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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

    A77-01;A-77-01

     A potent ALK5 inhibitor A 77-01 Chemical Structure
  3. GC10166 A 83-01 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 IC50 s of 12 nM,45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively . A 83-01 Chemical Structure
  4. GC35210 A 83-01 sodium salt

    3-(6-Methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide, 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. GC73338 ALK5-IN-34 ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 Chemical Structure
  7. GC50589 AZ 12799734 Potent TGF-βRI inhibitor AZ 12799734 Chemical Structure
  8. 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
  9. GC74516 Bintrafusp alfa

    M7824; MSB0011359C

     Bintrafusp alfa (M 7824) is a first-in-class bifunctional fusion protein composed of the extracellular domain of TGF-βRII fused to a human IgG1 mAb blocking programmed cell death ligand. Bintrafusp alfa Chemical Structure
  10. GC62868 BIO-013077-01 BIO-013077-01 is a pyrazole TGF-β inhibitor. BIO-013077-01 Chemical Structure
  11. GC50593 BMP signaling agonist sb4

    Potent BMP4 agonist

     BMP signaling agonist sb4 Chemical Structure
  12. GC73535 BMPR2-IN-1 TFA

    BMPR2-IN-1 (Compound 8a) is a BMPR2 inhibitor with an IC50 of 506 nM and a KD of 83.5 nM.

     BMPR2-IN-1 TFA Chemical Structure
  13. GC72917 BUR1 BUR1 is a BMP upregulator (EC50: 98 nM) and activates BMPRII signalling. BUR1 Chemical Structure
  14. GC70882 Chromenone 1 Chromenone 1 is a potent osteogenic bone morphogenetic protein (BMP) potentiator. Chromenone 1 Chemical Structure
  15. GC72448 Dalutrafusp alfa Dalutrafusp alfa (AGEN-1423; GS-1423) is a specific bifunctional antibody against CD73 and TGF-β, which is involved in the immunosuppressive pathway. Dalutrafusp alfa Chemical Structure
  16. GC14298 DMH-1

    BMP Inhibitor II, DorsoMorphin Homolog 1, VU036482

     Selective BMP ALK2 receptor DMH-1 Chemical Structure
  17. GC17243 Dorsomorphin (Compound C)

    Compound C

     Dorsomorphin (Compound C) is an agent that used as a cell-permeable AMPK inhibitor. Dorsomorphin (Compound C) Chemical Structure
  18. GC12560 Dorsomorphin (Compound C) 2HCl

    BML-275 2HCl,Compound C 2HCl

     IC50: Dorsomorphin inhibited BMP4-induced phosphorylation of BMP-responsive SMADs in a dose-dependent manner (half maximal inhibitory concentration (IC50) =0.47 mM). Dorsomorphin (Compound C) 2HCl Chemical Structure
  19. 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
  20. GC13354 EW-7197

    Vactosertib, TEW-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
  21. GC65539 Fresolimumab Fresolimumab is a high-affinity humanized monoclonal antibody that binds to and inhibits all isoforms of the protein transforming growth factor β (TGFβ). The Kd values of Fresolimumab for TGFβ1, TGFβ2, and TGFβ3 are 1.7±0.6nM, 3.0±1.2nM, and 2.0±1.2nM, respectively. Fresolimumab Chemical Structure
  22. GC11878 GW788388 ALK5 inhibitor,potent and selective GW788388 Chemical Structure
  23. GC50317 IN 1130 Potent and selective inhibitor of TGF-βRI IN 1130 Chemical Structure
  24. GC60210 Isosaponarin Isosaponarin is a flavone glycoside isolated from wasabi leaves. Isosaponarin Chemical Structure
  25. GC72815 Itacnosertib (hydrocholide)

    TP-0184 (hydrocholide

     Itacnosertib drocholide is an inhibitor of JAK2, ACVR1 (ALK2) and ALK5. Itacnosertib (hydrocholide) Chemical Structure
  26. GC12108 ITD 1 First selective TGFβ inhibitor ITD 1 Chemical Structure
  27. GC15567 K02288 ALK inhibitor K02288 Chemical Structure
  28. GC72215 KRFK TFA KRFK TFA, a peptide derived from TSP-1, can activate TGF-β. KRFK TFA Chemical Structure
  29. GC16580 LDN-193189

