- 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
(219)
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ALK1
(9)
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ALK2
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ALK3
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ALK4
(10)
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ALK5
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ALK6
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ALK7
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TGFβR2
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ACVR2A
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ACVR2B
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BMP
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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
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TGF-β Receptor Degraders
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TGF-β Receptor Controls
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TGF-beta Receptor Proteins
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ALK-3 Proteins
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ALK-6 Proteins
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BMP Type II Receptor (BMPR2) Proteins
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ALK-2/ACVR1 Proteins
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ALK-4/Activin RIB Proteins
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ALK-7 Proteins
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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
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Anti-Muellerian Hormone Type-2 Receptor (AMHR2) Proteins
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TGF-β Receptor 1 Proteins
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TGF-beta Receptor 2 Proteins
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Type III TGF-β Receptor Proteins
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ALK-3/CD292 Proteins
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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
- ALK2-IN-2
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TGFβRI-IN-3
0 ImagesTGFβRI-IN-3 inhibits TGFβR1 at an IC50 of 0.79 nM with 2000-fold selectivity against MAP4K4. TGFβRI-IN-3 represents a highly selective TGFβR1 inhibitor that has potential applications in immuno-oncology. -
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- Itacnosertib
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BMS-986260
0 ImagesBMS-986260, an immuno-oncology agent, is a potent, selective, and orally active TGFβR1 inhibitor (IC50=1.6 nM). BMS-986260 displays exquisite selectivity for TGFβR1 over its isozyme TGFβR2, as well as in a panel of more than 200 kinases examined. BMS-986260 inhibits TGFβ mediated nuclear translocation of pSMAD2/3 in MINK and NHLF cells lines with an IC50 of 350 nM and 190 nM, respectively. -
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H-Tyr-Ile-Gly-Ser-Arg-NH2
0 ImagesH-Tyr-Ile-Gly-Ser-Arg-NH2 is a hexapeptide that is an essential fragment of laminin responsible for efficient cell adhesion and receptor binding. H-Tyr-Ile-Gly-Ser-Arg-NH2 promotes various epithelial cell adhesion activities. -
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- AZ12799734
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Meloside A
0 ImagesSynonyms: Isovitexin 2''-O-glucoside; Isovitexin 2''-O-β-D-glucosideMeloside A (Isovitexin 2''-O-glucoside) is a flavonoid with antioxidant activity. Meloside A can inhibit cell apoptosis and ROS production. Meloside A can inhibit androgen receptor (AR) nuclear translocation and AR protein expression. Meloside A can reduce IL-6, TGF-β1 and DKK-1 levels. Meloside A can be used for the researches of inflammation and endocrinology, such as hair loss. -
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GFH018
0 ImagesGFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC50 of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer, breast cancer, and relapsed/metastatic nasopharyngeal carcinoma. -
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Clonixin
0 ImagesSynonyms: SCH-10304Clonixin (SCH-10304) 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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Dexamethasone phosphate disodium (Standard)
0 ImagesSynonyms: Dexamethasone 21-phosphate disodium (Standard)Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium (Standard) is the analytical standard of Dexamethasone phosphate disodium (HY-B1829A). This product is intended for research and analytical applications. Dexamethasone 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-505124 hydrochloride
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Murlentamab
0 ImagesCat. No.: HY-P99746CAS No.: 2058047-65-5Synonyms: 3C23K; GM102Murlentamab (3C23K; GM102) is a humanized anti-AMHRII antibody. AMHRII is the anti-Müllerian hormone receptor. Murlentama significantly promotes macrophage-mediated antibody-dependent cell-mediated cytotoxicity (ADCC). Murlentama stimulates pro-inflammatory and anti-tumor internal environment, recruits and activates T cells. Murlentama suppresses tumors growth by inducing naïve macrophage orientation and promoting tumor-associated macrophage (TAM) reprogramming. -
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Nisevokitug
0 ImagesCat. No.: HY-P990009CAS No.: 2649854-92-0Synonyms: NIS-793Nisevokitug (NIS-793) is a humanized IgG2λ monoclonal antibody and an inhibitor of the TGF-β signaling pathway. Nisevokitug blocks the binding of TGF-β to the membrane-bound TGF-βR1/TGF-βR2 receptors, inhibits both Smad-dependent and Smad-independent downstream cascade signaling, downregulates fibrosis-related genes, and reverses the TGF-β-mediated immunosuppressive microenvironment. Nisevokitug can be used in the research of diseases such as pancreatic ductal adenocarcinoma, colorectal cancer, myelofibrosis, and myelodysplastic syndrome. -
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HYL001
0 ImagesHYL001 (compund 338) is a potent inhibitor of TGFβ receptor 1 (ALK5) that is approximately 9 times more potent than the structurally related compound Galunisertib (HY-13226) and is able to eliminate liver metastases established in mice. -
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M4K-2009
0 ImagesM4K2009 is an orally active, blood-brain barrier permeable type I ALK2 inhibitor, with an IC50 value of 8-13 nM against human ALK2. M4K2009 exhibits moderate off-target inhibitory activity against hERG potassium channels (Potassium Channel), with an IC50 of 8 μM against the human channel. M4K2009 can be used in studies related to diffuse intrinsic pontine glioma. -
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Bakkenolide A
0 ImagesBakkenolide A is an anticancer agent. Bakkenolide A reduces the viability of leukemia cells, inhibits cell colony formation and invasion, and downregulates the expression of HDAC3 in cells. Bakkenolide A downregulates the expression of pro-inflammatory cytokines including TNF-α, interleukins such as IL-1β, TGF-β1 and IFN-γ, as well as the expression of PI3K, PDK and PKC in leukemia cells. Bakkenolide A downregulates activated Akt, GSK and Bad, while upregulates Cyto-c, cleaved Caspase3 and cleaved Caspase7, induces apoptosis (apoptosis) in leukemia cells and thereby inhibits inflammatory responses in leukemia cells. Bakkenolide A significantly slows the growth of subcutaneous leukemia tumors in nude mice. Bakkenolide A is applicable to leukemia-related research. -
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- TP-008
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- TGF-βRI inhibitor 3
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Anti-ACVR2A Antibody (Ab-14E1)
0 ImagesCat. No.: HY-P990326Synonyms: Ab-14E1Anti-ACVR2A Antibody (Ab-14E1) is a CHO-expressed human antibody that targets ACVR2A. Anti-ACVR2A Antibody (Ab-14E1) features an IgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for Anti-ACVR2A Antibody (Ab-14E1) can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001). -
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TP0427736 hydrochloride
0 ImagesTP0427736 hydrochloride is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50=836 nM). TP0427736 hydrochloride also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. TP0427736 hydrochloride can be used for the research of androgenic alopecia (AGA). -
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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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