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

TGF-β Receptor

Transforming growth factor beta receptors

TGF-β Receptor

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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-12071G
    LDN193189 (GMP)
    		Inhibitor
    LDN193189 (DM-3189) (GMP) is LDN193189 (HY-12071) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. LDN193189 is selective BMP type I receptor inhibitor.
    LDN193189 (GMP)
  • HY-145608
    Zilurgisertib
    		Inhibitor 98.25%
    Zilurgisertib (INCB-000928; NBU-928) is a selective ALK2 inhibitor with an IC50 value of 15 nM. Zilurgisertib inhibits SMAD1/5 phosphorylation with an IC50 value of 63 nM. Zilurgisertib inhibits hepcidin production and improve anemia. Zilurgisertib can be used in melanoma research.
    Zilurgisertib
  • HY-109179
    Itacnosertib
    		Inhibitor 99.06%
    Itacnosertib (TP-0184) is the inhibitor for FLT3, ACVR1 (ALK2, IC50=8 nM) and JAK2 (IC50=8540 nM). Itacnosertib exhibits anti-leukemic activity.
    Itacnosertib
  • HY-N2263
    Skimmin
    		99.64%
    Skimmin (Umbelliferone glucoside) is a major pharmacologically active and orally active molecule present in Hydrangea paniculata, a medical herb used in traditional Chinese medicine as an anti-inflammatory agent. Skimmin has renal protective activity. Skimmin can improve creatinine clearance, and reduce plasma creatinine, and kidney injuries. Skimmin has good anti-amoebic activity against the HM1:IMMS strain of Entamoeba histolytica. Skimmin has anti-cancer and neuroprotective activities. Skimmin reduces cardiac fibrosis as well as decreasing TNF-α, IL-6, IL1β, and TGFβ1 in cardiac tissues. Skimmin can be studied in research for diabetes and diabetes-related diseases.
    Skimmin
  • HY-N5124
    Meloside A
    		Inhibitor 98.55%
    Meloside A (Isovitexin 2''-O-glucoside) is a phenylpropanoid found in barley 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.
    Meloside A
  • HY-112815
    ALK2-IN-2
    		Inhibitor 99.93%
    ALK2-IN-2 is an orally active and selective inhibitor of ALK2 (ACVR1), with an IC50 value of 9 nM, and over 700-fold selectivity against ALK3. ALK2-IN-2 can inhibit oxidative stress and protect endothelial cells.
    ALK2-IN-2
  • HY-122856
    AZ12601011
    		Inhibitor 99.78%
    AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
    AZ12601011
  • HY-P99944
    SHR-1701
    		99.77%
    SHR-1701 (Retlirafusp alfa) is a bifunctional fusion protein targeting PD-L1 and TGF-β for cancer research.
    SHR-1701
  • HY-113604
    Pentabromopseudilin
    		Inhibitor 99.63%
    Pentabromopseudilin (PBrP) is a marine antibiotic isolated from the marine bacteria Pseudomonas bromoutilis and Alteromonas luteoviolaceus. PBrP exhibits antimicrobial, anti-tumour and phytotoxic activities. PBrP is a reversible and allosteric inhibitor of myosin Va (MyoVa). PBrP also is a potent inhibitor of transforming growth factor-β (TGF-β) activity. PBrP can be used for the research of fibrotic diseases and cancer.
    Pentabromopseudilin
  • HY-141645
    IMM-H007
    		Antagonist
    IMM-H007 (WS070117) is an orally active and potent AMPK (AMP-activated protein kinase) activator and TGFβ1 (transforming growth factor β1) antagonist. IMM-H007 has protective effects in cardiovascular diseases via activation of AMPK. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 degradation. IMM-H007 resolves hepatic steatosis in HFD-fed hamsters by the regulation of lipid metabolism. IMM-H007 can be used for the research of nonalcoholic fatty liver disease (NAFLD) and inflammatory atherosclerosis.
    IMM-H007
  • HY-125851
    TP-008
    		Inhibitor 99.42%
    TP-008, a chemical probe, is a potent, selective and orally active (Activin-Like Kinase 5) ALK5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose.
    TP-008
  • HY-78349
    A 77-01
    		Inhibitor 99.92%
    A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM.
    A 77-01
  • HY-15472
    PRX-08066
    		Inhibitor
    PRX-08066 is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki of 3.4 nM. PRX-08066 inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 inhibits pulmonary vascular remodeling. PRX-08066 can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET).
    PRX-08066
  • HY-P4651
    H-Tyr-Ile-Gly-Ser-Arg-NH2
    		Inhibitor 98.27%
    H-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.
    H-Tyr-Ile-Gly-Ser-Arg-NH2
  • HY-168990
    Ontunisertib
    		Inhibitor 99.95%
    Ontunisertib (Example 26) is an inhibitor of TGFβ receptor I/ALK5 (TGFβRI/ALK5), with IC50 values ranging from 100 to 500 nM for TGFβRI and an IC50 value of ≤100 nM for ALK5. Ontunisertib can be used in research on gastrointestinal diseases, as well as diseases and cancers related to fibrotic conditions in the skin and eyes.
    Ontunisertib
  • HY-10327
    GW-6604
    		Inhibitor 98.0%
    GW-6604 is an ALK5 inhibitor with an IC50 value of 140 nM for inhibiting its autophosphorylation, and can be used in the study of liver fibrosis.
    GW-6604
  • HY-P2294A
    pm26TGF-β1 peptide TFA
    		99.68%
    pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.
    pm26TGF-β1 peptide TFA
  • HY-128437
    TGFβ-IN-5
    		Inhibitor 98.03%
    TGFβ-IN-5(Compd 12) is a TGFβ inhibitor useful for the study of fibroproliferative diseases associated with TGF-β signaling.
    TGFβ-IN-5
  • HY-N2589
    Isosaponarin
    		Activator 99.59%
    Isosaponarin is a flavone glycoside isolated from wasabi leaves. Isosaponarin is a P4HA2 enzymatic agonist. Isosaponarin increases collagen synthesis via up-regulated TGF-β type II receptor (TβR-II) and prolyl 4-hydroxylase (P4H) proteins production, promoting skin health and wound healing. Isosaponarin-rich plants exhibit strong antimicrobial, antioxidant, anti-hyaluronidase, antiplatelet, anti-atopic dermatitis, and anti-tumor effects.
    Isosaponarin
  • HY-136773A
    KER047 succinate
    		Inhibitor 98.93%
    KER047 succinate (ALK2-IN-4 succinate) is a potent activin receptor-like kinase-2 (ALK2) inhibitor. KER047 succinate can be used for the research of metabolic disease, such as fibrodysplasia ossificans progressiva (FOP).
    KER047 succinate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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