1. Signaling Pathways
  2. TGF-beta/Smad
  3. TGF-β Receptor

TGF-β Receptor

Receptor

Transforming growth factor beta receptors

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-10431
    SB-431542
    Inhibitor 99.85%
    SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitory activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways.
    SB-431542
  • HY-13418A
    Dorsomorphin
    Inhibitor 99.91%
    Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).
    Dorsomorphin
  • HY-10432
    A 83-01
    Inhibitor 99.41%
    A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
    A 83-01
  • HY-13418
    Dorsomorphin dihydrochloride
    Inhibitor 99.91%
    Dorsomorphin (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. Dorsomorphin dihydrochloride can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).
    Dorsomorphin dihydrochloride
  • HY-12071
    LDN193189
    Inhibitor 99.48%
    LDN193189 is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.
    LDN193189
  • HY-P3970D
    KQFK TFA
    Control 99.12%
    KQFK TFA is the TFA salt form of KQFK (HY-P3970C). KQFK TFA is an inactive control of KRFK (HY-P3970). KRFK is a peptide derived from TSP-1 that can activate TGF-β.
    KQFK TFA
  • HY-W028145
    TGF-βRI inhibitor 2
    Inhibitor 98.32%
    TGF-βRI inhibitor 2 (compound 13) is a TGF-βRI inhibitor. TGF-βRI inhibitor 2 can be used in cancer research.
    TGF-βRI inhibitor 2
  • HY-P990974
    Bezeotermin alfa
    HY-P990974 is an BMP-6-targeting Fusion Protein.
    Bezeotermin alfa
  • HY-13226
    Galunisertib
    Inhibitor 99.95%
    Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
    Galunisertib
  • HY-13012
    RepSox
    Inhibitor 99.92%
    RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes.
    RepSox
  • HY-12273
    DMH-1
    Inhibitor 99.95%
    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.
    DMH-1
  • HY-P99355
    Bimagrumab
    Inhibitor 99.31%
    Bimagrumab (Anti-ACVR2B Reference Antibody) is a human monoclonal antibody that blocks activin type II receptor (ActRII), with KDs of 1.7 pM and 434 pM for human ActRIIB and ActRIIA, respectively. Bimagrumab can be used for the research of pathological muscle loss and weakness.
    Bimagrumab
  • HY-12075
    LY2109761
    Inhibitor 99.72%
    LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.
    LY2109761
  • HY-12043
    SB 525334
    Inhibitor 99.97%
    SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.
    SB 525334
  • HY-12071A
    LDN193189 Tetrahydrochloride
    Inhibitor 99.86%
    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).
    LDN193189 Tetrahydrochloride
  • HY-124697
    BMP signaling agonist sb4
    Agonist 99.98%
    BMP signaling agonist sb4 is a potent benzoxazole bone morphogenetic protein 4 (BMP4) signaling agonist with a EC50 value of 74 nM, activates BMP signaling by stabilizing intracellular p-SMAD-1/5/9. BMP signaling agonist sb4 activates BMP4 target genes (inhibitors of DNA binding, Id1 and Id3) canonical BMP signaling.
    BMP signaling agonist sb4
  • HY-19928
    Vactosertib
    Inhibitor 99.58%
    Vactosertib (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib has potently antimetastatic activity and anticancer effect.
    Vactosertib
  • HY-10432A
    A 83-01 sodium
    Inhibitor 98.43%
    A 83-01 sodium is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
    A 83-01 sodium
  • HY-P0299
    LSKL, Inhibitor of Thrombospondin (TSP-1)
    Antagonist 99.77%
    LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier.
    LSKL, Inhibitor of Thrombospondin (TSP-1)
  • HY-12071B
    LDN-193189 dihydrochloride
    Inhibitor 99.75%
    LDN-193189 (dihydrochloride) is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.
    LDN-193189 dihydrochloride
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

ALK1

ALK2

ALK3

ALK4

ALK5

ALK6

ALK7

TGFβR2

ACVR2A

ACVR2B

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.

