1. PROTAC Epigenetics Apoptosis
  2. PROTACs Epigenetic Reader Domain Apoptosis
  3. PROTAC BRD4 Degrader-17

PROTAC BRD4 Degrader-17 (compound 13i) 是一种有效的 PROTAC BRD4 降解剂,IC50 值为 29.54 nM (BRD4 (BD1) ) 和 3.82 nM (BRD4 (BD2))。 PROTAC BRD4 Degrader-17 显著减弱 G2/M 进程相关的细胞周期蛋白 B1 (Cyclin B1) 表达。 PROTAC BRD4 Degrader-17 显著诱导 MV-4-11 细胞细胞凋亡 (apoptosis)。

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PROTAC BRD4 Degrader-17 Chemical Structure

PROTAC BRD4 Degrader-17 Chemical Structure

CAS No. : 2585561-49-3

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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-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells[1].

IC50 & Target

BRD4 (BD2)

3.82 ± 0.0 nM (IC50)

BRD4 (BD1)

29.54 ± 2. nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MV4-11 IC50
10.67 nM
Compound: 13i
Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK8 assay
[PMID: 35395439]
体外研究
(In Vitro)

PROTAC BRD4 Degrader-17 (compound 13i) (100 nM,4-24 h) 在MV-4-11细胞中 4 h以 100 nM 的浓度显着诱导 BRD4 L 和 BRD4 S 降解,然后像 dBET6 一样在 24 h 恢复 BRD4 S[1]

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

分子量

877.94

Formula

C49H47N7O9

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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  • 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:
PROTAC BRD4 Degrader-17
目录号:
HY-143328
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