GlpBio

TGF-β Receptor

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.

TGF-β Receptor 相关产品(49)

  • GC10166 structure
    GC10166A 83-01
    CAS: 909910-43-6
    纯度: >98.00%

    A 83-01 是 TGF-β I 型受体 ALK5 激酶、I 型淋巴结受体 ALK4 和 I 型淋巴结受体 ALK7 的有效抑制剂，IC50 s 分别为 12 nM、45 nM和 7.5 nM 分别抑制 ALK5、ALK4 和 ALK7 诱导的转录。

  • GC10421 structure
    GC10421SB-505124 hydrochloride
    CAS: 356559-13-2

    SB-505124 hydrochloride是一种选择性TGF-β I型受体（ALK4、ALK5、ALK7）抑制剂，对ALK4和ALK5的IC 50 值分别为129nM和47nM。

  • GC11545 structure
    GC11545SB 431542
    CAS: 301836-41-9
    纯度: >98.00%

    SB-431542是一种小分子抑制剂，可以阻止TGF-β受体类型I的内部介导物，从而降低TGF-β1介导的增殖、细胞因子和胶原蛋白表达。

  • GC11604 structure
    GC11604LY364947
    CAS: 396129-53-6
    纯度: >99.00%

    LY364947是一种强效的ATP竞争性TGFβR-I抑制剂，其IC 50 为59nM。

  • GC11878 structure
    GC11878GW788388
    CAS: 452342-67-5
    纯度: >99.50%

    GW788388是一种有效的、选择性ALK5抑制剂（IC 50 =18nM）。GW788388还抑制TGF-βII型受体（IC 50 =93nM）和激活素II型受体的活性，但不抑制BMP II型受体。

  • GC12108 structure
    GC12108ITD 1
    CAS: 1099644-42-4
    纯度: >99.50%

    ITD 1是一种选择性TGFβ受体抑制剂（IC 50 = 460nM）。

  • GC12363 structure
    GC12363LY2109761
    CAS: 700874-71-1
    纯度: >99.50%

    LY2109761是一种口服小分子双TGF-β受体（TβR）I/II激酶抑制剂（TβRI: K i = 38nM；TβRII: K i = 300nM）。

  • GC12560 structure
    GC12560Dorsomorphin (Compound C) 2HCl
    CAS: 1219168-18-9
    纯度: >99.50% / >98.00%

    IC50:Dorsomorphin 以剂量依赖性方式抑制 BMP4 诱导的 BMP 反应性 SMAD 磷酸化（半数最大抑制浓度 (IC50) =0.47 mM）。

  • GC13225 structure
    GC13225LDN-214117
    CAS: 1627503-67-6
    纯度: >99.50%

    A selective ALK1 and ALK2 inhibitor

  • GC13354 structure
    GC13354EW-7197
    CAS: 1352608-82-2
    纯度: >99.00%

    EW-7197是一种口服有效的丝氨酸/苏氨酸激酶抑制剂，靶向转化生长因子（TGF）-β受体I（TGFBR1），也称为激活素受体样激酶5（ALK5），其IC 5 0 值为12.9nM。

  • GC13769 structure
    GC13769SB505124
    CAS: 694433-59-5
    纯度: >99.50%

    SB505124是一种选择性TGF-β I型受体（ALK4、ALK5、ALK7）抑制剂，对ALK4和ALK5的IC 50 值分别为129nM和47nM。

  • GC13904 structure
    GC13904SD-208
    CAS: 627536-09-8
    纯度: >99.00%

    A potent, selective inhibitor of TGF-βRI

  • GC13927 structure
    GC13927A 77-01
    CAS: 607737-87-1
    纯度: >99.50%

    A potent ALK5 inhibitor

  • GC14298 structure
    GC14298DMH-1
    CAS: 1206711-16-1
    纯度: >99.50% / >99.00%

    A potent ALK2 inhibitor

  • GC14349 structure
    GC14349SB525334
    CAS: 356559-20-1
    纯度: >99.50% / >98.00%

    SB525334已被鉴定为一种高效且选择性的转化生长因子β1（TGF-β1）受体、活化素受体样激酶（ALK5）抑制剂。SB525334对ALK5激酶活性的IC 50 为14.3nM。

  • GC15567 structure
    GC15567K02288
    CAS: 1431985-92-0
    纯度: >98.00%

    A BMP signaling inhibitor

  • GC16580 structure
    GC16580LDN-193189
    CAS: 1062368-24-4
    纯度: >99.00%

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

  • GC16793 structure
    GC16793RepSox
    CAS: 446859-33-2
    纯度: >98.00%

    RepSox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，IC 50 为23nM。RepSox抑制ALK5自身磷酸化，IC 50 值为4nM。

  • GC17035 structure
    GC17035LDN-212854
    CAS: 1432597-26-6
    纯度: >98.00%

    An ALK2 inhibitor

  • GC17243 structure
    GC17243Dorsomorphin (Compound C)
    CAS: 866405-64-3
    纯度: >99.50% / >98.00%

    Dorsomorphin（Compound C）是一种细胞渗透的AMPK抑制剂。

  • GC17582 structure
    GC17582ML347
    CAS: 1062368-49-3
    纯度: >98.00%

    A selective ALK1 and ALK2 inhibitor

  • GC18015 structure
    GC18015LY2157299
    CAS: 700874-72-2
    纯度: >99.50%

    LY2157299是一种口服的、选择性TGF-β受体I型（TGF-βRI）激酶抑制剂，IC 50 值为56nM。

  • GC19234 structure
    GC19234LY3200882
    CAS: 1898283-02-7
    纯度: >99.50%

    An inhibitor of TGF-βRI

  • GC19447 structure
    GC19447SM 16
    CAS: 614749-78-9
    纯度: >99.50%

    An inhibitor of ALK5