PROTAC BRD4 Degrader-7 | whatman (沃特曼)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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。

PROTAC BRD4 Degrader-7 Chemical Structure

CAS No. : 2413382-30-4

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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].

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

475.61

Formula

C₂₆H₂₉N₅O₂S

CAS 号

2413382-30-4

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.

参考文献

[1]. Robert Anthony BLAKE, et al. Tert-butyl (s)-2-(4-(phenyl)-6h-thieno[3,2-f][1,2,4]triazolo[4,3-a] [1,4]diazepin-6-yl) acetate derivatives and related compounds as bromodomain brd4 inhibitors for treating cancer. WO2020055976A1.

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