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TGF-β Receptor(TGF-β受体)

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.

Products for  TGF-β Receptor

  1. Cat.No. 产品名称 Information
  2. GC65539 Fresolimumab Fresolimumab (GC1008) 是一种高亲和力的全人单克隆抗体,可中和人 TGFβ1、TGFβ2 和 TGFβ3 的活性形式。Fresolimumab 可用于癌症和纤维性疾病的研究。
  3. GC65329 EW-7195 EW-7195 是一种有效的、选择性 ALK5 (TGFβR1) 抑制剂,IC50 为 4.83 nM。EW-7195 对 ALK5 的选择性是 p38α 的 300 多倍。EW-7195 能有效抑制 TGF-β1 诱导的 Smad 信号转导、上皮间质转化 (EMT) 和乳腺癌向肺转移。
  4. GC65294 ALK2-IN-2 ALK2-IN-2 是一种有效的、选择性的活化素受体样激酶 2 (ALK2) 抑制剂,IC50 值为 9 nM,对 ALK2 的抑制作用是 ALK3 的 700 倍。
  5. GC62868 BIO-013077-01 BIO-013077-01 是一种吡唑类的 TGF-β 抑制剂。
  6. GC62146 XST-14 XST-14 是一种有效的,竞争性强且高度选择性的 ULK1 抑制剂,IC50 为 26.6 nM。XST-14 通过减少 ULK1 下游底物的磷酸化来诱导自噬抑制。XST-14 诱导肝细胞癌 (HCC) 细胞凋亡,并具有抗肿瘤作用。
  7. GC60210 Isosaponarin Isosaponarin是一种从芥末叶中分离出的黄酮苷,可以增加胶原蛋白(collagen)的合成,这是由上调的TGF-βII型受体(TβR-II)和脯氨酰4-羟化酶(P4H)蛋白产生引起的。
  8. GC39398 LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)

    LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 是一种衍生自 LAP-TGFβ 的四肽,是一种竞争性的 TGF-β1 拮抗剂。LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 抑制 TSP-1 与 LAP 的结合并减轻肾间质纤维化和肝纤维化。LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 通过抑制 TSP-1 介导的 TGF-β1 活性来抑制蛛网膜下纤维化,防止慢性脑积水的发生并改善蛛网膜下腔出血后的长期神经认知缺陷。LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 可以轻松穿越血脑屏障。

  9. GC50593 BMP signaling agonist sb4 BMP signaling agonist sb4 是一种有效的苯并恶唑骨形态发生蛋白 4 (BMP4) 信号激动剂,EC50 值为 74 nM,通过稳定细胞内 p-SMAD-1/5/9 来激活 BMP 信号传导。 BMP 信号激动剂 sb4 激活 BMP4 靶基因(DNA 结合抑制剂,Id1 和 Id3)经典 BMP 信号。
  10. GC50589 AZ 12799734 AZ 12799734 是一种选择性的、口服活性的 TGFBR1 激酶抑制剂,IC50 为 47 nM。
  11. GC50317 IN 1130 IN 1130 是一种高度选择性的转化生长因子-β I 型受体激酶 (ALK5) 抑制剂,对 ALK5 介导的 Smad3 磷酸化的 IC50 为 5.3 nM。
  12. GC37880 Vactosertib Hydrochloride Vactosertib Hydrochloride (EW-7197 Hydrochloride) 是 TGFβRI (ALK5) 的小分子 ATP 竞争性抑制剂,其 IC50 值为 12.9 nM。
  13. GC36433 LDN193189 Tetrahydrochloride An inhibitor of BMP receptors ALK1, ALK2, ALK3, and ALK6
  14. GC35210 A 83-01 sodium salt A TGF-β type I receptor inhibitor
  15. GC44303 N-Acetylpuromycin A non-ribotoxic form of puromycin
  16. GC34493 BIBF0775 BIBF-0775 is a selective inhibitor of transforming growth factor β Receptor I (TGFβRI,Alk5) with an IC50 of 34nM.
  17. GC32840 R-268712 R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
  18. GC32788 SJ000291942 A BMP signaling activator
  19. GC32728 LSKL, Inhibitor of Thrombospondin TSP-1

    LSKL,InhibitorofThrombospondin(TSP-1)是一种四肽,源于潜在联系多肽,能够抑制TSP-1的活性,来降低TGF-β的活性,能够阻止肝损伤和肝纤维化。

  20. GC19447 SM 16 An inhibitor of ALK5
  21. GC19234 LY3200882 An inhibitor of TGF-βRI
  22. GC13354 EW-7197 A potent inhibitor of ALK5
  23. GC12108 ITD 1 An inhibitor of TGF-β
  24. GC13225 LDN-214117 A selective ALK1 and ALK2 inhibitor
  25. GC17582 ML347 A selective ALK1 and ALK2 inhibitor
  26. GC17035 LDN-212854 An ALK2 inhibitor
  27. GC14298 DMH-1 A potent ALK2 inhibitor
  28. GC11604 LY364947 Inhibitor of TGF-β type-1 receptors
  29. GC13769 SB505124 Inhibitor of receptors ALK4, ALK5, and ALK7
  30. GC17243 Dorsomorphin (Compound C)

    A potent, selective AMPK inhibitor

  31. GC15567 K02288 A BMP signaling inhibitor
  32. GC12560 Dorsomorphin (Compound C) 2HCl

    A potent, reversible AMPK inhibitor

  33. GC12363 LY2109761 A dual inhibitor of TGF-β type 1/type II receptor kinases
  34. GC18015 LY2157299 A TGF-β type 1 receptor kinase inhibitor
  35. GC16580 LDN-193189

    An inhibitor of BMP receptors ALK1, ALK2, ALK3, and ALK6

  36. GC11878 GW788388 An inhibitor of ALK5 (TGFBR1)
  37. GC14349 SB525334 A potent inhibitor of TGF-β R1/ALK5 kinase
  38. GC11545 SB 431542

    SB-431542是一种小分子抑制剂。

  39. GC13904 SD-208 A potent, selective inhibitor of TGF-βRI
  40. GC10421 SB-505124 hydrochloride Inhibitor of receptors ALK4, ALK5, and ALK7
  41. GC16793 RepSox A selective inhibitor of ALK5
  42. GC10166 A 83-01 A TGF-β type I receptor inhibitor
  43. GC13927 A 77-01 A potent ALK5 inhibitor

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