- 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
(221)
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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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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
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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 (352)
Related Products (352)
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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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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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GW-6604 (Standard)
0 ImagesCat. No.: HY-10327RCAS No.: 452342-37-9 -
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GW788388 (Standard)
0 ImagesCat. No.: HY-10326RCAS No.: 452342-67-5GW788388 (Standard) is the analytical standard of GW788388 (HY-10326). This product is intended for research and analytical applications. 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. -
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LY550410
0 ImagesCat. No.: HY-W684904CAS No.: 737791-20-7LY550410 is a small-molecule ATP-competitive inhibitor against type I TGF-β receptor kinase, which contains heteroaryl rings for potent binding to the kinase-domain active site. LY550410 modulates TGF-β signalling, thereby regulates gene expression and ultimately cell growth. LY550410 is promising for research of cancers. -
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Buloxibutid (Standard)
0 ImagesCat. No.: HY-100113RCAS No.: 477775-14-7Synonyms: AT2 receptor agonist C21 (Standard)Buloxibutid (AT2 receptor agonist C21) (Standard) is the analytical standard of Buloxibutid (HY-100113). This product is intended for research and analytical applications. Buloxibutid is an orally active, selective angiotensin II type 2 receptor (AT2R) agonist, with a Ki value of 0.4 nM for porcine AT2R. Buloxibutid exerts effects such as vasodilation, anti-inflammation, anti-fibrosis (promoting the expression of collagenase MMP-13) and tissue repair mainly by activating the NO/cGMP pathway, inhibiting the pro-proliferative MAPK signaling, and suppressing the pro-fibrotic TGF-β/Smad pathway as well as the inflammatory NF-κB pathway. Buloxibutid can be used in research related to idiopathic pulmonary fibrosis, hypertension, and systemic sclerosis. -
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LY3200882 (Standard)
0 ImagesCat. No.: HY-103021RCAS No.: 1898283-02-7LY3200882 (Standard) is the analytical standard of LY3200882 (HY-103021). This product is intended for research and analytical applications. 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. -
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Nicousamide
0 ImagesCat. No.: HY-123409CAS No.: 704881-43-6Nicousamide is a potent inhibitor of TGF-β RII phosphorylation. Nicousamide can be used to study renal fibrosis in animal models of diabetic nephropathy. -
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SM 16 (Standard)
0 ImagesCat. No.: HY-111482RCAS No.: 614749-78-9 -
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Sitaxsentan sodium (Standard)
0 ImagesSynonyms: IPI 1040 sodium (Standard); TBC11251 sodium (Standard)Sitaxsentan (sodium) (Standard) is the analytical standard of Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) (HY-11103). This product is intended for research and analytical applications. Sitaxsentan 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 sodium exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan sodium is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan sodium can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension. -
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Clonixin (Standard)
0 ImagesSynonyms: SCH-10304 (Standard)Clonixin (SCH-10304) (Standard) is the analytical standard of Clonixin. This product is intended for research and analytical applications. Clonixin is an orally active non-steroidal anti-inflammatory agent (NSAID) that inhibits COX synthesis. Clonixin acts as a voltage-gated L-type calcium channel blocker, exerts vasodilatory effects by antagonizing Ca2+ in vascular smooth muscle. Clonixin inhibits TGF-β, reduces lung coefficient, immune cell infiltration level, oxidative stress response, airway resistance, hydroxyproline content and collagen deposition. Clonixin can be used in research related to inflammation such as idiopathic pulmonary fibrosis and moderate to severe pain. -
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S58 aptamer
0 ImagesCat. No.: HY-185185S58 aptamer is a ssDNA aptamer targeting transforming growth factor-beta receptor II (TGF-β RII). S58 aptamer inhibits the TGF-β RII interaction with TGF-β. S58 aptamer effectively improves glaucoma filtration surgery (GFS) surgical outcomes by activating the intracellular antioxidant defense PI3K/Akt/Nrf2 signaling pathway. -
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IN-1130 (Standard)
0 ImagesIN-1130 (Standard) is the analytical standard of IN-1130. This product is intended for research and analytical applications. IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis. -
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Suberic acid (Standard)
