- 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
(215)
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ALK1
(9)
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ALK2
(31)
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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
(6)
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ACVR2A
(5)
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ACVR2B
(3)
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BMP
(1)
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GDF15
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All Product Categories
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TGF-β Receptor Inhibitors
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TGF-β Receptor Agonists
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TGF-β Receptor Antagonists
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TGF-β Receptor Activators
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TGF-β Receptor Modulators
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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
(7)
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TGF-beta Receptor 2 Proteins
(13)
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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 (346)
Related Products (346)
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Recombinant Proteins (98)
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Antibodies (16)
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TGF-β Receptor Isoform Comparison
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TJN-331
0 ImagesCat. No.: HY-178850CAS No.: 219964-53-1TJN-331 is a potent and orally active TGF-β1 Inhibitor. TJN-331 ameliorates anti-glomerular basement membrane (GBM) nephritis in rats by inhibitng TGF-β1 production, thereby reducing extracapillary proliferation in glomeruli. TJN-331 inhibits mesangial expansion in experimental IgA nephropathy in ddY mice. TJN-331 can be used for the research of nephritis and IgA nephropathy. -
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ALK5-IN-6
0 ImagesCat. No.: HY-142950CAS No.: 2657720-04-0ALK5-IN-6 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-6 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 1). -
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TGFβRI-IN-4
0 ImagesCat. No.: HY-146780CAS No.: 2421135-03-5TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC50s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model. -
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TP0427736
0 ImagesCat. No.: HY-118528CAS No.: 864374-00-5TP0427736 is a selective inhibitor of ALK5 with an IC50 of 2.72 nM. TP0427736 inhibits Smad2/3 phosphorylation in A549 cells. TP0427736 decreases the growth inhibition of human outer root sheath cells. -
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HCTZ-CH2-HCTZ
0 ImagesCat. No.: HY-Z8643CAS No.: 402824-96-8HCTZ-CH2-HCTZ is an isomer of HCTZ (HY-B0252). Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. -
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(+)-ITD-1
0 ImagesCat. No.: HY-137063CAS No.: 1409968-46-2(+)-ITD-1 is an inhibitor for TGF-β, that inhibits the TGF-β2 with an IC50 of 0.46 μM. (+)-ITD-1 promotes the degradation of TGF-b type II receptor (TGFBR2) and the differentiation of cardiomyocyte, and inhibits the mesoderm formation in the early differentiation stage of mouse embryonic stem cells (mESCs). -
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DMH-1 (GMP)
0 ImagesCat. No.: HY-12273GCAS No.: 1206711-16-1DMH-1 (GMP) is GMP grade DMH-1 (HY-12273). DMH-1 (GMP) is a selective BMP inhibitor. DMH-1 (GMP) upregulates the expression of SOX1. DMH-1 (GMP) increases cardiomyocyte progenitor cells and promotes the differentiation of mouse embryonic stem cells into cardiomyocytes. DMH-1 (GMP) induces the differentiation of hiPSC-derived neural progenitor cells into β3-tubulin-positive neurons. -
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Lysyl-phenylalanyl-lysine
0 ImagesCat. No.: HY-165339CAS No.: 54925-87-0Lysyl-phenylalanyl-lysine (Compound KFK) is a tripeptide and belongs to the peptide segments related to thrombospondin-1 (TSP-1) (HY-P0299). Lysyl-phenylalanyl-lysine can activate LAP-TGF-β1 and release active TGF-β1, thereby inhibiting abnormal expression of MMP. Lysyl-phenylalanyl-lysine can be used for research on skin aging-related diseases and poor wound healing. -
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RepSox (Standard)
0 ImagesSynonyms: E-616452 (Standard); SJN 2511 (Standard)RepSox (Standard) is the analytical standard of RepSox. This product is intended for research and analytical applications. RepSox (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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CDD-1281
