1. PROTAC Epigenetics Apoptosis
  2. PROTACs Epigenetic Reader Domain c-Myc
  3. PROTAC BRD4 Degrader-46

PROTAC BRD4 Degrader-46 是一种异双功能 BRD4 PROTAC 降解剂。PROTAC BRD4 Degrader-46 可同时结合 BRD4CRBN,从而触发 BRD4 的泛素化及蛋白酶体降解。PROTAC BRD4 Degrader-46 可下调下游 BRD2BRD3MYC 的水平。PROTAC BRD4 Degrader-46 可用于多发性骨髓瘤等癌症的研究。
(粉色: BRD4 配体 (HY-78695);蓝色: Cereblon E3 连接酶配体;黑色: 连接子)。

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PROTAC BRD4 Degrader-46

PROTAC BRD4 Degrader-46 Chemical Structure

CAS No. : 2766179-68-2

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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-46 is a heterobifunctional BRD4 PROTAC degrader. PROTAC BRD4 Degrader-46 binds to both BRD4 and CRBN, thereby triggering ubiquitination and proteasomal degradation of BRD4. PROTAC BRD4 Degrader-46 downregulates the levels of downstream BRD2, BRD3 and MYC. PROTAC BRD4 Degrader-46 can be used in the research of cancers such as multiple myeloma[1]. (Pink: BRD4 ligand (HY-78695); Blue: Cereblon E3 ligase ligand; Black: linker).

IC50 & Target[1]

Cereblon

 

BRD4

 

BRD2

 

BRD3

 

体外研究
(In Vitro)

PROTAC BRD4 Degrader-46 (Compound 6) (5 h) 可通过 CRBN 依赖的机制在 HiBiT-BRD4 标记的 HEK293 细胞中强效降解 BRD4,其 DC50 为 172 nM,Dmax 达 95%[1]
PROTAC BRD4 Degrader-46 (0.003-1 μM; 5 h) 可在 NB-4 细胞中选择性降解 BRD4、BRD2、BRD3 和 MYC,不会降解与 IMiD 相关的新底物 Ikaros、Aiolos、GSPT1、CSNK1A1 和 RAB28[1]

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

分子量

712.22

Formula

C35H34ClN9O4S

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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    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:
PROTAC BRD4 Degrader-46
目录号:
HY-182801
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