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 相关产品 (32):

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-13418
    Dorsomorphin dihydrochloride Inhibitor 99.91%
    Dorsomorphin dihydrochloride (BML-275 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。
  • HY-13418A
    Dorsomorphin Inhibitor 99.65%
    Dorsomorphin (BML-275; Compound C) 是一种有效的 ATP 竞争性的选择性 AMPK 抑制剂,Ki 为 109 nM。Dorsomorphin 通过靶向抑制 I 型受体 ALK2ALK3ALK6 来抑制 BMP 途径。
  • HY-13226
    Galunisertib Inhibitor 99.89%
    Galunisertib (LY2157299) 是一种选择性的 TGF-β 受体抑制剂,IC50 为 56 nM。
  • HY-10432
    A 83-01 Inhibitor >98.0%
    A 83-01 是有效的 TGF-β I 型受体 ALK5ALK4ALK7 的抑制剂,能够抑制 ALK5,ALK4 和 ALK7 诱导的转录,IC50 值分别为 12,45 和 7.5 nM。
  • HY-13783
    BIBF0775 Inhibitor 99.90%
    BIBF0775是有效,选择性的TGFβI型受体 (Alk5)的抑制剂,IC50为34 nM。
  • HY-117887
    ALK2-IN-1 Inhibitor
    ALK2-IN-1 是一种活化素受体样激酶 2 (ALK2) 抑制剂,IC50<10 nM。详细信息请参考专利文献 WO2017181117A1 中的化合物 876。
  • 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-12071
    LDN193189 Inhibitor
    LDN193189是 BMP 信号传导抑制剂,抑制ALK1ALK2ALK3ALK6IC50分别为0.8,0.8,5.3,16.7 nM。
  • HY-13012
    RepSox Inhibitor 99.94%
    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 Hydrochloride Inhibitor 99.92%
    LDN193189 Hydrochloride是 BMP 信号传导抑制剂,抑制 ALK1ALK2ALK3ALK6IC50 分别为0.8,0.8,5.3,16.7 nM。
  • HY-12043
    SB 525334 Inhibitor 99.45%
    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-19928
    Vactosertib Inhibitor 99.58%
    Vactosertib (EW-7197) 是 ALK5 的 ATP 竞争性抑制剂,IC50 为 12.9 nM。抑制 ALK2 和 ALK4 在纳摩尔级别。
  • HY-13462
    LY-364947 Inhibitor 98.91%
    LY-364947 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-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 ALK5,及 ALK4ALK7 抑制剂,能够抑制 ALK5,ALK4 和 ALK7 诱导的转录,IC50 值分别为 12,45 和 7.5 nM。
  • HY-12273
    DMH-1 Inhibitor 99.58%
    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-103021
    LY3200882 Inhibitor 99.49%
    LY3200882 是一个新型且具有高选择性的 TGF-β 受体 1 型 (TGFβRI) 抑制剂。
  • HY-P0299
    LSKL, Inhibitor of Thrombospondin TSP-1 Inhibitor 98.29%
    LSKL, Inhibitor of Thrombospondin (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。
  • HY-10326
    GW788388 Inhibitor 99.84%
    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-13521
    SB-505124 Inhibitor 99.73%
    SB-505124 是一种选择性的 TGFβR 抑制剂,对 ALK4ALK5IC50 值分别为 129 nM 和 47 nM。
Isoform Specific Products

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