产品说明书

dBET57

Print
Chemical Structure| 1883863-52-2 同义名 : -
CAS号 : 1883863-52-2
货号 : A176193
分子式 : C34H31ClN8O5S
纯度 : 99%+
分子量 : 699.178
MDL号 : MFCD32174278
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(357.56 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • BET

    BRD4BD1, DC50:500 nM
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.43mL

0.29mL

0.14mL

7.15mL

1.43mL

0.72mL

14.30mL

2.86mL

1.43mL
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.