1. Signaling Pathways
  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 Isoform Specific Products:

  • ALK1

  • ALK2

  • ALK3

  • ALK6

TGF-β Receptor Related Products (34):

Cat. No. Product Name Effect Purity
  • HY-10431
    SB-431542 Inhibitor 99.89%
    SB-431542 is a potent and selective inhibitor of ALK5/TGF-β type I Receptor with an IC50 value of 94 nM.
  • 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. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6.
  • HY-13418A
    Dorsomorphin Inhibitor 99.65%
    Dorsomorphin (BML-275; Compound C) is a potent and selective AMPK inhibitor, that is competitive with ATP, with Ki=109 nM in the absence of AMP. Dorsomorphin inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6.
  • HY-13226
    Galunisertib Inhibitor 99.89%
    Galunisertib (LY2157299) is a oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
  • HY-10432
    A 83-01 Inhibitor >98.0%
    A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12, 45 and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
  • HY-13783
    BIBF0775 Inhibitor 99.90%
    BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.
  • HY-112815
    ALK2-IN-2 Inhibitor
    ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3.
  • HY-101113
    San78-130 Inhibitor
    San78-130 is a selective and potent ALK1 inhibitor with an IC50 of 62 nM. San78-130 also inhibits FLT4/VEGFR3, KDR/VEGFR2, MEK2, and FLT3 with IC50s of 114, 162, 186.7, and 188 nM, respectively.
  • HY-12075
    LY2109761 Inhibitor 99.95%
    LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.
  • HY-12071
    LDN193189 Inhibitor
    LDN193189 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).
  • HY-13012
    RepSox Inhibitor 99.96%
    RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with IC50 of 4 nM.
  • HY-12071A
    LDN193189 Tetrahydrochloride Inhibitor 99.92%
    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).
  • HY-12043
    SB 525334 Inhibitor 99.45%
    SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.
  • HY-10432A
    A 83-01 sodium salt Inhibitor >98.0%
    A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12, 45 and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
  • HY-19928
    Vactosertib Inhibitor 99.58%
    Vactosertib (EW-7197) is an ATP-competitive inhibitor of ALK5 with an IC50 of 12.9 nM. It also inhibits ALK2 and ALK4 at nanomolar concentrations.
  • HY-13462
    LY-364947 Inhibitor 98.91%
    LY-364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II.
  • HY-12273
    DMH-1 Inhibitor 99.58%
    DMH-1 is a potent and selective BMP inhibitor with IC50s of 27/107.9/<5/47.6 nM for ALK1/ALK2/ALK3/ALK6, respectively.
  • HY-P0299
    LSKL, Inhibitor of Thrombospondin TSP-1 Inhibitor 98.29%
    LSKL, Inhibitor of Thrombospondin (TSP-1) is a peptide derived from the latency-associated peptide, inhibits thrombospondin (TSP-1) activation of TGF-β and prevents the progression of hepatic damage and fibrosis.
  • HY-13521
    SB-505124 Inhibitor 99.73%
    SB-505124 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.
  • HY-103021
    LY3200882 Inhibitor 99.49%
    LY3200882 is a novel and highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).
Isoform Specific Products

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