GlpBio

TGF-β / Smad Signaling

TGF-β / Smad Signaling(TGF-β / Smad 信号转导)

Transforming growth factor-beta (TGF-beta) is a multifunctional cytokine that regulates proliferation, migration, differentiation, and survival of many different cell types. Deletion or mutation of different members of the TGF-β family have been shown to cause vascular remodeling defect and absence of mural cell formation, leading to embryonic lethality or severe vascular disorders. TGF-β induces smooth muscle differentiation via Notch or SMAD2 and SMAD3 signaling in ES cells or in a neural crest stem cell line. TGF-β binds to TGF-βRI and to induce phosphorylation of SMAD2/3, thereby inhibiting proliferation, tube formation, and migration of endothelial cells (ECs).

TGF-β is a pluripotent cytokine with dual tumour-suppressive and tumour-promoting effects. TGF-β induces the epithelial-to-mesenchymal transition (EMT) leading to increased cell plasticity at the onset of cancer cell invasion and metastasis.

研究方向

TGF-β / Smad Signaling 相关产品(360)

  • GC35682 structure
    GC35682CHMFL-ABL/KIT-155
    CAS: 2081093-21-0

    CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) 是一种高效的，具有口服活性的 type II ABL/c-KIT 双激酶抑制剂 (IC50 分别为 46 nM 和 75 nM)，对 BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM), PDGFRβ (IC50=80 nM) 激酶也具有明显的抑制活性。CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) 阻止细胞周期进展和诱导细胞凋亡。

  • GC35753 structure
    GC35753CT-721
    CAS: 1388710-60-8

    CT-721 是一种有效的，时间依赖性的 Bcr-Abl 激酶抑制剂，抑制野生型 Bcr-Abl 激酶的 IC50 值为 21.3 nM，具有抗慢性骨髓白血病 (CML) 活性。

  • GC35812 structure
    GC35812Dasatinib hydrochloride
    CAS: 854001-07-3
    纯度: >98.50% / >99.00%

    An inhibitor of Abl and Src

  • GC35897 structure
    GC35897DPH
    CAS: 484049-04-9
    纯度: >98.00%

    DPH是一种具有细胞渗透性的小分子c-Abl激酶激活剂。

  • GC36167 structure
    GC36167GMB-475
    CAS: 2490599-18-1
    纯度: >99.00%

    GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.

  • GC36207 structure
    GC36207H-1152
    CAS: 451462-58-1

    A ROCK inhibitor

  • GC36208 structure
    GC36208H-1152 dihydrochloride
    CAS: 871543-07-6
    纯度: >99.50%

    H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.

  • GC36282 structure
    GC36282Hypocrellin A
    CAS: 77029-83-5
    纯度: >98.00%

    A perylenequinoid with diverse biological activities

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

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

  • GC36807 structure
    GC36807ON 146040
    CAS: 1404231-34-0

    ON 146040 是一种有效的 PI3Kα 和 PI3Kδ 抑制剂，IC50 分别约为 14 和 20 nM。ON 146040 也抑制 Abl1 (IC50<150 nM)。

  • GC36833 structure
    GC36833p32 Inhibitor M36
    CAS: 802555-85-7
    纯度: >98.00%

    p32 inhibitor M36 (M36) 是一种 p32 线粒体蛋白小分子抑制剂，可直接与 p32 结合，抑制 p32 与 LyP-1 的结合。

  • GC36974 structure
    GC36974Procyanidin A1
    CAS: 103883-03-0
    纯度: >99.00%

    原花青素 A1 (Proanthocyanidin A1) 是一种原花青素二聚体，抑制蛋白激酶 C 激活下游脱粒或 RBL-213 细胞内部储存的 Ca2+ 流入。原花青素 A1 具有抗过敏作用。

  • GC37014 structure
    GC37014Protein Kinase C 19-31
    CAS: 121545-65-1
    纯度: >98.00%

    Protein Kinase C (19-31)是蛋白激酶 C (PKC)的抑制剂,是由 PKCa (残基 19-31) 伪底物调控域衍生而来，25 位丝氨酸取代野生型丙氨酸作为蛋白激酶 C 底物肽，用于检测蛋白激酶 C 的活性。Protein kinase C (PKC) 通过磷酸化丝氨酸和苏氨酸氨基酸残基上的羟基来调控其它蛋白的功能。

  • GC37015 structure
    GC37015Protein Kinase C 19-36
    CAS: 113731-96-7

    Protein Kinase C (19-36) 是蛋白激酶 C (PKC) 的伪底物肽抑制剂，其IC50 值为 0.18 μM。Protein Kinase C (19-36) 有效减缓血管增生和肥大，抑制葡萄糖诱导的利钠肽受体反应。

  • GC37534 structure
    GC37534Ripasudil free base
    CAS: 223645-67-8

    Ripasudil free base (K-115 free base) 是 ROCK 特异性抑制剂，能够抑制 ROCK2 和 ROCK1 的活性，IC50 值分别为 19 和 51 nM。

  • GC37551 structure
    GC37551ROCK inhibitor-2
    CAS: 1127308-52-4
    纯度: >98.00% / >99.50%

    ROCK inhibitor-2是一种选择性Rho激酶（ROCK）抑制剂，抑制ROCK1和ROCK2的IC 50 值分别为17nM和2nM，具有抗肿瘤活性。

  • 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。

  • GC37947 structure
    GC37947Y-33075
    CAS: 199433-58-4
    纯度: >98.00%

    Y-33075是一种有效的ROCK（Rho相关蛋白激酶）抑制剂，IC 50 值为3.6nM。

  • GC38186 structure
    GC38186Daphnoretin
    CAS: 2034-69-7
    纯度: >99.50%

    A coumarin with diverse biological activities

  • GC38388 structure
    GC38388DCPLA-ME
    CAS: 56687-67-3
    纯度: >98.00%

    DCPLA-ME 是 DCPLA 的甲酯形式。DCPLA-ME 是一种有效的 PKCε 激活剂。DCPLA-ME 可用于治疗神经退行性疾病。

  • GC38482 structure
    GC38482Desmethylglycitein
    CAS: 17817-31-1

    An active metabolite of daidzein

  • GC38791 structure
    GC38791GSK-25
    CAS: 874119-56-9
    纯度: >99.50%

    GSK-25 是一种有效的、选择性的，具有口服活性的 ROCK1 抑制剂 (IC50=7 nM)。GSK-25 对 31 种激酶以及 RSK1 和 p70S6K 保持良好的选择性 (RSK1: IC50=398 nM, p70S6K: IC50=1 μM)。GSK-25 可抑制 P450 (CYP2C9、CYP2D6、CYP3A4的IC50 分别为2.5、5.2、2.5 μM)。

  • GC38898 structure
    GC38898CCG-222740
    CAS: 1922098-69-8
    纯度: >99.50%

    CCG-222740 is a Rho/MRTF pathway inhibitor. CCG-222740 decreases the activation of stellate cells in vitro and in vivo, by reducing the levels of alpha smooth muscle actin(α-SMA) expression.

  • GC38931 structure
    GC38931N-Desmethyltamoxifen hydrochloride
    CAS: 15917-65-4
    纯度: >99.50%

    N-Desmethyltamoxifen hydrochloride (N-Desmethyl tamoxifen HCl), the primary metabolite of tamoxifen, is an estrogen response modifer and protein kinase C inhibitor with IC50 of 25 ?M.