- Signaling Pathways
- TGF-beta/Smad
- 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.
TGF-β Receptor Isoform Specific Products
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TGF-β Receptor
(203)
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ALK1
(8)
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ALK2
(29)
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ALK3
(12)
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ALK4
(10)
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ALK5
(31)
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ALK6
(7)
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ALK7
(7)
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TGFβR2
(4)
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ACVR2A
(5)
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ACVR2B
(3)
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BMP
(1)
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GDF15
(12)
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All Product Categories
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TGF-β Receptor Inhibitors
(223)
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TGF-β Receptor Agonists
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TGF-β Receptor Antagonists
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TGF-β Receptor Activators
(17)
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TGF-β Receptor Modulator
(1)
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TGF-β Receptor Inducer
(1)
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TGF-β Receptor Degraders
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TGF-β Receptor Controls
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TGF-beta Receptor Proteins
(22)
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ALK-3 Proteins
(4)
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ALK-6 Proteins
(3)
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BMP Type II Receptor (BMPR2) Proteins
(5)
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ALK-2/ACVR1 Proteins
(14)
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ALK-4/Activin RIB Proteins
(7)
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ALK-7 Proteins
(6)
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Activin A Receptor Type 2A (ACTR-IIA) Proteins
(9)
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Activin A Receptor Type 2B (ACVR2B) Proteins
(10)
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ALK-1/ACVRL1 Proteins
(9)
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Anti-Muellerian Hormone Type-2 Receptor (AMHR2) Proteins
(8)
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TGF-β Receptor 1 Proteins
(6)
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TGF-beta Receptor 2 Proteins
(12)
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Type III TGF-β Receptor Proteins
(3)
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ALK-3/CD292 Proteins
(4)
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TGF-β Receptor Related Products (313)
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Recombinant Proteins (97)
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Antibodies (16)
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TGF-β Receptor Isoform Comparison
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SB-431542
0 ImagesSB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitory activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways. -
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- A 83-01
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Dorsomorphin
0 ImagesSynonyms: BML-275 -
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LDN193189
0 ImagesSynonyms: DM-3189LDN193189 (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. -
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Galunisertib
0 ImagesSynonyms: LY2157299Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM. -
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THR-123 TFA
0 ImagesCat. No.: HY-P11354ATHR-123 TFA is an orally active ALK3 peptide agonist. THR-123 TFA has a relatively weak binding to ALK2, but does not bind to ALK6. THR-123 TFA suppresses inflammation, Apoptosis and the epithelial-to-mesenchymal transition program and reverses established fibrosis in five mouse models of acute and chronic renal injury. THR-123 TFA can be used for the study of kidney fibrosis. -
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TGFβ1-IN-5
0 ImagesCat. No.: HY-183258TGFβ1-IN-5 is a TGF-β1 inhibitor with blood-brain barrier permeability. TGFβ1-IN-5 reduces extracellular TGF-β1 levels in glioblastoma cells. TGFβ1-IN-5 exerts antiproliferative, antimigratory and clonogenic inhibitory effects in glioblastoma cells while maintaining the viability of non-cancerous cells. TGFβ1-IN-5 can be used for the research of glioblastoma. -
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JMT203
0 ImagesCat. No.: HY-P992393 -
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Dorsomorphin dihydrochloride
0 ImagesSynonyms: Compound C dihydrochloride; BML-275 dihydrochlorideDorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599). -
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RepSox
0 ImagesSynonyms: E-616452; SJN 2511RepSox (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. -
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Bimagrumab
0 ImagesSynonyms: Anti-ACVR2B Reference Antibody; BYM338Bimagrumab (Anti-ACVR2B Reference Antibody) is a human monoclonal antibody that blocks activin type II receptor (ActRII), with KDs of 1.7 pM and 434 pM for human ActRIIB and ActRIIA, respectively. Bimagrumab can be used for the research of pathological muscle loss and weakness. -
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DMH-1
0 ImagesDMH-1 is a selective BMP inhibitor. DMH-1 upregulates the expression of SOX1. DMH-1 increases cardiomyocyte progenitor cells and promotes the differentiation of mouse embryonic stem cells into cardiomyocytes. DMH-1 induces the differentiation of hiPSC-derived neural progenitor cells into β3-tubulin-positive neurons. -
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Dexamethasone phosphate disodium
0 ImagesDexamethasone phosphate (Dexamethasone 21-phosphate) disodium is a prodrug form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone phosphate disodium is produced by introducing a phosphate ester group at the 21-position of the Dexamethasone molecule, forming a salt with sodium ions, thereby significantly improving water solubility. Dexamethasone phosphate disodium inhibits LPS (HY-D1056)-induced degradation of IRAK-1 and IRAK-4, and blocks LPS-induced activation of TRAF6, p-TAK1 and p-JNK. Dexamethasone phosphate disodium inhibits the secretion of RANTES, TGF-β1 and NO, promotes the production of MIP-1α and IL-10, and blocks microglial migration. Dexamethasone phosphate disodium is almost completely converted to Dexamethasone in rat blood, and supports transdermal delivery via iontophoresis. Dexamethasone phosphate disodium can be used in research related to steroid-dependent ulcerative colitis, chemotherapy-induced vomiting, allergic asthma and acute colitis (inflammatory bowel disease). -
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- SB 525334
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LY2109761
0 ImagesLY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively. -
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LDN193189 dihydrochloride
0 ImagesSynonyms: DM-3189 dihydrochlorideLDN193189 (DM-3189) dihydrochloride 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. -
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Ponsegromab
0 ImagesSynonyms: PF 06946860Ponsegromab is a Growth differentiation factor 15 (GDF15) inhibitor with human, cynomolgus monkey, and mouse target IC50 values of 0.123 nM, 0.053 nM, and 0.102 nM, respectively. Ponsegromab acts as a chemosensitizer, increases intracellular reactive oxygen species, reduces glutathione levels. Ponsegromab can be used for the research of oxaliplatin-resistant colorectal cancer. -
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Vactosertib
0 ImagesSynonyms: EW-7197; TEW-7197Vactosertib (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib has potently antimetastatic activity and anticancer effect. -
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LDN193189 Tetrahydrochloride
0 ImagesSynonyms: DM-3189 TetrahydrochlorideLDN193189 (DM-3189) Tetrahydrochloride 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. -
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LSKL, Inhibitor of Thrombospondin (TSP-1)
0 ImagesLSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) 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) can readily crosse the blood-brain barrier. -
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