PROTAC BRD4 Degrader-1 | 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-1

PROTAC BRD4 Degrader-1 是由Cereblon配体和BRD4配体相连的PROTAC，抑制 BRD4 BD1 的 IC₅₀ 为 41.8 nM。PROTAC BRD4 Degrader-1 可以有效降解 BRD4 蛋白并抑制 c-Myc 表达。

PROTAC BRD4 Degrader-1 Chemical Structure

CAS No. : 2133360-00-4

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生物活性

PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC₅₀ of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression^[1].

IC₅₀ & Target

BRD4 (BD1)

41.8 nM (IC₅₀)

体外研究
(In Vitro)

PROTAC BRD4 Degrader-1 (compound 21) (2.5 μM; 24 hours) shows high inhibitory activity against the growth of human monocyte lymphoma cell line THP-1, with the IC₅₀ value of 0.81 μM, and moderate activity against Raji and HL-60 cell lines^[1].
PROTAC BRD4 Degrader-1 (1 μM; 24 hours) effectively induces the degradation of BRD4 protein and suppression of c-Myc, while pomalidomide couldn’t degrade BRD4 at the low concentration^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	HL-60, Raji and THP-1 cell
Concentration:	2.5 μM
Incubation Time:	24 hours
Result:	Inhibited HL-60, Raji and THP-1 cell growth.

Western Blot Analysis^[1]

Cell Line:	THP-1 cell
Concentration:	1 μM
Incubation Time:	3 hours
Result:	Degraded BRD4 protein and suppressed c-Myc expression.

分子量

771.78

Formula

C₄₀H₃₇N₉O₈

CAS 号

2133360-00-4

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]. Zhang F, et al. Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide.Bioorg Med Chem. 2020 Jan 1;28(1):115228.

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