2. TGF-beta/Smad
  3. TGF-β Receptor

TGF-β Receptor

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 Related Products (185):

Cat. No. Product Name Effect Purity
  • HY-10431
    SB-431542 Inhibitor 99.85%
    SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitory activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways[1][2][3].
  • HY-13418
    Dorsomorphin dihydrochloride Inhibitor 99.91%
    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).
  • HY-12071
    LDN193189 Inhibitor 99.48%
    LDN193189 is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva[1][2][3].
  • HY-13418A
    Dorsomorphin Inhibitor
    Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599)[1][2].
  • HY-10432
    A 83-01 Inhibitor
    A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively[1].
  • HY-P991158
    Rinvatercept
    Rinvatercept, a fusion protein, is a glycyl (1)-chimeric N-terminal (1-108)-peptide (2-109) combined from the sequences of the extracellular domains of the human ACVR2A/B, and is fused via a G3 peptide linker (110-112) to an immunoglobulin G1 (IgG1) Fc fragment. Rinvatercept can be used for research of neuromuscular disease[1].
  • HY-172108
    TGFβRI-IN-7 Inhibitor
    TGFβRI-IN-7 (compound 16W) is a potent inhibitor of TGFβRI. TGFβRI-IN-7 inhibits SMAD2/3 phosphorylation and H22 cell viability with IC50 values of 12 and 65 nM, respectively. TGFβRI-IN-7 shows anti-tumor efficacy in a xenograft model of H22 cells, with TGI of 79.6 %[1].
  • HY-170227
    Autotaxin-IN-7 Inhibitor
    Autotaxin-IN-7 (45), a pyridine-2-carboxylic derivative, demonstrates subnanomolar ATX inhibition (IC50 = 0.086 nM), with a favorable heart safety profile (hERG > 30 μM) and minimal fibroblast toxicity. Autotaxin-IN-7 (45) suppresses the TGF-β/Smad signaling pathway, downregulating α-smooth muscle actin (α-SMA) and extracellular matrix components (ECM). Autotaxin-IN-7 (45) is used in the research for pulmonary fibrosis[1].
  • HY-W107024
    BMS-986260 Inhibitor
    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[1].
  • HY-B1260
    Cetrimonium bromide
    Cetrimonium bromide (CTAB), a quaternary ammonium, is an orally active cationic surfaetant. Cetrimonium bromide has toxicity and anticancer effect. Cetrimonium bromide inhibits cell migration and invasion through modulating the canonical and non-canonical TGF-β signaling pathways. Cetrimonium bromide can be used for DNA extraction[1][2][3][4].
  • HY-RS14445
    Tgfbr1 Mouse Pre-designed siRNA Set A Inhibitor

    Tgfbr1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Tgfbr1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

  • HY-P990107
    Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) Inhibitor
    Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) is an anti-mouse/human/rat/monkey/hamster/canine/bovine IgG antibody inhibitor of TGF-β[1]. The recommend isotype control of Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8): Mouse IgG1 kappa, Isotype Control (HY-P99977).
  • HY-P3972
    H-ILE-ARG-VAL-VAL-MET-OH
    H-ILE-ARG-VAL-VAL-MET-OH is a pentapeptide from C7 with a domain that supports cell attachment. H-ILE-ARG-VAL-VAL-MET-OH is also the sequence fragment that binds to the thrombospondin-1 (TS1) receptor[1][2].
  • HY-146693
    CJJ300 Inhibitor 99.77%
    CJJ300 is a transforming growth factor-β (TGF-β) inhibitor with an IC50 of 5.3 µM. CJJ300 inhibits TGF-β signaling by disrupting the formation of the TGF-β-TβR-I-TβR-II signaling complex[1].
  • HY-137506
    XST-14 Inhibitor 99.26%
    XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects[1].
  • HY-100167
    TAK-778 Agonist
    TAK-778 is a derivative of ipriflavone and has been shown to induce bone growth in in vitro and in vivo models.
  • HY-118528
    TP0427736 Inhibitor
    TP0427736 is a selective inhibitor of ALK5 with an IC50 of 2.72 nM. TP0427736 inhibits Smad2/3 phosphorylation in A549 cells. TP0427736 decreases the growth inhibition of human outer root sheath cells[1].
  • HY-10432A
    A 83-01 sodium Inhibitor 98.43%
    A 83-01 sodium is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively[1].
  • HY-150793
    SY-LB-57 Agonist 99.26%
    SY-LB-57 is a highly potent bone morphogenetic protein (BMP) receptor signaling agonist. SY-LB-57 can be used in studies of diseases such as fractures and pulmonary arterial hypertension[1].
  • HY-112864
    TGFβRI-IN-6 Inhibitor