TGF-β Receptor Degraders & Inhibitors
Product NameALK1ALK2ALK3ALK4ALK5ALK6ALK7TGFβR2ACVR2AACVR2BPurity    
SB-431542   
ALK4, IC50: 1 μM
ALK5, IC50: 0.75 μM
 
ALK7, IC50: 2 μM
   99.85%
Dorsomorphin 
ACVR1
BMPR1A
  
ALK6
    99.91%
A 83-01   
ALK4, IC50: 45 nM
ALK5, IC50: 12 nM
 
ALK7, IC50: 7.5 nM
   99.41%
Dorsomorphin dihydrochloride 
ACVR1
BMPR1A
  
ALK6
    99.91%
LDN193189 
ACVR1, IC50: 5 nM
BMPR1A, IC50: 30 nM
       99.48%
RepSox    
ALK5, IC50: 4 nM
     99.92%
Bimagrumab        
ACVR2A, Kd: 434 pM
ACVR2B, Kd: 1.7 pM
99.31%
LDN193189 Tetrahydrochloride 
ACVR1, IC50: 5 nM
BMPR1A, IC50: 30 nM
       99.86%
Vactosertib    
ALK5, IC50: 12.9 nM
     99.58%
A 83-01 sodium   
ALK4, IC50: 45 nM
ALK5, IC50: 12 nM
 
ALK7, IC50: 7.5 nM
   98.43%
LDN-212854
ALK1, IC50: 2.4 nM
ACVR1, IC50: 1.3 nM
BMPR1A, IC50: 85.8 nM
ALK4, IC50: 2133 nM
ALK5, IC50: 9276 nM
     99.70%
Sotatercept        
ACVR2A
 99.61%
ML347
ALK1, IC50: 46 nM
ACVR1, IC50: 32 nM
BMPR1A, IC50: 10800 nM
       99.94%
R-268712    
TGFBR1, IC50: 2.5 nM
     99.88%
SB-431542 (GMP)   
ALK4, IC50: 1 μM
ALK5, IC50: 0.75 μM
 
ALK7, IC50: 2 μM
   
Vactosertib Hydrochloride    
ALK5, IC50: 12.9 nM
     99.22%
OD36 
ACVR1, Kd: 37 nM
ACVR1, IC50: 47 nM
ALK2 R206H, IC50: 22 nM
        99.33%
IN-1130    
ALK5
     99.93%
EW-7195    
ALK5, IC50: 4.83 nM
     99.20%
AZ12799734
ALK1, Kd: 7.1 μM
ACVR1, Kd: 6.2 μM
BMPR1A, Kd: 40 μM
ALK4, Kd: 1 μM
ALK5, Kd: 0.74 μM
TGFBR1, IC50: 47 nM
ALK6, Kd: 0.017 μM
    98.07%
Itacnosertib 
ACVR1
  
ALK5
     99.06%
Zilurgisertib 
ALK2
        99.77%
AZ12601011   
ALK4
  
ALK7
   99.88%
THRX-144644    
ALK5, IC50: 0.14 nM
     99.90%
ALK2-IN-2 
ACVR1, IC50: 9 nM
        99.93%
KER047 succinate 
ACVR1
        98.93%
KER047 
ACVR1
        99.35%
ALK5-IN-34    
ALK5, IC50: <10 nM
     98.21%
TGFBR1-IN-1    
ALK5, IC50: 10-100 nM
     
M4K2281 
ALK2, IC50: 2 nM
  
ALK5, IC50: 350 nM
     
ALK5-IN-33    
ALK5, IC50: ≤10 nM
     
J-1149    
ALK5, IC50: 0.017 μM
     
TGFβRII-IN-2       
TGF-βR2, IC50: 2.4 μM
  
ALK5-IN-25    
ALK5, IC50: ≤10 nM
     
M4K2308 
ALK2, IC50: 2 nM
  
ALK5, IC50: 224 nM
     
MU1700
ALK1, IC50: 13 nM
ALK2, IC50: 6 nM
   
ALK6, IC50: 41 nM
    
TGFβRII-IN-3       
TGF-βR2, IC50: 4.1 μM
  
ALK5-IN-27    
ALK5, IC50: ≤10 nM
     
OD36 hydrochloride 
ACVR1, Kd: 37 nM
ACVR1, IC50: 47 nM
ALK2 R206H, IC50: 22 nM
        
J-1063    
ALK5
     
ALK5-IN-28    
ALK5, IC50: ≤10 nM
     
M4K2306 
ALK2, IC50: 7 nM
  
ALK5, IC50: 3915 nM
     
A 83-01 (Standard)   
ALK4, IC50: 45 nM
ALK5, IC50: 12 nM
 
ALK7, IC50: 7.5 nM