PROTAC BRD4 Degrader-1

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2133360-00-4

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

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。

生物活性

PROTACBRD4 Degrader-1 is aPROTACconnected by ligands forCereblonandBRD4with anIC₅₀of 41.8 nM againstBRD4BD1.PROTACBRD4 Degrader-1 can effectively degradeBRD4proteinand suppressc-Mycexpression^[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 IC₅₀value 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].

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.