0 ImagesCat. No.: HY-W015300RCAS No.: 505-48-6Synonyms: Octanedioic acid (Standard)Suberic acid (Standard) is the analytical standard of Suberic acid. This product is intended for research and analytical applications. Suberic acid is an orally active crystalline dibasic acid. Suberic acid activates the Akt signaling pathway and regulates the expression of molecules related to the TGF-β and MAPK signaling pathways. Suberic acid inhibits skin dryness. -
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Cilengitide hydrochloride
0 ImagesCat. No.: HY-16142CAS No.: 188969-00-8Synonyms: EMD 121974 hydrochlorideCilengitide hydrochloride (EMD 121974 hydrochloride) is an integrin (integrin) inhibitor with blood-brain barrier permeability, with IC50 values against human targets as follows: 0.61 nM for αvβ3, 8.4 nM for αvβ5, 14.9 nM for α5β1, 5400 nM for αIIbβ3, 2050 nM for αvβ6, 2350 nM for αvβ8. Cilengitide hydrochloride inhibits the binding of integrins to vitronectin, fibronectin, fibrinogen and LAP (TGF-β), and serves as an internal standard for solid-phase integrin binding assays. Cilengitide hydrochloride inhibits tumor cell viability, induces apoptosis, reduces the phosphorylation levels of STAT3, AKT and mTOR, downregulates the expression of PD-L1, inhibits cell viability and angiogenesis, regulates anti-tumor immune responses and slows tumor growth. Cilengitide hydrochloride can be used in research related to glioblastoma, melanoma, advanced solid tumors and refractory brain tumors. -
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SB-505124 hydrochloride (Standard)
0 ImagesCat. No.: HY-13521ARCAS No.: 356559-13-2SB-505124 (hydrochloride) (Standard) is the analytical standard of SB-505124 (hydrochloride). This product is intended for research and analytical applications. SB-505124 hydrochloride is a selective inhibitor of TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6. -
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LDN193189 (Standard)
0 ImagesCat. No.: HY-12071RCAS No.: 1062368-24-4Synonyms: DM-3189 (Standard)LDN193189 (Standard) is the analytical standard of LDN193189 (HY-12071). This product is intended for research and analytical applications. 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. -
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Dexamethasone phosphate (Standard)
0 ImagesDexamethasone phosphate (Standard) (Dexamethasone 21-phosphate (Standard)) is the analytical standard of Dexamethasone phosphate (HY-B1829). This product is intended for research and analytical applications. Dexamethasone phosphate (Dexamethasone 21-phosphate) is a prodrug form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone phosphate is prepared by introducing a phosphate ester group to the hydroxyl group at position 21 of the Dexamethasone molecule. Dexamethasone phosphate 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 inhibits the secretion of RANTES, TGF-β1 and NO, promotes the production of MIP-1α and IL-10, and blocks microglial migration. Dexamethasone phosphate is almost completely converted to Dexamethasone in rat blood, and supports transdermal delivery via iontophoresis. Dexamethasone phosphate 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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Curcumenol (Standard)
0 ImagesCat. No.: HY-N2259RCAS No.: 19431-84-6Synonyms: (+)-Curcumenol (Standard)Curcumenol (Standard) ((+)-Curcumenol (Standard)) is the analytical standard of Curcumenol (HY-N2259). This product is intended for research and analytical applications. Curcumenol ((+)-Curcumenol) is a natural compound with oral efficacy, exhibiting an IC50 of 12.6 μM and a Ki of 10.8 μM against human CYP3A4. Curcumenol inhibits TNFα-induced phosphorylation/degradation of IκBα, phosphorylation/nuclear translocation of NF-κB p65, as well as the upregulation of MMP3, MMP9, MMP13, TRAF3, IL1RL1, TNFα and IL-1β. Curcumenol suppresses LPS-induced phosphorylation of Akt and p38 MAPK, as well as the production of pro-inflammatory mediators/proteins, and downregulates the SLC7A11/NF-κB/TGF-β pathway. Curcumenol binds to and inhibits the activation of Fyn and Lyn, blocks the function of downstream FcεRI signaling components, and reduces the release of allergic mediators/cytokines. Curcumenol upregulates the expression of KDM6B, and promotes chondrocyte proliferation and cartilage repair. Curcumenol induces ferroptosis and apoptosis, regulates the EMT process, and inhibits tumor growth and metastasis of triple-negative breast cancer. Curcumenol possesses anti-inflammatory, neuroprotective, antioxidant, antitumor, antiviral and hepatoprotective activities. Curcumenol can be used in research related to intervertebral disc degeneration, cancer, inflammation, central nervous system neurodegenerative diseases, allergic reactions and knee osteoarthritis. -
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SB-505124 (Standard)
0 ImagesSB-505124 (Standard) is the analytical standard of SB-505124. This product is intended for research and analytical applications. SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6. -
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Sorry. There is currently no product that acts on isoform Bcl-2, Bcl-W and Bim together.Please
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