1. Epigenetics PROTAC
  2. PROTACs Epigenetic Reader Domain Ligands for Target Protein for PROTAC
  3. PROTAC BRD4 Degrader-7

PROTAC BRD4 Degrader-7 是一种有效的溴结构域 BRD4 降解剂,对 BRD4-BD1 和 BRD4-BD2 的 IC50 分别为 15.5 和 12.3 nM。详细信息请参见专利 WO2020055976A1,example 1a。

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PROTAC BRD4 Degrader-7 Chemical Structure

PROTAC BRD4 Degrader-7 Chemical Structure

CAS No. : 2413382-30-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC BRD4 Degrader-7 is a potent bromodomain BRD4 degrader extracted from patent WO2020055976A1, example 1a, has IC50s of 15.5 and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively[1]. PROTAC BRD4 Degrader-7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target[1]

BRD4 BD1

15.5 nM (IC50)

BRD4 BD2

12.3 nM (IC50)

体外研究
(In Vitro)

PROTAC BRD4 Degrader-7 shows an IC50 of 27.1 nM in BRD4 Full Length Binding assay. PROTAC BRD4 Degrader-7 degrades BRD4 with an EC50 of 1.4 nM for PC3-Steapl cells and an IC50 of 1.3 nM for EoL-1 Cells. PROTAC BRD4 Degrader-7 inhibits PC-3-STEAP-1 and EoL-l proliferation with IC50s of 6.6 and 2.2 nM, respectively. PROTAC BRD4 Degrader-7 inhibits MYC expression in MV-4-11 cells with an IC50 of 2.9 nM[1].

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

分子量

475.61

Formula

C26H29N5O2S

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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产品名称:
PROTAC BRD4 Degrader-7
目录号:
HY-136857
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