1. Antibody-drug Conjugate/ADC Related Epigenetics
  2. Epigenetic Reader Domain ADC Cytotoxin
  3. EBET-1055

EBET-1055 是一种溴结构域和额外末端 (BET) 蛋白质降解剂 (EBET),由 BET 抑制剂 (EBET-590,HY-161387)、E3 泛素连接酶配体和接头组成。EBET-1055 能有效抑制胰腺导管腺癌 (PDAC) 生长。EBET-1055 还同时调节癌症相关成纤维细胞 (CAF) 活性,上调类器官共培养物中所有报告基因活性。

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EBET-1055 Chemical Structure

EBET-1055 Chemical Structure

1.  客户无需承担相应的运输费用。

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     可免费申领三个不同产品的试用装。

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EBET-1055 is a bromodomain and extra-terminal (BET) protein degrader (EBET) composed of a BET inhibitor (EBET-590, HY-161387), an E3 ubiquitin ligase ligand and connectors. EBET-1055 effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC). EBET-1055 also simultaneously modulates cancer-associated fibroblast (CAF) activity, upregulating all reporter gene activities in organoid co-cultures[1].

体外研究
(In Vitro)

EBET-1055 (1 nM, 10 nM; 2 d) 在小鼠 CAF 与 PC-3 或 PC-42 癌细胞的共培养时,抑制 CAF 受诱导而出现的 IL-6 和 LIF 分泌[1]
EBET-1055 具有潜在抗炎或抗纤维化活性。STAT3 信号介导炎症性 CAF (iCAF) 表型,SMAD 信号介导肌成纤维细胞 CAF (myCAF) 表型;而 EBET-1055 (1-100 nM; 24 h) 可能抑制 BRD 蛋白与 STAT3SMAD3 相互作用,抑制肌成纤维细胞分化,并降低小鼠纤维化肾中 SMAD3STAT3 的磷酸化水平[1]

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

Western Blot Analysis[1]

Cell Line: PC-3 cells or mouse CAFs
Concentration: 0.1, 1, 10, 100 nM
Incubation Time: 24 h
Result: Decreased the phosphorylation levels of STAT3Y705, SMAD2S465/467, and SMAD3S423/425 24 h after addition.
分子量

923.02

Formula

C51H54N8O9

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 *
= × ×

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:
EBET-1055
目录号:
HY-161346
需求量: