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 (41):

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-13226
    Galunisertib Inhibitor 99.95%
    Galunisertib (LY2157299) 是一种选择性的 TGF-β 受体 I 型 (TGF-βRI) 激酶抑制剂,IC50 为 56 nM。
  • 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-136773
    ALK2-IN-4 Inhibitor 99.86%
    ALK2-IN-4 是一种有效的 ALK2 抑制剂,详细信息请参见专利 WO2020086963A1,compound Formula I free base。
  • HY-P2294
    pm26TGF-β1 peptide
    pm26TGF-β1 peptide 是一种模拟人 TGF-β1 分子的肽,并对 TGF-β1 受体具有高亲和力。pm26TGF-β1 peptide 具有有效的抗炎特性,并且不表现出嗜中性粒细胞的趋化性。
  • HY-136773A
    ALK2-IN-4 succinate Inhibitor
    ALK2-IN-4 succinate 是一种有效的 ALK2 抑制剂,详细信息请参见专利 WO2020086963A1,compound Formula I free base。
  • HY-12071
    LDN193189 Inhibitor
    LDN193189 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-12075
    LY2109761 Inhibitor 99.95%
    LY2109761是可口服,选择性的 TGF-β receptor type I/II 抑制剂,Ki分别为38 nM 和 300 nM。
  • HY-13012
    RepSox Inhibitor 99.96%
    RepSox 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 99.92%
    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 >98.0%
    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-13462
    LY-364947 Inhibitor 99.49%
    LY-364947 (HTS466284) 是一种有效的,ATP 竞争性的 TGFβR-I 抑制剂,IC50 值为 59 nM,是对 TGFβR-II 选择性的 7 倍。
  • HY-19928
    Vactosertib Inhibitor 99.58%
    Vactosertib (EW-7197) 是一种有效的,具有口服活性且具有 ATP 竞争性激活素受体样激酶 5 (ALK5) 抑制剂,IC50 为 12.9 nM。Vactosertib 还以纳摩尔浓度抑制 ALK2 和 ALK4 (IC50 为 17.3 nM)。Vactosertib 具有强大的抗转移活性和抗癌作用。
  • 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-112331
    SJ000291942 Activator 99.20%
    SJ000291942 是经典骨形态发生蛋白 (BMP) 信号传导途径的激活剂。BMP 是转化生长因子 β (TGFβ) 分泌信号分子家族的成员。
  • HY-103021
    LY3200882 Inhibitor 99.60%
    LY3200882 是一种有效的,高度选择性的,具有 ATP 竞争性和口服活性的 TGF-β 受体 1 型 (ALK5) 抑制剂,IC50 为 38.2 nM。LY3200882 可抑制多种促肿瘤活性,还用作免疫调节剂。
Isoform Specific Products

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