1. TGF-beta/Smad Stem Cell/Wnt
  2. TGF-β Receptor TGF-beta/Smad
  3. TGFβRII-IN-3

TGFβRII-IN-3 (Compound 2r) 是一种选择性的 TGFβ 类型 II 受体 (TGFβ RII) 的抑制剂 (IC50= 4.1 μM)。其通过促进 TGFβ RII 的蛋白质降解来抑制 TGFβ 信号传导。TGFβRI-IN-7 可以阻断内皮向间充质的转变和细胞迁移。TGFβRI-IN-7 还能够用于癌症研究。

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TGFβRII-IN-3 Chemical Structure

TGFβRII-IN-3 Chemical Structure

CAS No. : 2351149-20-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TGFβRII-IN-3 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) (IC50 = 4.1 μM). TGFβRII-IN-3 inhibits TGFβ signaling by promoting the proteolytic degradation of TGFβ RII. TGFβRII-IN-3 can block endothelial-to-mesenchymal transition and cell migration. TGFβRII-IN-3 can be used in cancer research[1].

IC50 & Target[1]

TGF-βR2

4.1 μM (IC50)

体外研究
(In Vitro)

TGFβRII-IN-3 (5-15μM; 24 h) 通过降低 A549 细胞中的 Smad2 的磷酸化水平来抑制 TGFβ 信号通路的活性。并且对 TGFβ RII 的选择性降解作用[1]
TGFβRII-IN-3 (2.5-10 μM; 48 h) 能有效抑制 A549 细胞中的由 TGFβ1 诱导的 E-cadherin 丢失,同时抑制 Snail 和 N-cadherin 的上调[1]
TGFβRII-IN-3 (5 μM; 48h) 通过抑制 A549 和 H1299 细胞对 TGFβ 信号传导,从而抑制了细胞迁移和形态变化[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: A549 cell
Concentration: 5;10;15 μM
Incubation Time: 24h
Result: Significantly and dose-dependently inhibited TGFβ1-induced phosphorylation of Smad2 in A549 cells.
Significantly reduced the steady-state levels of TβRII in a dose-dependent manner. At the same time, the levels of TGFβ type I receptor were not significantly affected.
分子量

468.51

Formula

C27H27F3N2O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
TGFβRII-IN-3
目录号:
HY-161398
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