest, along with reducing invasion and metastasis in cells. Theophylline-platinum(IV) prodrug-1 exhibits superior antitumor activity in the xenograft SKOV3-BRCA1-KD tumor model. Theophylline-platinum(IV) prodrug-1 can be used for the study of ovarian cancer.
    Theophylline-platinum(IV) prodrug-1
  • HY-P992076
    Anti-Candida auris β-1, 3 glucans Antibody (2G8)
    		Inhibitor
    Anti-Candida auris β-1,3-glucans Antibody (2G8) is an antibody targeting Candida auris β-1,3-glucans, and also acts as an inhibitor of AChE and TGF-β receptor 2. Anti-Candida auris β-1,3-glucans Antibody (2G8) also targets fungal cell wall components, effectively inhibits fungal growth and interferes with capsule formation, thereby significantly reducing the fungal load in mouse tissues. Anti-Candida auris β-1,3-glucans Antibody (2G8) not only blocks TGF-β receptor binding to inhibit the Smad signaling pathway, reduces fibroblast activation and collagen deposition, but also induces epithelial differentiation of tumor cells and reduces pancreatic tumor metastasis. Anti-Candida auris β-1,3-glucans Antibody (2G8) specifically binds to the conserved N-linked glycoepitope on AChE to inhibit its activity without interfering with BChE, and can be used in studies of cryptococcosis and related tumor mechanisms.The isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-Candida auris β-1, 3 glucans Antibody (2G8)
  • HY-160215A
    GFH018 methylbenzenesulfonate
    		Inhibitor
    GFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC50 of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer, breast cancer, and relapsed/metastatic nasopharyngeal carcinoma.
    GFH018 methylbenzenesulfonate
  • HY-177657B
    Pixofisiran sodium scrambled negative control
    		Inhibitor
    Pixofisiran sodium scrambled negative control is the sequence scrambled negative control of Pixofisiran sodium.
    Pixofisiran sodium scrambled negative control
  • HY-P991856
    ANB012
    ANB012 is an antibody against human ACVR2B.
    ANB012
  • HY-W012856
    3-Ethyltoluene
    3-Ethyltoluene (3-Methylethylbenzene) is an isomer of Ethyltoluenes. 3-Ethyltoluene inhibits cell survival and proliferation and increases ROS production. 3-Ethyltoluene upregulates cellular inflammatory gene expression. 3-Ethyltoluene induces cell fibrosis with increased level of AST, FGF-23, Cyt-7 p21, TGFβ, TIMP2, and MMP2. 3-Ethyltoluene can be used for liver diseases such as NAFLD research.
    3-Ethyltoluene
  • HY-12278G
    K02288 (GMP)
    		Inhibitor
    K02288 (GMP) is K02288 (HY-12278) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC50s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC50s of of 5-34 nM.
    K02288 (GMP)
  • HY-124487
    GK-136901
    		Inhibitor
    GK-136901 is an orally active, dual Nox1/Nox4 NADPH oxidase inhibitor with a Ki of 160 nM for Nox1 and 165 nM for Nox4. GK-136901 potently blocks high glucose-induced intracellular reactive oxygen species production, p38-MAPK phosphorylation, and upregulation of TGF-β1/2 and fibronectin (fibronectin) in renal cells. GK-136901 also inhibits the proliferation of mouse pulmonary vascular cells under hypoxic conditions. GK-136901 is applicable to the research on the pathogenesis of type 2 diabetic nephropathy, high glucose-related renal lesions and pulmonary hypertension.
    GK-136901
  • HY-P5081A
    Endotrophin (Mus musculus) TFA
    		Activator
    Endotrophin (Mus musculus) TFA is an adipokine, a cleavage fragment derived from Collagen VI, whose levels are elevated in adipose tissue and breast tumors of obese mice. Endotrophin (Mus musculus) TFA activates the TGF-β signaling pathway and reduces the expression of hormone-sensitive lipase. Endotrophin (Mus musculus) TFA induces adipogenesis, lipid accumulation, fibrosis, inflammation, angiogenesis, adipose tissue expansion, epithelial-mesenchymal transition, and insulin resistance; it also induces Cisplatin (HY-17394) resistance in cancer cells. Endotrophin (Mus musculus) TFA can be used in research related to metabolic diseases such as obesity and type 2 diabetes, as well as cancers such as breast cancer.
    Endotrophin (Mus musculus) TFA
  • HY-151283
    ALK5-IN-33
    		Inhibitor
    ALK5-IN-33 (Compound EX-10) is a selective, orally active ALK-5 inhibitor with an IC50 ≤10 nM.
    ALK5-IN-33
  • HY-P5081
    Endotrophin (Mus musculus)
    		Activator
    Endotrophin (Mus musculus) is an adipokine, a cleavage fragment derived from Collagen VI, whose levels are elevated in adipose tissue and breast tumors of obese mice. Endotrophin (Mus musculus) activates the TGF-β signaling pathway and reduces the expression of hormone-sensitive lipase. Endotrophin (Mus musculus) induces adipogenesis, lipid accumulation, fibrosis, inflammation, angiogenesis, adipose tissue expansion, epithelial-mesenchymal transition, and insulin resistance; it also induces Cisplatin (HY-17394) resistance in cancer cells. Endotrophin (Mus musculus) can be used in research related to metabolic diseases such as obesity and type 2 diabetes, as well as cancers such as breast cancer.
