PROTAC BRD4 Degrader-15

发表于由

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-15 

PROTAC BRD4 Degrader-15 是一种由von Hippel-Lindau配体和BRD4配体相连的PROTAC，对 BRD4 BD1 和 BD2 的 IC50 值分别为 7.2 nM 和 8.1 nM。PROTAC BRD4 Degrader-15 能够有效降解 PC3 前列腺癌细胞中的 BRD4 蛋白。

PROTAC BRD4 Degrader-15

PROTAC BRD4 Degrader-15 Chemical Structure

CAS No. : 2417370-67-1

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生物活性

PROTAC BRD4 Degrader-15 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 7.2 nM and 8.1 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-15 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells[1].

IC50 & Target[1]

BRD4 BD1

7.2 nM (IC50)

BRD4 BD2

8.1 nM (IC50)

体外研究
(In Vitro)

PROTAC BRD4 Degrader-15 (compound 13) (4 h) inhibits suppresses MYC gene transcript in MV4-11 AML cells, with an IC50 of 15 nM[1].
PROTAC BRD4 Degrader-15 (6 days) inhibits the proliferation of HL-60 and PC3-S1 cells, with an IC50 of 4.2 nM and 91 nM[1].

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

1149.29

Formula

C57H62F2N10O10S2
CAS 号

2417370-67-1
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]. Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64(5):2576-2607.

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