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)

  • GC32728 structure
    GC32728LSKL, Inhibitor of Thrombospondin TSP-1
    CAS: 283609-79-0
    纯度: >98.00% / >99.50%

    LSKL, Inhibitor of Thrombospondin TSP-1是一种来源于潜伏相关蛋白（LAP）-TGFβ的四肽，可竞争性结合抑制TGF-β1。

  • GC32788 structure
    GC32788SJ000291942
    CAS: 425613-09-8
    纯度: >98.00%

    A BMP signaling activator

  • GC32840 structure
    GC32840R-268712
    CAS: 879487-87-3
    纯度: >99.50%

    R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.

  • GC34493 structure
    GC34493BIBF0775
    CAS: 334951-90-5
    纯度: >99.50%

    BIBF-0775 is a selective inhibitor of transforming growth factor β Receptor I (TGFβRI,Alk5) with an IC50 of 34nM.

  • GC35210 structure
    GC35210A 83-01 sodium salt
    CAS: 2828431-89-4
    纯度: >98.00%

    A TGF-β type I receptor inhibitor

  • GC36433 structure
    GC36433LDN193189 Tetrahydrochloride
    CAS: 2310134-98-4
    纯度: >98.00%

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

  • GC37880 structure
    GC37880Vactosertib Hydrochloride
    CAS: 1352610-25-3

    Vactosertib Hydrochloride (EW-7197 Hydrochloride) 是 TGFβRI (ALK5) 的小分子 ATP 竞争性抑制剂，其 IC50 值为 12.9 nM。

  • GC39398 structure
    GC39398LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)
    纯度: >98.00%

    LSKL, Inhibitor of Thrombospondin TSP-1是一种来源于潜伏相关蛋白（LAP）-TGFβ的四肽，可竞争性结合抑制TGF-β1。

  • GC44303 structure
    GC44303N-Acetylpuromycin
    CAS: 22852-13-7
    纯度: >98.00%

    A non-ribotoxic form of puromycin

  • GC50317 structure
    GC50317IN 1130
    CAS: 868612-83-3
    纯度: >98.00%

    IN 1130 是一种高度选择性的转化生长因子-β I 型受体激酶 (ALK5) 抑制剂，对 ALK5 介导的 Smad3 磷酸化的 IC50 为 5.3 nM。

  • GC50589 structure
    GC50589AZ 12799734
    CAS: 1117684-36-2

    AZ 12799734 是一种选择性的、口服活性的 TGFBR1 激酶抑制剂，IC50 为 47 nM。

  • GC50593 structure
    GC50593BMP signaling agonist sb4
    CAS: 100874-08-6
    纯度: >98.00%

    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 来激活 BMP 信号传导。 BMP 信号激动剂 sb4 激活 BMP4 靶基因（DNA 结合抑制剂，Id1 和 Id3）经典 BMP 信号。

  • GC60210 structure
    GC60210Isosaponarin
    CAS: 19416-87-6
    纯度: >99.50%

    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。

  • GC62146 structure
    GC62146XST-14
    CAS: 2607143-50-8
    纯度: >99.50%

    XST-14 是一种有效的，竞争性强且高度选择性的 ULK1 抑制剂，IC50 为 26.6 nM。XST-14 通过减少 ULK1 下游底物的磷酸化来诱导自噬抑制。XST-14 诱导肝细胞癌 (HCC) 细胞凋亡，并具有抗肿瘤作用。

  • GC62868 structure
    GC62868BIO-013077-01
    CAS: 746667-48-1
    纯度: >98.00%

    BIO-013077-01 是一种吡唑类的 TGF-β 抑制剂。

  • GC65294 structure
    GC65294ALK2-IN-2
    CAS: 2254409-25-9
    纯度: >99.00%

    ALK2-IN-2 是一种有效的、选择性的活化素受体样激酶 2 (ALK2) 抑制剂，IC50 值为 9 nM，对 ALK2 的抑制作用是 ALK3 的 700 倍。

  • GC65329 structure
    GC65329EW-7195
    CAS: 1352609-28-9
    纯度: >99.00%

    EW-7195 是一种有效的、选择性 ALK5 (TGFβR1) 抑制剂，IC50 为 4.83 nM。EW-7195 对 ALK5 的选择性是 p38α 的 300 多倍。EW-7195 能有效抑制 TGF-β1 诱导的 Smad 信号转导、上皮间质转化 (EMT) 和乳腺癌向肺转移。

  • GC65539 structure
    GC65539Fresolimumab
    CAS: 948564-73-6
    纯度: >99.50% / >95.00%

    Fresolimumab是一种高亲和力的人源化单克隆抗体，能够结合并抑制蛋白转化生长因子β（TGFβ）的所有亚型。Fresolimumab对TGFβ1、TGFβ2和TGFβ3的K d 值分别为1.7±0.6nM、3.0±1.2nM、2.0±1.2nM。

  • GC72815 structure
    GC72815Itacnosertib (hydrocholide)
    CAS: 2409543-84-4
    纯度: >99.00%

    Itacnosertib (hydrocholide)是JAK2、ACVR1、ALK2和ALK5的抑制剂。

  • GC72917 structure
    GC72917BUR1
    CAS: 23000-46-6
    纯度: >99.00%

    BUR1是BMP上调剂（EC50:98nM），并激活BMPRII信号传导。

  • GC73292 structure
    GC73292THRX-144644
    CAS: 2442519-59-5
    纯度: >99.00%

    THRX-144644是肺限制性ALK5抑制剂，IC50值为0.14 nM。

  • GC73338 structure
    GC73338ALK5-IN-34
    CAS: 2785430-90-0
    纯度: >98.00%

    ALK5-IN-34是一种选择性口服活性激活素受体样激酶（ALK）抑制剂。

  • GC73535 structure
    GC73535BMPR2-IN-1 TFA
    纯度: >99.00%

    BMPR2-IN-1 TFA（化合物8a）是一种BMPR2抑制剂，IC50为506 nM， KD为83.5 nM。

  • GC74516 structure
    GC74516Bintrafusp alfa
    CAS: 1918149-01-5
    纯度: >97.00%

    Bintrafusp alfa（M 7824）是一种一流的双功能融合蛋白，由TGF-βRII的细胞外结构域与阻断程序性细胞死亡配体的人IgG1单克隆抗体融合而成。