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

TGF-β Receptor (TGF-β受体)

Transforming growth factor beta receptors

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-10431
    SB-431542 Inhibitor 99.89%
    SB-431542 是 TGF-β 受体激酶抑制剂 (TRKI)。SB-431542 对 ALK4、ALK5 和 ALK7 活性有抑制作用, IC50 值分别为 1 μM、0.75 μM 和 2 μM。SB-431542 还能抑制 TGF-β 诱导的转录、基因表达、细胞凋亡和生长抑制。SB-431542 可用于癌症及其信号转导途径的研究。
    SB-431542
  • HY-13418A
    Dorsomorphin Inhibitor 99.91%
    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 还能够逆转 Urolithin A (HY-100599) 导致的自噬 (autophagy) 激活和抗炎作用。
    Dorsomorphin
  • HY-10432
    A 83-01 Inhibitor 99.41%
    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。
    A 83-01
  • HY-13418
    Dorsomorphin dihydrochloride Inhibitor 99.91%
    Dorsomorphin (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 还能够逆转 Urolithin A (HY-100599) 导致的自噬 (autophagy) 激活和抗炎作用。
    Dorsomorphin dihydrochloride
  • 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。
    Galunisertib
  • HY-117887
    Fidrisertib 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。
    Fidrisertib
  • HY-109179A
    Itacnosertib (hydrocholide) Inhibitor 98.98%
    Itacnosertib hydrocholide 是 JAK2ACVR1 (ALK2)ALK5 的抑制剂。
    Itacnosertib (hydrocholide)
  • HY-154970A
    BMPR2-IN-1 TFA Inhibitor 99.40%
    BMPR2-IN-1 (Compound 8a) 是一种 BMPR2 抑制剂,IC50 为 506 nM,K D 为 83.5 nM。BMPR2-IN-1 可用于肺动脉高压、阿尔茨海默病和癌症的研究。
    BMPR2-IN-1 TFA
  • HY-12071
    LDN193189 Inhibitor 99.48%
    LDN193189 是一种有效的选择性 BMP I 型受体抑制剂。LDN-193189 有效抑制 BMP I 型受体 ALK2ALK3 的转录活性,IC50 值分别为 5 nM 和 30 nM。LDN-193189 可用于骨形态发生蛋白信号传导的研究,例如进行性骨化纤维发育不良。
    LDN193189
  • HY-13012
    RepSox Inhibitor 99.93%
    RepSox (E-616452) 是一种有效的选择性转化生长因子-β 受体 I/激活素样激酶 5 (TGF-β-RI/ALK5) 抑制剂。RepSox 抑制 ALK5 自身磷酸化,IC50 值为 4 nM。RepSox 可用于肥胖和相关代谢疾病(如 2 型糖尿病)的研究。
    RepSox
  • HY-12075
    LY2109761 Inhibitor 99.91%
    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。
    LY2109761
  • HY-12273
    DMH-1 Inhibitor 99.95%
    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。
    DMH-1
  • HY-12043
    SB 525334 Inhibitor 99.97%
    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。
    SB 525334
  • HY-12071A
    LDN193189 Tetrahydrochloride Inhibitor 99.86%
    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 ALK4ALK5ALK7 的作用效果弱 (IC50≥500 nM)。
    LDN193189 Tetrahydrochloride
  • 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 ALK2ALK4 (IC50 为 17.3 nM)。Vactosertib 具有强大的抗转移活性和抗癌作用。
    Vactosertib
  • HY-10432A
    A 83-01 sodium Inhibitor ≥98.0%
    A 83-01 sodium 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。
    A 83-01 sodium
  • HY-124697
    BMP signaling agonist sb4 Agonist 99.98%
    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)。
    BMP signaling agonist sb4
  • HY-13521
    SB-505124 Inhibitor 99.99%
    SB-505124 是一种选择性的 TGF-βI 型受体 (ALK4ALK5ALK7) 抑制剂,对 ALK4ALK5 的 IC50 值分别为 129 nM 和 47 nM,对 ALK1,2,3 或 6 无作用。
    SB-505124
  • HY-13462
    LY-364947 Inhibitor 99.14%
    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。
    LY-364947
  • HY-P99355
    Bimagrumab Inhibitor 99.07%
    Bimagrumab (Anti-ACVR2B Reference Antibody) 是一种人单克隆抗体,可阻断激活素 II 型受体 (ActRII),对 ActRIIBActRIIAKD 值分别为 1.7 pM 和 434 pM。Bimagrumab 可用于病理性肌肉损失和无力的研究。
    Bimagrumab
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