0 ImagesCat. No.: HY-171247CAS No.: 3034215-91-0CDD-1281 is a highly potent and selective BMPR2 kinase inhibitor with an IC50 of 1.2 nM. CDD-1281 can effectively inhibit BMP-mediated gene expression. -
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LY2109761 (Standard)
0 ImagesLY2109761 (Standard) is the analytical standard of LY2109761. This product is intended for research and analytical applications. LY2109761 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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Gdf15 Rat Pre-designed siRNA Set A
0 ImagesCat. No.: HY-RS22974 -
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ALK5-IN-82
0 ImagesCat. No.: HY-162902CAS No.: 3001361-04-9ALK5-IN-82 is a potent and selective inhibitor against activin receptor-like kinase 5 (ALK5) with an IC50 value of 9.1 nM. ALK5-IN-82 inhibits the protein expression of α-smooth muscle actin (α-SMA), collagen I and tissue inhibitor of metalloproteinase 1 (TIMP-1)/matrix metalloproteinase 13 (MMP-13) in transforming growth factor-β-induced human umbilical vein endothelial cells. ALK5-IN-82 is promising for research of cardiac fibrosis. -
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L-Seryl-L-leucyl-L-leucyl-L-lysine
0 ImagesCat. No.: HY-W928653CAS No.: 464924-27-4Synonyms: SLLKL-Seryl-L-leucyl-L-leucyl-L-lysine (SLLK) is the control peptide for LSKL (HY-P0299). -
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NCX 466
0 ImagesCat. No.: HY-103388CAS No.: 1262956-64-8NCX 466 is an orally active COX-1 and COX-2 inhibitor that exhibits anti-inflammatory and analgesic effects. Additionally, NCX 466 acts as a NO donor, exerting anti-inflammatory and antioxidant effects by improving microcirculation. NCX 466 significantly reduces the levels of transforming growth factor-β (TGF-β) and oxidative stress markers (such as thiobarbituric acid reactive substances (TBARS) and 8-hydroxy-2'-deoxyguanosine (8-OHdG)), and it decreases leukocyte recruitment during inflammation by reducing myeloperoxidase (MPO) activity, thereby preventing bleomycin (HY-108345)-induced pulmonary fibrosis in mice. -
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LDN193189 dihydrochloride (Standard)
0 ImagesSynonyms: DM-3189 dihydrochloride (Standard)LDN193189 (DM-3189) dihydrochloride (Standard) is the analytical standard of LDN193189 dihydrochloride (HY-12071B). This product is intended for research and analytical applications. LDN193189 (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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- SD-208 (Standard)
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Sitaxsentan-13C6
0 ImagesCat. No.: HY-76520SSynonyms: IPI 1040-13C6 ; TBC-11251-13C6Sitaxsentan-13C6 (IPI 1040-13C6) is 13C labeled Sitaxsentan (HY-76520). Sitaxsentan (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension. -
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Nuvisertib (Standard)
0 ImagesSynonyms: TP-3654 (Standard)Nuvisertib (Standard) (TP-3654 (Standard)) is the analytical standard of Nuvisertib (HY-101126). This product is intended for research and analytical applications. Nuvisertib (TP-3654) is an orally active second-generation pan-PIM kinase inhibitor with Ki values of 5 nM, 239 nM, and 42 nM against PIM-1, PIM-2, and PIM-3, respectively. Nuvisertib inhibits JAK-independent inflammatory and survival signaling pathways, reduces the production of proinflammatory cytokines, restores apoptotic sensitivity, inhibits mTORC1, MYC, and TGF-β signaling pathways, and decreases the expression of fibrosis markers. Nuvisertib selectively impairs the transport function of ABCG2, resensitizes multidrug-resistant cancer cells to cytotoxic drugs, and overcomes JAK2 inhibitor resistance. Nuvisertib can be used in research related to myelofibrosis, renal cell carcinoma, multidrug-resistant cancer, advanced solid tumors, urothelial carcinoma, and prostate adenocarcinoma. -
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Arecaidine hydrochloride (Standard)
0 ImagesCat. No.: HY-N2368ARCAS No.: 6018-28-6Arecaidine hydrochloride (Standard) is the analytical standard of Arecaidine hydrochloride (HY-N2368A). This product is intended for research and analytical applications. Arecaidine hydrochloride is a GABA transport system inhibitor. Arecaidine hydrochloride inhibits the proliferation of oral mucosal fibroblasts, increases the secretion of IL-6, TGF-β and TNF-α in cells, downregulates the expression of PPAR-γ and PCK1 in cells, and upregulates the expression of TGF-β1. Arecaidine hydrochloride inhibits the uptake of γ-aminobutyric acid and β-alanine by the central nervous system of cats. Arecaidine hydrochloride inhibits hPAT1-mediated L-[3H]proline uptake in cells. Arecaidine hydrochloride can be used in research related to neurological diseases. -
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