    LDN 193189;LDN193189

     ALK inhibitor,potent and selective LDN-193189 Chemical Structure
  30. GC17035 LDN-212854 BMP receptor inhibitor,potent and selective LDN-212854 Chemical Structure
  31. GC13225 LDN-214117 potent and selective ALK2 inhibitor LDN-214117 Chemical Structure
  32. GC36433 LDN193189 Tetrahydrochloride A selective BMP type I receptor inhibitor LDN193189 Tetrahydrochloride Chemical Structure
  33. 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
  34. 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
  35. GC12363 LY2109761 TβRI/II kinase inhibitor LY2109761 Chemical Structure
  36. GC18015 LY2157299

    LY-2157299;LY 2157299

     LY2157299 is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 value of 56nM. LY2157299 Chemical Structure
  37. GC19234 LY3200882 LY3200882 is a novel and highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). LY3200882 Chemical Structure
  38. GC11604 LY364947

    HTS 466284, TGFβ RI Kinase Inhibitor

    Inhibitor of TGF-β type I receptor kinase domain

     LY364947 Chemical Structure
  39. GC17582 ML347

    LDN193719

     BMP receptor inhibitor,potent and selective ML347 Chemical Structure
  40. 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
  41. 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
  42. GC16793 RepSox

    E 616452, RepSox, SJN 2511

     RepSox is a potent and selective inhibitor of transforming growth factor-β receptor I/activin-like kinase 5 (TGF-β-RI/ALK5) with an IC50 of 23nM. RepSox inhibits ALK5 autophosphorylation with an IC50 of 4nM. RepSox Chemical Structure
  43. GC11545 SB 431542 SB-431542, a small molecule inhibitor of the type I TGF-β receptor, blocks intracellular mediators of TGF-1 signaling, which leads to decreased TGF-β1–mediated proliferation, cytokines and collagen expression. SB 431542 Chemical Structure
  44. GC10421 SB-505124 hydrochloride

    SB 505124 hydrochloride;SB505124 hydrochloride

     Inhibitor of receptors ALK4, ALK5, and ALK7 SB-505124 hydrochloride Chemical Structure
  45. GC13769 SB505124 ALK4/ALK5/ALK7 inhibitor SB505124 Chemical Structure
  46. GC14349 SB525334

    TGF-β RI Kinase Inhibitor VIII

     (TGF-beta1) receptor inhibitor SB525334 Chemical Structure
  47. GC13904 SD-208

    TGF-β RI Kinase Inhibitor V

     A potent, selective inhibitor of TGF-βRI SD-208 Chemical Structure
  48. GC74617 SHR-1701

    Retlirafusp alfa

     SHR-1701 (Retlirafusp alfa) is a bifunctional fusion protein targeting PD-L1 and TGF-β for cancer research. SHR-1701 Chemical Structure
  49. GC32788 SJ000291942 A BMP signaling activator SJ000291942 Chemical Structure
  50. GC19447 SM 16

    SM 16 is a ALK5/ALK4 kinase inhibitor

     SM 16 Chemical Structure
  51. GC72410 Stamulumab Stamulumab (MYO-029) is a recombinant human IgG1λ antibody that binds to myostatin and neutralizes its activity by preventing binding to its endogenous high-affinity receptor ActRIIB. Stamulumab Chemical Structure
  52. GC73292 THRX-144644 THRX-144644 is a Lung-restricted ALK5 inhibitor with an IC50 value of 0.14 nM. THRX-144644 Chemical Structure
  53. GC37880 Vactosertib Hydrochloride

    EW-7197 Hydrochloride; TEW-7197 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
  54. GC72283 Vicatertide Vicatertide is a TGF beta-1 inhibitor. Vicatertide Chemical Structure
  55. 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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