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Home >> Signaling Pathways >> TGF-β / Smad Signaling >> 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.

Targets for  TGF-β Receptor

Products for  TGF-β Receptor

  1. Cat.No. Product Name Information
  2. GC13927 A 77-01 A potent ALK5 inhibitor A 77-01 Chemical Structure
  3. GC10166 A 83-01 A TGF-β type I receptor inhibitor A 83-01 Chemical Structure
  4. GC35210 A 83-01 sodium salt A potent inhibitor of TGF-β type I receptor ALK5 kinase A 83-01 sodium salt Chemical Structure
  5. GC65294 ALK2-IN-2 ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3. ALK2-IN-2 Chemical Structure
  6. GC50589 AZ 12799734 Potent TGF-βRI inhibitor AZ 12799734 Chemical Structure
  7. GC34493 BIBF0775 BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM. BIBF0775 Chemical Structure
  8. GC62868 BIO-013077-01 BIO-013077-01 is a pyrazole TGF-β inhibitor. BIO-013077-01 Chemical Structure
  9. GC50593 BMP signaling agonist sb4

    Potent BMP4 agonist

     BMP signaling agonist sb4 Chemical Structure
  10. GC14298 DMH-1 Selective BMP ALK2 receptor DMH-1 Chemical Structure
  11. GC17243 Dorsomorphin (Compound C) Dorsomorphin (Compound C) (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (Compound C) (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin (Compound C) induces autophagy. Dorsomorphin (Compound C) Chemical Structure
  12. GC12560 Dorsomorphin (Compound C) 2HCl Dorsomorphin (Compound C) 2HCl (BML-275 dihydrochloride; Compound C dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin (Compound C) 2HCl inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin (Compound C) 2HCl induces autophagy. Dorsomorphin (Compound C) 2HCl Chemical Structure
  13. GC65329 EW-7195 EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung. EW-7195 Chemical Structure
  14. GC13354 EW-7197 EW-7197 (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. EW-7197 also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. EW-7197 has potently antimetastatic activity and anticancer effect. EW-7197 Chemical Structure
  15. GC65539 Fresolimumab Fresolimumab (GC1008) is a high-affinity fully human monoclonal antibody that neutralizes the active form of human TGFβ1, TGFβ2, and TGFβ3. Fresolimumab Chemical Structure
  16. GC11878 GW788388 ALK5 inhibitor,potent and selective GW788388 Chemical Structure
  17. GC50317 IN 1130 Potent and selective inhibitor of TGF-βRI IN 1130 Chemical Structure
  18. GC60210 Isosaponarin Isosaponarin is a flavone glycoside isolated from wasabi leaves. Isosaponarin Chemical Structure
  19. GC12108 ITD 1 First selective TGFβ inhibitor ITD 1 Chemical Structure
  20. GC15567 K02288 ALK inhibitor K02288 Chemical Structure
  21. GC16580 LDN-193189 ALK inhibitor,potent and selective LDN-193189 Chemical Structure
  22. GC17035 LDN-212854 BMP receptor inhibitor,potent and selective LDN-212854 Chemical Structure
  23. GC13225 LDN-214117 potent and selective ALK2 inhibitor LDN-214117 Chemical Structure
  24. GC36433 LDN193189 Tetrahydrochloride A selective BMP type I receptor inhibitor LDN193189 Tetrahydrochloride Chemical Structure
  25. GC39398 LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA) LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 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) TFA can readily crosse the blood-brain barrier. LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA) Chemical Structure
  26. GC32728 LSKL, Inhibitor of Thrombospondin TSP-1 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 Chemical Structure
  27. GC12363 LY2109761 TβRI/II kinase inhibitor LY2109761 Chemical Structure
  28. GC18015 LY2157299 LY2157299 (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM. LY2157299 Chemical Structure
  29. GC19234 LY3200882 LY3200882 is a novel and highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). LY3200882 Chemical Structure
  30. GC11604 LY364947

    Inhibitor of TGF-β type I receptor kinase domain

     LY364947 Chemical Structure
  31. GC17582 ML347 BMP receptor inhibitor,potent and selective ML347 Chemical Structure
  32. GC44303 N-Acetylpuromycin N-Acetylpuromycin is a non-ribotoxic form of the antibiotic puromycin that is formed in puromycin-resistant S. N-Acetylpuromycin Chemical Structure
  33. GC32840 R-268712 R-268712 is an orally active and selective ALK-5 inhibitor, with an IC50 of 2.5 nM. R-268712 Chemical Structure
  34. GC16793 RepSox A selective inhibitor of ALK5 RepSox Chemical Structure
  35. GC11545 SB 431542 SB-431542, a small molecule inhibitor SB 431542 Chemical Structure
  36. GC10421 SB-505124 hydrochloride Inhibitor of receptors ALK4, ALK5, and ALK7 SB-505124 hydrochloride Chemical Structure
  37. GC13769 SB505124 ALK4/ALK5/ALK7 inhibitor SB505124 Chemical Structure
  38. GC14349 SB525334 (TGF-beta1) receptor inhibitor SB525334 Chemical Structure
  39. GC13904 SD-208 A potent, selective inhibitor of TGF-βRI SD-208 Chemical Structure
  40. GC32788 SJ000291942 A BMP signaling activator SJ000291942 Chemical Structure
  41. GC19447 SM 16

    SM 16 is a ALK5/ALK4 kinase inhibitor

     SM 16 Chemical Structure
  42. GC37880 Vactosertib Hydrochloride Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect. Vactosertib Hydrochloride Chemical Structure
  43. GC62146 XST-14 XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects. XST-14 Chemical Structure

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