Signaling Pathway

TGF-β Receptor

TGF-β Receptor

Related Products

PDF File 0.26MB

TGF-β receptors are single pass serine/threonine kinase receptors. TGF-β receptor exist in several different isoforms that can be homo- or heterodimeric. TGF (Transforming Growth Factor) are 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 receptors, 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 type III has a high affinity for both TGF-β1 and -β2 and in addition TGF-β1.2.

TGF-β Receptor Inhibitors & Modulators (13)

Product Name Catalog No. Brief Description
A 77-01

HY-78349

A 77-01 is a potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM.

A 83-01

HY-10432

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 (IC50 values are 12, 45 and 7.5 nM respectively).

EW-7197

HY-19928

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.

GW788388

HY-10326

GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, also inhibits TGF-β type II receptor and activin type II receptor activities, but does not inhibit BMP type II receptor.

ITD-1

HY-12704

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).

LY-364947

HY-13462

LY364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, exhibits 7-fold selectivity over TGFβR-II.

LY2109761

HY-12075

LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM, respectively; shown to negatively affect the phosphorylation of Smad2.

LY2157299

HY-13226

LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM.

R-268712

HY-12953

R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.

RepSox

HY-13012

RepSox(E-616452; SJN 2511) is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation, respectively.

SB 525334

HY-12043

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.

SB-431542

HY-10431

SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM, also inhibits the phosphorylation of immobilized Smad3 with an IC50 of 94 nM.

SD-208

HY-13227

SD-208 is a potent, orally active ATP-competitive transforming growth factor-β receptor 1 (TGF-βRI) inhibitor (IC50= 49 nM); displays > 100-fold and > 17-fold selectivity over TGF-βRII and other common kinases respectively.