1. TGF-beta/Smad
  2. TGF-β Receptor

TGF-β Receptor

TGF-β (Transforming growth factor-β) receptors are single pass serine/threonine kinase receptors. TGF-β receptor exists in several different isoforms that can be homo- or heterodimeric. TGF is involved in paracrine signalling and can be found in many different tissue types, including brain, heart, kidney,liver, and testes. Over-expression of TGF can induce renal fibrosis, causing kidney disease, as well as diabetes, and ultimately end-stage renal disease (ESRD). Recent developments have found that, using certain types of protein antagonists against TGFβ receptor, can halt and in some cases reverse the effects of renal fibrosis. Three TGF-β receptor types can be distinguished by their structural and functional properties. Receptor types I and II have similar ligand-binding affinities and can be distinguished from each other only by peptide mapping. Both receptor types I and II have a high affinity for TGF-β1 and low affinity for TGF-β2.

TGF-β Receptor Related Products (13):

Cat. No. Product Name Effect Purity
  • HY-10431
    SB-431542 Inhibitor
    SB-431542 is a potent and selective inhibitor of ALK5 and ALK4 with IC50 values of 94 nM and 14 nM, respectivelly, and is also an inhibitor of TGF-β Receptor.
  • HY-13226
    LY2157299 Inhibitor
    LY2157299 is a selective TGF-βR inhibitor with IC50 of 56 nM.
  • HY-10432
    A 83-01 Inhibitor
    A 83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC50 values of 12, 45 and 7.5 nM, respectively.
  • HY-12075
    LY2109761 Inhibitor
    LY2109761 is an orally active, selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM, respectively, and negatively affects the phosphorylation of Smad2.
  • HY-13012
    RepSox Inhibitor
    RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor, inhibits ALK5 autophosphorylation with IC50 of 4 nM.
  • HY-13227
    SD-208 Inhibitor
    SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, > 100-fold selectivity over TGF-βRII.
  • HY-19928
    EW-7197 Inhibitor
    EW-7197 is a highly potent, selective, and orally bioavailable TGF-(beta) receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively.
  • HY-13462
    LY-364947 Inhibitor
    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-12043
    SB 525334 Inhibitor
    SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM, is 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6.
  • HY-10326
    GW788388 Inhibitor
    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 Activator
    ITD-1 is an inducer of TGF(beta) type II receptor degradation-1, is a potent and highly selective TGF(beta) pathway inhibitor (IC50 = 0.85 (mu)M).
  • HY-12953
    R-268712 Inhibitor
    R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
  • HY-78349
    A 77-01 Inhibitor
    A 77-01 is a potent inhibitor of TGF-(beta) type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM.