1. Stem Cell/Wnt
  2. YAP
  3. TEAD-IN-21

TEAD-IN-21 是一种强效且口服有效的泛 TEAD 抑制剂,其 IC50 为 3 nM。TEAD-IN-21 可有效抑制 Huh-7 细胞的增殖。TEAD-IN-21 选择性下调 TEAD 依赖的下游基因。TEAD-IN-21 在肝癌衍生肿瘤异种移植小鼠模型中实现了肿瘤消退。TEAD-IN-21 可用于肝细胞癌 (HCC) 的研究。

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TEAD-IN-21

TEAD-IN-21 Chemical Structure

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查看 YAP 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TEAD-IN-21 is a potent and orally active pan-TEAD inhibitor with an IC50 of 3 nM. TEAD-IN-21 effectively inhibited the proliferation of Huh-7 cells. TEAD-IN-21 selectively downregulates TEAD-dependent downstream genes. TEAD-IN-21 achieves tumor regression in a liver cancer-derived tumor xenograft mice model. TEAD-IN-21 can be used in the research of hepatocellular carcinoma (HCC)[1].

IC50 & Target[1]

TEAD

3 nM (IC50)

体外研究
(In Vitro)

TEAD-IN-21 (Compound C11) (0.1-100 μM) 对 Bel-7402、SNU182 和 Li-7 细胞具有中等抑制作用,对 Huh-7 细胞的抑制作用最佳[1]
TEAD-IN-21 (0.3-40 μM, 14 days) 显著降低这些细胞的克隆形成,而对 TEAD 不敏感的肝癌细胞系活性极小[1]
TEAD-IN-21 (0-40 μM) 具有剂量依赖性下调 TEAD 下游基因转录水平的作用[1]

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

体内研究
(In Vivo)

TEAD-IN-21 (Compound C11) (50 mg/kg,口服,每日一次,连续 20 天) 可在小鼠模型中有效抑制 Huh-7 异种移植瘤的生长[1]

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

分子量

412.39

Formula

C16H15F3N6O2S

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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:
TEAD-IN-21
目录号:
HY-178098
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