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

TGF-β Receptor

Transforming growth factor beta receptors

TGF-β Receptor

Related Products

PDF 0.93 MB

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-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-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-P99588
    Stamulumab
    		Inhibitor
    Stamulumab (MYO-029) is a recombinant human IgG1λ antibody that binds to myostatin and neutralizes its activity by preventing binding to its endogenous high-affinity receptor ActRIIB. Stamulumab leads to muscle fiber hypertrophy and not hyperplasia in SCID mice. Stamulumab has the potential for Becker muscular dystrophy (BMD), facioscapulohumeral dystrophy (FSHD), and limb-girdle muscular dystrophy (LGMD) research.
    Stamulumab
  • 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-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-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-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-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-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-W107024
    BMS-986260
    		Inhibitor 99.95%
    BMS-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.
    BMS-986260
  • 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-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-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
  • HY-109179A
    Itacnosertib hydrochloride
    		Inhibitor 99.43%
    Itacnosertib hydrochloride (TP-0184 hydrochloride) is the inhibitor for FLT3, ACVR1 (ALK2, IC50=8 nM) and JAK2 (IC50=8540 nM). Itacnosertib hydrochloride exhibits anti-leukemic activity.
    Itacnosertib hydrochloride
  • 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-118528A
    TP0427736 hydrochloride
    		Inhibitor 99.22%
    TP0427736 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).
    TP0427736 hydrochloride
  • 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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.