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

TGF-β Receptor

Transforming growth factor beta receptors

TGF-β Receptor

Related Products

PDF 0.93 MB

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-19767
    GSK 3008348
    		Inhibitor 98.04%
    GSK 3008348 is a small molecule antagonist of integrin αvβ6 with IC50 values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 can be used for research on pulmonary fibrosis and various types of cancer.
    GSK 3008348
  • HY-P991504
    LAE-102
    		Antagonist 99.46%
    LAE-102 is the selective anti-ActRIIA (activin receptor type IIA or ACVR2) monoclonal antibody. LAE-102 increases muscle mass and reduces fat mass. LAE102 can increase serum activin A levels in vivo. LAE-102 is promising for research of obesity.
    LAE-102
  • HY-N1472
    Levistolide A
    		Inhibitor 99.34%
    Levistolide A is an apoptosis inducer and a PEDV virus inhibitor. Levistolide A can induce apoptosis in colon cancer cells and suppress the replication of porcine epidemic diarrhea virus (PEDV) by promoting ROS generation. Levistolide A activates peroxisome proliferator-activated receptor γ (PPARγ) in N2a/APP695swe cells and reduces excessive phosphorylation of tau through the GSK3α/β pathway, improving symptoms in Alzheimer’s mice. Levistolide A improves kidney damage in 5/6 nephrectomy (Nx) mice by inhibiting the RAS,TGF-β1/Smad, and MAPK pathways.
    Levistolide A
  • HY-P0301A
    SLLK, Control Peptide for TSP1 InhibitorTFA
    		Control 99.83%
    SLLK, Control Peptide for TSP1 Inhibitor (TFA) is a control peptide for LSKL, which is a Thrombospondin (TSP-1) inhibitor.
    SLLK, Control Peptide for TSP1 InhibitorTFA
  • HY-19767A
    GSK 3008348 hydrochloride
    		Inhibitor 99.86%
    GSK 3008348 hydrochloride is a small molecule antagonist of integrin αvβ6 with IC50 values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 hydrochloride can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 hydrochloride prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 hydrochloride can be used for research on pulmonary fibrosis and various types of cancer.
    GSK 3008348 hydrochloride
  • HY-117887
    Fidrisertib
    		Inhibitor 98.58%
    Fidrisertib (BLU-782) is the orally active inhibitor for activin receptor-like kinase 2 (ALK2) that inhibits ALK2R206H, ALK2, ALK1, ALK6, ALK3, ALK4, TGFβR2 and ALK5 with IC50s of 0.2, 0.6, 3, 24, 45, 65, 67 and 155 nM, respectively.
    Fidrisertib
  • HY-150169
    THRX-144644
    		Inhibitor 99.90%
    THRX-144644 is a Lung-restricted ALK5 inhibitor with an IC50 value of 0.14 nM. THRX-144644 avoids systemic toxicities associated with TGFβ pathway inhibition.
    THRX-144644
  • HY-154970A
    BMPR2-IN-1 TFA
    		Inhibitor 99.40%
    BMPR2-IN-1 TFA is a selective BMPR2 inhibitor with a human BMPR2 IC50 of 506 nM and a Kd of 83.5 nM. BMPR2-IN-1 TFA functions as an ATP mimetic, forming hydrogen bonds with the BMPR2 kinase domain backbone and hydrophobic interactions with specific residues, and demonstrates high selectivity for BMPR2 over other kinases.BMPR2-IN-1 TFA can be used for the researches of cancer, pulmonary arterial hypertension and Alzheimer’s disease.
    BMPR2-IN-1 TFA
  • HY-12071G
    LDN193189 (GMP)
    		Inhibitor
    LDN193189 GMP is LDN193189 (HY-12071) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. LDN193189 (DM-3189) is a potent selective BMP type I receptor (BMP I) inhibitor. LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.
    LDN193189 (GMP)
  • HY-Y1117
    Melamine
    		99.97%
    Melamine is an orally active inducer of Apoptosis. Melamine induces animal disease models. Melamine affects the activity of Sertoli cell and can be used for research on male reproductive function. Melamine also has neurotoxicity and nephrotoxicity. Melamine induces cognitive impairment and acute kidney injury models. Melamine can also be used to induce bladder cancer and urinary stone models.
    Melamine
  • HY-113604
    Pentabromopseudilin
    		Inhibitor 99.63%
    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-100434
    PD-161570
    		Inhibitor 99.82%
    PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.
    PD-161570
  • HY-111482
    SM 16
    		Inhibitor 99.82%
    SM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively.
    SM 16
  • HY-164793
    TGFBR1-IN-2
    		Inhibitor
    TGFBR1-IN-2 (Compound AQA) is a TGFBR1 inhibitor and an antibacterial agent. TGFBR1-IN-2 is a substrate for cytochrome P450s. TGFBR1-IN-2 contains the pyridyl-6-methyl moiety necessary for Mycobacterium tuberculosis inhibition and has potent inhibitory activity against non-replicating and persistent Mycobacterium tuberculosis.
    TGFBR1-IN-2
  • 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-150793
    SY-LB-57
    		Agonist 99.66%
    SY-LB-57 is a highly potent bone morphogenetic protein (BMP) receptor signaling agonist. SY-LB-57 can be used in studies of diseases such as fractures and pulmonary arterial hypertension.
    SY-LB-57
  • HY-168990
    Ontunisertib
    		Inhibitor 99.95%
    Ontunisertib (AGMB-129) is an orally active and selective gastrointestinal-restricted ALK5 (TGFβR1) inhibitor. Ontunisertib blocks signalling of the pro-fibrotic TGFβ pathway. Ontunisertib can be used for the research of fibrostenotic Crohn’s disease.
    Ontunisertib
  • HY-145608
    Zilurgisertib
    		Inhibitor 98.25%
    Zilurgisertib (INCB-000928; NBU-928) is a selective ALK2 inhibitor with an IC50 value of 15 nM. Zilurgisertib inhibits SMAD1/5 phosphorylation with an IC50 value of 63 nM. Zilurgisertib inhibits hepcidin production and improve anemia. Zilurgisertib can be used in melanoma research.
    Zilurgisertib
  • HY-N0891
    Tubeimoside II
    		99.90%
    Tubeimoside II is an orally active triterpenoid saponin and antiviral agent that binds to PACT/PRKRA with Kd values of 5.37 μM and 133.1 μM, respectively. Tubeimoside II inhibits oxidase-dependent EGFR activation and reduces TGF-β1-induced oxidative stress. Tubeimoside II activates the RIG-I signaling pathway and increases IFN-β secretion. Tubeimoside II suppresses TPA-induced ear edema, mouse sarcoma 180 growth, and TPA-induced skin tumor formation. Tubeimoside II exerts broad-spectrum antiviral activity against SARS-CoV-2, HCoV-OC43, and IAV-H1N1/FM1. Tubeimoside II can be used in research related to retinoblastoma, respiratory viral infections, skin tumors, and sarcoma 180.
    Tubeimoside II
  • HY-78349
    A 77-01
    		Inhibitor 99.92%
    A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM.
    A 77-01
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.