1. TGF-beta/Smad
  2. 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 (30):

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-13226
    Galunisertib Inhibitor 99.89%
    Galunisertib (LY2157299) is a selective TGF-β receptor 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-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 BMP signaling inhibitor, inhibiting ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8, 0.8, 5.3, 16.7 nM, 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-117887
    ALK2-IN-1 Inhibitor
    ALK2-IN-1 is a activin receptor-like kinase-2 (ALK2) inhibitor extracted from patent WO2017181117A1, Compound 876, has an IC50 of <10 nM.
  • HY-13012
    RepSox Inhibitor 99.94%
    RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with IC50 of 4 nM.
  • HY-12071A
    LDN193189 Hydrochloride Inhibitor 99.92%
    LDN193189 Hydrochloride is a BMP signaling inhibitor, inhibiting ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8, 0.8, 5.3, 16.7 nM, respectively.
  • 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-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-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-12273
    DMH-1 Inhibitor 99.65%
    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-103021
    LY3200882 Inhibitor 99.49%
    LY3200882 is a novel and highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).
  • 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 TGFβR with IC50 of 129 nM and 47 nM for ALK4, ALK5, respectively, and it does not inhibits ALK1, 2, 3, or 6 but ALK7.
  • HY-10326
    GW788388 Inhibitor 99.84%
    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-12704
    ITD-1 Inhibitor 99.94%
    ITD-1 is the first selective TGFβ receptor inhibitor with an IC50 of 460 nM.
  • HY-112331
    SJ000291942 Activator 99.20%
    SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway. BMPs are members of the transforming growth factor beta (TGFβ) family of secreted signaling molecules.
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