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-13462
    LY-364947
    		Inhibitor 99.14%
    LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II.
    LY-364947
  • HY-12071B
    LDN-193189 dihydrochloride
    		Inhibitor 99.75%
    LDN-193189 (dihydrochloride) is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.
    LDN-193189 dihydrochloride
  • HY-N1472
    Levistolide A
    		Inhibitor 99.26%
    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-10326
    GW788388
    		Inhibitor 99.92%
    GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
    GW788388
  • HY-15897
    LDN-212854
    		Inhibitor 99.70%
    LDN-212854 is a bone morphogenetic protein (BMP) inhibitor that potently inhibits ALK2 (IC50: 1.3 nM). LDN-212854 also inhibits ALK1 (IC50: 2.40 nM). LDN-212854 can be used in the research of fibrodysplasia ossificans progressive and cancers, such as hepatocellular carcinoma (HCC).
    LDN-212854
  • HY-13227
    SD-208
    		Inhibitor 99.87%
    SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.
    SD-208
  • HY-16712
    LDN-214117
    		Inhibitor 99.92%
    LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) [2]
    LDN-214117
  • HY-P99020
    Fresolimumab
    		Inhibitor 99.51%
    Fresolimumab (GC1008) is a high-affinity fully human monoclonal antibody that neutralizes the active form of human TGFβ1, TGFβ2, and TGFβ3. Fresolimumab can be used for the research of cancer and fibrotic diseases .
    Fresolimumab
  • HY-12953
    R-268712
    		Inhibitor 99.88%
    R-268712 is an orally active and selective ALK-5 inhibitor, with an IC50 of 2.5 nM. R-268712 inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM. R-268712 suppresses glomerulonephritis as well as glomerulosclerosis by inhibiting TGF-β signaling, which can be used in studies of renal fibrosis and cancer.
    R-268712
  • HY-12704
    ITD-1
    		Inhibitor 99.41%
    ITD-1 is the first selective TGFβ receptor inhibitor with an IC50 of 460 nM.
    ITD-1
  • HY-12274
    ML347
    		Inhibitor 99.94%
    ML347 (LDN193719) is a highly selective ALK1/ALK2 inhibitor. ML347 has IC50 values of 46 and 32 nM against ALK1 and ALK2, respectively, >300-fold selective over ALK3. ML347 block the phosphorylation of Smad1/5 by TGF-β1.
    ML347
  • HY-P3970A
    KRFK TFA
    		Agonist 99.25%
    KRFK TFA, a peptide derived from TSP-1, can activate TGF-β. KRFK TFA promotes TGF-β-mediated signaling and its downstream role, independent of thrombospondin (TSP) receptors such as CD47 and CD36. KRFK TFA can be used for chronic ocular surface inflammatory disorders reseach.
    KRFK TFA
  • HY-P99590
    Sotatercept
    		99.61%
    Sotatercept (ACE-011) is a soluble activin receptor 2A (ACVR2A) type IgG Fc fusion protein. Sotatercept combines activin and growth differentiation factor to try to restore the balance between growth promotion and growth inhibition signal pathways. Sotatercept has potential application in pulmonary arterial hypertension, anemia, bone loss, erythropoiesis, multiple myeloma (MM) osteolytic lesions.
    Sotatercept
  • HY-112331
    SJ000291942
    		Activator 99.41%
    SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway. BMPs are members of the transforming growth factor beta (TGFβ) family of secreted signaling molecules.
    SJ000291942
  • HY-12278
    K02288
    		Inhibitor 99.73%
    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
  • HY-P0299A
    LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)
    		Antagonist 99.73%
    LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier.
    LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)
  • HY-B1260
    Cetrimonium bromide
    		≥98.0%
    Cetrimonium bromide (CTAB), a quaternary ammonium, is an orally active cationic surfaetant. Cetrimonium bromide has toxicity and anticancer effect. Cetrimonium bromide inhibits cell migration and invasion through modulating the canonical and non-canonical TGF-β signaling pathways. Cetrimonium bromide can be used for DNA extraction.
    Cetrimonium bromide
  • HY-A0183
    Phosphatidylserine
    		Inducer ≥98.0%
    Phosphatidylserine (Phospholipids) is a well-conserved anti-inflammatory and immunosuppressive signal. Phosphatidylserine is involved in membrane translocation and the activation of protein kinase C, participating in Akt signaling through its interaction with PIP3. The local exposure of Phosphatidylserine can interact with complement and other proteins, promoting microglial phagocytosis during critical periods of synaptic refinement. Phosphatidylserine can promote blood coagulation in the extracellular environment and acts as a "eat me" signal to clear out apoptotic cells. Phosphatidylserine can suppress inflammation in tissues by inducing TGF-β secretion and inhibiting immune responses.
    Phosphatidylserine
  • HY-103021
    LY3200882
    		Inhibitor 99.86%
    LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC50 of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent.
    LY3200882
  • HY-P1068
    Lysozyme
    		Agonist
    Lysozyme (Muramidase) is a conserved antimicrobial protein. Lysozyme exerts its bactericidal effect by hydrolyzing bacterial cell wall peptidoglycan (PG). Lysozyme plays an important role in limiting bacterial growth on mucosal surfaces and other sites, not only controlling potential pathogens but also limiting overgrowth of microbiota to prevent dysbiosis. Extracellular lysozyme can also degrade polymeric PG into soluble fragments, activate NOD receptors in mucosal epithelial cells, and lead to the secretion of chemokines and activating factors by neutrophils and macrophages.
    Lysozyme
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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