TD-428

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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。

TD-428 

TD-428是由Cereblon配体和BRD4配体相连的PROTAC。TD-428 是一种高度特异的 BRD4 降解剂，DC50 为 0.32 nM。TD-428 是一种 BET PROTAC，其中 TD-106 (CRBN 配体) 连接到 JQ1 (BET 抑制剂)，TD-428 可有效诱导 BET 蛋白降解。

TD-428

TD-428 Chemical Structure

CAS No. : 2334525-50-5

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生物活性

TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM[1]. TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation[1].

IC50 & Target[1]

BRD4

0.32 nM (DC50)

Cereblon

 

体外研究
(In Vitro)

TD-428, which comprises TD-106 linked to a BET inhibitor, JQ1 efficiently induce BET protein degradation in the prostate cancer cell line 22Rv1[1].
TD-428 (0.01-10,000 nM; 72 hours) inhibits the proliferation of 22RV1 cells with a CC50 of  20.1 nM[1].
TD-428 (1 nM-10 μM; 12 hours) induces the degradation of BRD4, IKZF1, and IKZF3 proteins[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: 22RV1 cells
Concentration: 0.01, 0.1, 1, 10, 100, 1000, and 10000 nM
Incubation Time: 72 hours
Result: Inhibited cell proliferation with a CC50 of 20.1 nM.

Western Blot Analysis[1]

Cell Line: U266 cells
Concentration: 1 nM, 10 nM, 100 nM, 1000 nM, and 10 μM
Incubation Time: 12 hours
Result: Induced the degradation of BRD4, IKZF1, IKZF3 proteins.

分子量

879.38

Formula

C43H43ClN10O7S
CAS 号

2334525-50-5
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]. Kim SA, et al. A novel cereblon modulator for targeted protein degradation. Eur J Med Chem. 2019 Mar 15;166:65-74.

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