|2-((S)-4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-f][1,2,4]三唑并[4,3-a][1,4]二氮杂卓-6-基)-N-(2-((2-(2,6-二氧代哌啶-3-基)-1,3-双氧代异吲哚啉-4-基)氨基)乙基)乙酰胺|CsnPharm

CAS No.: 1883863-52-2

dBET57 Catalog No. CSN22300

Synonyms: dBET57

dBET57 is a BRD4 heterobifunctional small-molecule ligand (PROTAC), exhibits significant and selective degradation of BRD4 BD1 (DC50/5h=500 nM), but is inactive on BRD4 BD2.

规格	价格	促销价格	库存	数量

400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述BRD4 belongs to bromodomain and extra-terminal domain (BET) family, that reads and translates epigenetic marks into transcription. BRD4 contains two bromodomain, BRD4D1 and BRD4D2, which tightly binds to chromosomes during mitosis and affects gene expression in the newly divided cells. dBET57 is a potent and selective degrader of BRD4BD1 with DC50/5h value of 500nM, but is inactive on BRD4BD2. dBET57 exhibits negative cooperativity and a preference for binding to BRD4BD1 with IC50[binary]/IC50[ternary] value of 0.8^[1].
参考文献

[1] Nowak RP. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol. 2018 Jul;14(7):706-714. doi: 10.1038/s41589-018-0055-y. Epub 2018 Jun 11.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.4302 mL
- 7.1512 mL
- 14.3025 mL
- 5 mM
- 0.2860 mL
- 1.4302 mL
- 2.8605 mL
- 10 mM
- 0.1430 mL
- 0.7151 mL
- 1.4302 mL

技术信息

CAS号

1883863-52-2

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C34H31ClN8O5S

运输

蓝冰

分子量

699.18

别名

dBET57

溶解度

DMSO	136.67 mg/mL (195.5 mM)
Water	insoluble

动物实验配方

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