    Endotrophin (Mus musculus)
  • HY-179535
    Axl-IN-21
    		Inhibitor
    Axl-IN-21 is an orally active and selective AXL inhibitor (Kd = 2.7 nM, IC50 = 4.0 nM). Axl-IN-21 displays kinase selectivity and retains strong activity against cancer-related mul-kinases (Mer with Kd = 1.4 nM, DDR1 with IC50 = 22.2 nM, HIPK4 with Kd = 11.0 nM and LOK with Kd =10 nM). Axl-IN-21 overcomes tumor microenvironment-driven resistance by blocking CAF-derived GAS6-induced AXL/STAT3/ABCG1 signaling, restoring chemosensitivity and inhibiting drug efflux in gastric cancer (GC). Axl-IN-21 suppresses TGF-β1-induced epithelial-mesenchymal transition (EMT), migration, and invasion in MDA-MB-231 cells. Axl-IN-21 exhibits no significant cytotoxicity in non-cancerous cells. Axl-IN-21 can be research for triple negative breast cancer and gastric cancer[1] [2] .
    Axl-IN-21
  • HY-107614G
    1-Oleoyl lysophosphatidic acid sodium (GMP)
    		Activator
    1-Oleoyl lysophosphatidic acid sodium (GMP) is the GMP-grade form of 1-Oleoyl lysophosphatidic acid sodium (HY-107614). GMP-grade small molecules serve as auxiliary reagents in cell therapy. 1-Oleoyl lysophosphatidic acid sodium is a bioactive lipid signaling molecule. 1-Oleoyl lysophosphatidic acid sodium inhibits lysoPLD-catalyzed hydrolysis of lysophosphatidylcholine and FS-3. 1-Oleoyl lysophosphatidic acid sodium activates LPA1 and LPA2, thereby triggering calcium mobilization, NFATc1 translocation, Rho/ROCK activation, Smad2/3 phosphorylation and c-Fos expression. 1-Oleoyl lysophosphatidic acid sodium induces anxiety-like, depression-like and hypoactivity phenotypes, regulates osteoclast cytoskeleton and viability, reduces osteoclast bone resorptive activity, and drives mesenchymal stem cell differentiation into myofibroblast-like cells. 1-Oleoyl lysophosphatidic acid sodium stimulates the secretion of transforming growth factor-β1 and stromal cell-derived factor-1. 1-Oleoyl lysophosphatidic acid sodium is applicable to research related to anxiety, depression and ovarian cancer.
    1-Oleoyl lysophosphatidic acid sodium (GMP)
  • HY-162929
    TP-DEA2
    		Inhibitor
    TP-DEA2, a predictable-release Triptolide (HY-32735) prodrug, block Bleomycin-induced pulmonary fibrosis and inflammation. TP-DEA2 significantly inhibits α-SMA production.
    TP-DEA2
  • HY-161662
    ALK5-IN-80
    		Inhibitor
    ALK5-IN-80 (Compound 29b) is a selective ALK5 inhibitor with an IC50 value of 3.7 nM. ALK5-IN-80 can be used for cancer research.
    ALK5-IN-80
  • HY-P991863
    GM103 antibody
    GM103 Antibody is a humanized IgG1 antibody against AMHRII. GM103 Antibody can generate antibody drug conjugate (ADC) (GM103) with a potent auristatin derivative. GM103 Antibody can be used for the study of ovarian cancer and hepatocarcinoma.
    GM103 antibody
  • HY-P3970
    KRFK
    		Agonist
    KRFK, a peptide derived from TSP-1, can activate TGF-β. KRFK promotes TGF-β-mediated signaling and its downstream role, independent of thrombospondin (TSP) receptors such as CD47 and CD36. KRFK can be used for chronic ocular surface inflammatory disorders reseach.
    KRFK
  • HY-P991158
    Rinvatercept
    Rinvatercept, a fusion protein, is a glycyl (1)-chimeric N-terminal (1-108)-peptide (2-109) combined from the sequences of the extracellular domains of the human ACVR2A/B, and is fused via a G3 peptide linker (110-112) to an immunoglobulin G1 (IgG1) Fc fragment. Rinvatercept can be used for research of neuromuscular disease.
    Rinvatercept
  • HY-P992453
    RO-7303509
    		Inhibitor
    RO-7303509 (MTBT1466A; RG-6315) is a human monoclonal antibody and TGFβ3 neutralizer. RO-7303509 targets the profibrotic mediator TGFβ3 to alleviate fibrosis. RO-7303509 can be administered via subcutaneous or intravenous routes and is used in research on systemic sclerosis. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001).
    RO-7303509
  • HY-100113A
    Buloxibutid hydrochloride
    		Inhibitor
    Buloxibutid (AT2 receptor agonist C21) hydrochloride is an orally active, selective angiotensin II type 2 receptor (AT2R) agonist, with a Ki value of 0.4 nM for porcine AT2R. Buloxibutid hydrochloride exerts vasodilatory, anti-inflammatory, antifibrotic (promoting the expression of collagenase MMP-13) and tissue repair effects mainly by activating the NO/cGMP pathway, inhibiting the pro-proliferative MAPK signaling, and suppressing the pro-fibrotic TGF-β/Smad pathway and inflammatory NF-κB pathway. Buloxibutid hydrochloride can be used in research related to idiopathic pulmonary fibrosis, hypertension, systemic sclerosis and other conditions.
    Buloxibutid hydrochloride
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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