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

TGF-β Receptor Isoform Specific Products:

  • ALK2

  • ALK3

  • ALK6

  • ALK5

  • ALK4

  • ALK7

TGF-β Receptor 相关产品 (27):

Cat. No. Product Name Effect Purity
  • HY-10431
    SB-431542 Inhibitor 99.89%
    SB-431542 是一种有效,选择性的 ALK5/TGF-β type I Receptor 抑制剂,IC50 值为 94 nM。
  • HY-13418A
    Dorsomorphin Inhibitor 99.65%
    Dorsomorphin (Compound C) 是一种选择性,ATP 竞争性的 AMPK 抑制剂 (在没有 AMP 的情况下,Ki 为 109 nM)。Dorsomorphin 选择性抑制 BMP I 型受体 ALK2ALK3ALK6。Dorsomorphin 诱导自噬 (autophagy) 作用。
  • HY-13418
    Dorsomorphin dihydrochloride Inhibitor 99.91%
    Dorsomorphin dihydrochloride (Compound C dihydrochloride) 是一种有效,选择性和 ATP 竞争性的 AMPK 抑制剂,Ki 为 109 nM。Dorsomorphin dihydrochloride 通过靶向抑制 I 型受体 ALK2ALK3ALK6 来抑制 BMP 途径。Dorsomorphin dihydrochloride 诱导自噬 (autophagy) 作用。
  • HY-10432
    A 83-01 Inhibitor >98.0%
    A 83-01 是一种有效的 TGF-β I 型受体 ALK5ALK4ALK7 的抑制剂,能够抑制 ALK5ALK4ALK7 诱导的转录,IC50 值分别为 12 nM,45 nM 和 7.5 nM。
  • HY-12071
    LDN193189 Inhibitor 99.48%
    LDN193189 (DM-3189) 是一种选择性的 BMP I 型受体抑制剂,抑制 ALK2ALK3IC50 分别为 5 nM 和 30 nM。对 ALK4,ALK5 和 ALK7 的作用效果弱 (IC50≥500 nM)。
  • HY-N2589
    Isosaponarin Activator
    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。
  • HY-13012
    RepSox Inhibitor 99.96%
    RepSox (E-616452) 是一种有效,选择性的 TGFβR-1/ALK5 抑制剂, 抑制ALK5自磷酸化,IC50 为 4 nM。
  • HY-12071A
    LDN193189 Tetrahydrochloride Inhibitor 98.04%
    LDN193189 Tetrahydrochloride 是一种选择性的 BMP I 型受体抑制剂,抑制 ALK2ALK3IC50 分别为 5 nM 和 30 nM。对 ALK4,ALK5 和 ALK7 的作用效果弱 (IC50≥500 nM)。
  • HY-10432A
    A 83-01 sodium salt Inhibitor
    A 83-01 sodium salt 是一种有效的 TGF-β I 型受体 ALK5ALK4ALK7 的抑制剂,能够抑制 ALK5ALK4ALK7 诱导的转录,IC50 值分别为 12 nM,45 nM 和 7.5 nM。
  • HY-12043
    SB 525334 Inhibitor 99.96%
    SB 525334是一种有效,选择性的转化生长因子β1受体 (ALK5) 抑制剂,IC50 为 14.3 nM。
  • HY-13521
    SB-505124 Inhibitor 99.63%
    SB-505124 是一种选择性的 TGF-β Receptor type I receptor (ALK4ALK5ALK7) 抑制剂,对 LK4,ALK5 的 IC50 值分别为 129 nM 和 47 nM,对 ALK1,2,3 或 6 无作用。
  • HY-12273
    DMH-1 Inhibitor 99.72%
    DMH-1 是一种有效的,具有选择性的 BMP 抑制剂,对 ALK1/ALK2/ALK3/ALK6的IC50 值分别为 27/107.9/<5/47.6 nM。
  • HY-10326
    GW788388 Inhibitor 99.91%
    GW788388 是一种有效的 ALK5 抑制剂,IC50 值 18 nM;同时抑制 TGF-β II 型受体 和激活素 II 型受体的活性,但对 BMP II 型受体无作用。
  • HY-12704
    ITD-1 Inhibitor 99.94%
    ITD-1 是第一个选择性的 TGFβ 受体抑制剂,IC50 为 460 nM。
  • HY-13227
    SD-208 Inhibitor 99.87%
    SD-208 是一种选择性的 TGF-βRI (ALK5) 抑制剂,IC50 值为 48 nM,对其选择性是对 TGF-βRII 的 100 多倍。
  • HY-12278
    K02288 Inhibitor 99.80%
    K02288是一种有效的骨形态发生蛋白 (BMP) I型受体抑制剂,抑制ALK1,ALK2,ALK6的 IC50 为1.8,1.1,6.4 nM。对 ALK3 和 ALK6 的抑制稍弱,IC50在5-34 nM之间。
  • HY-15897
    LDN-212854 Inhibitor 99.87%
    LDN-212854是新型BMP抑制剂,对ALK2的IC50为1.3 nM,比对ALK1,ALK3,ALK4和ALK5的抑制性高2,66,1641和7135倍。
  • HY-12953
    R-268712 Inhibitor 99.70%
    R-268712是一种有效的选择性ALK5抑制剂, IC50为2.5 nM。
  • HY-P0299A
    LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA) Antagonist 99.30%
    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。
  • HY-124697
    BMP signaling agonist sb4 Agonist 99.86%
    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 激活 BMP 信号。BMP signaling agonist sb4 还能激活典型 BMP 信号通路中的 BMP4 靶基因 (DNA 结合抑制剂,Id1 和 Id3)。
Isoform Specific Products

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