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 (104):

Cat. No. Product Name Effect Purity
  • HY-10431
    SB-431542 Inhibitor 99.89%
    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 dihydrochloride (BML-275 dihydrochloride; Compound C dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM[1]. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride induces autophagy[2].
  • 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 induces autophagy[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-13226
    Galunisertib Inhibitor 99.95%
    Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
  • HY-P99944
    SHR-1701
    SHR-1701 (Retlirafusp alfa) is a bifunctional fusion protein targeting PD-L1 and TGF-β for cancer research[1].
  • HY-P99839
    Dalantercept Inhibitor
    Dalantercept (ACE-041) is an activin receptor like kinase 1 (ALK1) inhibitor, a ligand trap for bone morphogenetic proteins (BMP) 9 and BMP 10. Dalantercept reduces tumor angiogenesis and delays tumor growth by binding to BMP 9 and BMP 10. As an anti angiogenic agent, Dalantercept has potential applications in persistent or recurrent ovarian cancer, renal cell carcinoma (RCC), and related malignant tumors[1][2][3][4].
  • HY-P99748
    Nadecnemab Inhibitor
    Nadecnemab is an IgG4κ antibody targeting to GFRA3, glial cell derived neurotrophic factor family receptor alpha 3. Nadecnemab can be used for research of osteoarthritis of the knee/pain[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-146693
    CJJ300 Inhibitor
    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 99.69%
    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-10432A
    A 83-01 sodium Inhibitor
    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
    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
  • HY-10326
    GW788388 Inhibitor 99.92%
    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.
  • HY-P3642
    Gp100:209-217 Inhibitor
    Gp100:209-217 is a gp 100-derived human CTL epitope presented by HLA-A2. Gp100:209-217 is a polypeptide containing eight amino acids. Gp100:209-217 is a potent TGF-β inhibitor and blocks TGF-β signaling pathway[1].
  • HY-P2294
    pm26TGF-β1 peptide
    pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction[1][2].
  • HY-118810
    BIO-013077-01 Inhibitor 98.16%
    BIO-013077-01 is a pyrazole TGF-β inhibitor[1].
  • HY-12071A
    LDN193189 Tetrahydrochloride Inhibitor 98.04%
    LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM)[1].
  • HY-144043
    ALK5-IN-8 Inhibitor
    ALK5-IN-8 is a potent inhibitor of TGFβRI (ALK5). ALK5-IN-8 Inhibits the phosphorylation of ALK5 on its downstream signaling proteins (Smad2 or Smad3) by blocking the binding of TGFβRI to ligands, thereby affecting or blocking TGF-β signaling. ALK5-IN-8 has the potential for the research of various ALK5-mediated related diseases (extracted from patent WO2021190425A1, compound 1)[1].