dBET57 is a potent and selective degrader of BRD4 BD1 based on the PROTAC technology. dBET57 mediates recruitment to the CRL4 E3 ubiquitin ligase, with a DC 50/5h of 500 nM for BRD4 BD1 , and is inactive on BRD4 BD2 .
性状
Solid
IC50 & Target[1][2]
BRD4 (BD1) 500 nM (DC50)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Nowak RP, et al. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol. 2018 Jul;14(7):706-714.
溶解度数据
In Vitro: DMSO : 250 mg/mL (357.56 mM; Need ultrasonic)配制储备液