2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain c-Myc
  4. PROTAC BET Degrader-14

PROTAC BET Degrader-14 是一种高效的 PROTAC，靶向 BET (溴结构域和末端结构域)。PROTAC BET Degrader-14 可以降解所有 BET (BRD2、BRD3、BRD4) 家族蛋白。PROTAC BET Degrader-14 能有效降解 U2OS 骨肉瘤细胞系 (BRD4 DC50 = 130 nM) 和 KYSE180 食管鳞状细胞癌细胞系 (DC50 = 40 nM) 中的 BET 蛋白。PROTAC BET Degrader-14 的降解依赖于泛素-蛋白酶体系统。PROTAC BET Degrader-14 可降低 BET 调控基因产物 c-Myc、RUNX2 和 KRT14 的表达水平。PROTAC BET Degrader-14 可用于骨肉瘤的研究。
(粉色: BRD4 配体 (HY-78695)；蓝色: Ligands for E3 Ligase 配体 (HY-149452)；黑色: 连接子)。

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PROTAC BET Degrader-14

PROTAC BET Degrader-14 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

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PROTAC BET Degrader-14 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC BET Degrader-14 is a highly efficient PROTAC targeting BET (bromodomain and extra-terminal domain). PROTAC BET Degrader-14 can degrade all BET (BRD2, BRD3, BRD4) family proteins. PROTAC BET Degrader-14 potently degrades BET proteins in U2OS osteosarcoma cell lines (BRD4 DC50 = 130 nM) and KYSE180 esophageal squamous cell carcinoma cell lines (DC50 = 40 nM). PROTAC BET Degrader-14’s dependence on the ubiquitin-proteasome system. PROTAC BET Degrader-14 decreases levels of BET-regulated gene products c-Myc, RUNX2, and KRT14. PROTAC BET Degrader-14 can be used for the study of osteosarcoma[1]. (Pink: BRD4 ligand (HY-78695); Blue: Ligands for E3 Ligase ligand (HY-149452); Black: linker).

IC50 & Target[1]

BRD4

130 nM (DC50)

BRD4

40 nM (DC50)

BRD2

 

BRD3

 

体外研究
(In Vitro)

PROTAC BET Degrader-14 (Compound 105B) (0.01-10 μM，24 小时) 呈剂量依赖性地降解 U2OS 骨肉瘤细胞中的 BRD4[1]。
PROTAC BET Degrader-14 (10 nM，0-24 小时) 可诱导 U2OS 骨肉瘤细胞中 BRD4 的快速降解，但由于 BRD4 的重新合成，这种作用可能会反弹[1]。
PROTAC BET Degrader-14 (0.01 nM-1 μM，24 小时) 可降低 U2OS 骨肉瘤细胞中 c-Myc 和 RUNX2 的表达水平[1]。
PROTAC BET Degrader-14 (0.51 nM-10 μM) 可降低 KYSE180 食管鳞状细胞癌细胞中 KRT14 的表达水平，但不降解 BRDT[1]。

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

PROTAC BET Degrader-14 相关抗体:

Western Blot Analysis[1]

Cell Line: U2OS osteosarcoma cells
Concentration: 10 nM
Incubation Time: 0 h, 0.5 h, 1 h, 1.5 h, 2 h, 4 h, 6 h, 8 h, 24 h
Result: BRD4 degradation occurs within 4 hours and rebounds after 24 hours.
分子量

1161.80

Formula

C59H73ClN12O9S
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

PROTAC BET Degrader-14 相关分类

  • 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.

Keywords:

PROTAC BET Degrader-14PROTAC BET Degrader14PROTAC BET Degrader 14PROTACsEpigenetic Reader Domainc-MycMycPROTACUbiquitin-proteasome systemUPSRUNX2KRT14Inhibitorinhibitorinhibit

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