2. Signaling Pathways
  3. TGF-beta/Smad
  4. TGF-β Receptor

TGF-β Receptor

Transforming growth factor beta receptors

TGF-β Receptor

Related Products

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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-10326R
    GW788388 (Standard)
    		Inhibitor
    GW788388 (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.
    GW788388 (Standard)
  • HY-W684904
    LY550410
    		Inhibitor
    LY550410 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.
    LY550410
  • HY-100113R
    Buloxibutid (Standard)
    		Inhibitor
    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.
    Buloxibutid (Standard)
  • HY-103021R
    LY3200882 (Standard)
    		Inhibitor
    LY3200882 (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.
    LY3200882 (Standard)
  • HY-123409
    Nicousamide
    		Inhibitor
    Nicousamide is a potent inhibitor of TGF-β RII phosphorylation. Nicousamide can be used to study renal fibrosis in animal models of diabetic nephropathy.
    Nicousamide
  • HY-11103R
    Sitaxsentan sodium (Standard)
    		Activator
    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.
    Sitaxsentan sodium (Standard)
  • HY-121235R
    Clonixin (Standard)
    		Inhibitor
    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.
    Clonixin (Standard)
  • HY-185185
    S58 aptamer
    		Inhibitor
    S58 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.
    S58 aptamer
  • HY-18758R
    IN-1130 (Standard)
    		Inhibitor
    IN-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.
    IN-1130 (Standard)
  • HY-13521AR
    SB-505124 hydrochloride (Standard)
    		Inhibitor
    SB-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.
    SB-505124 hydrochloride (Standard)
  • HY-B1829R
    Dexamethasone phosphate (Standard)
    		Inhibitor
    Dexamethasone 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).
    Dexamethasone phosphate (Standard)
  • HY-13521R
    SB-505124 (Standard)
    		Inhibitor
    SB-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.
    SB-505124 (Standard)
  • HY-10591R
    Neuropathiazol (Standard)
    Neuropathiazol (Standard) is the analytical standard of Neuropathiazol (HY-10591). This product is intended for research and analytical applications. Neuropathiazol, a neuronal differentiation inducer, selectively induces neuronal differentiation of multipotent hippocampal neural progenitor cells.
    Neuropathiazol (Standard)
  • HY-12071AR
    LDN193189 Tetrahydrochloride (Standard)
    		Inhibitor
    LDN193189 (DM-3189) Tetrahydrochloride (Standard) is the analytical standard of LDN193189 Tetrahydrochloride (HY-12071A). This product is intended for research and analytical applications. LDN193189 (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.
    LDN193189 Tetrahydrochloride (Standard)
  • HY-13418R
    Dorsomorphin dihydrochloride (Standard)
    		Inhibitor
    Dorsomorphin (dihydrochloride) (Standard) is the analytical standard of Dorsomorphin (dihydrochloride). This product is intended for research and analytical applications. Dorsomorphin (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).
    Dorsomorphin dihydrochloride (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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