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 (26):

Cat. No. Product Name Effect Purity
  • HY-10431
    SB-431542 Inhibitor 98.79%
    SB-431542 is a potent and selective inhibitor of ALK5 with an IC50 value of 94 nM, and is also an inhibitor of TGF-β Receptor.
  • 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-13226
    LY2157299 Inhibitor 99.89%
    LY2157299 is a selective TGF-βR inhibitor with IC50 of 56 nM.
  • HY-12075
    LY2109761 Inhibitor 99.60%
    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-12071
    LDN193189 Inhibitor 99.40%
    LDN193189 is a selective BMP type I receptor kinases inhibitor, which inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with substantially weaker effects on activin and the TGF-β type I receptors ALK4, ALK5 and ALK7 (IC50≥500 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-19928A
    EW-7197 Hydrochloride Inhibitor 98.02%
    EW-7197 Hydrochloride is a small-molecule ATP-competitive inhibitor of TGFβRI (ALK5) with an IC50 of 12.9 nM.
  • HY-13012
    RepSox Inhibitor 99.94%
    RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor, inhibits ALK5 autophosphorylation with IC50 of 4 nM.
  • HY-19928
    EW-7197 Inhibitor 99.12%
    EW-7197 is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively.
  • HY-12043
    SB 525334 Inhibitor 99.18%
    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-12071A
    LDN193189 Hydrochloride Inhibitor 99.68%
    LDN193189 hydrochloride is a selective BMP type I receptor kinases inhibitor, which inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with substantially weaker effects on activin and the TGF-β type I receptors ALK4, ALK5 and ALK7 (IC50≥500 nM).
  • 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-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-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-12278
    K02288 Inhibitor 99.43%
    K02288 is a potent inhibitor of ALK, and inhibits ALK1/2/3/6 with IC50s of 1.8/1.1/34.4/6.3 nM; K02288 is less potent against ALK4/5, with IC50s of 302 nM and 321 nM.
  • HY-15897
    LDN-212854 Inhibitor 98.17%
    LDN-212854 is a novel BMP inhibitor that exhibits substantially greater selectivity for BMP versus the TGF-β type I receptors; possesses a bias towards ALK2(IC50=1.3 nM) versus ALK1 and ALK3 compared to other inhibitors.
  • HY-13227
    SD-208 Inhibitor 98.33%
    SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, > 100-fold selectivity over TGF-βRII.
  • HY-103021
    LY3200882 Inhibitor 99.49%
    LY3200882 is a novel and highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).
  • HY-12704
    ITD-1 Activator 98.66%
    ITD-1 is an inducer of TGFβ type II receptor degradation-1, is a potent and highly selective TGFβ pathway inhibitor (IC50 = 0.85 μM).
Isoform Specific Products

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