dBET57 是一种有效选择性的 BRD4BD1 降解剂，基于 PROTAC 技术。dBET57 介导了 E3 泛素连接酶 CRL4CRBN 的招募，对 BRD4BD1 作用的 DC50/5h 值为 500 nM，对 BRD4BD2 不起作用。
CAS：1883863-52-2
分子式：C34H31ClN8O5S
分子量：699.18
纯度：98%
存储：Store at -20°C

Background:

dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology. dBET57 mediates recruitment to the CRL4CRBN E3 ubiquitin ligase, with a DC50/5h of 500 nM for BRD4BD1, and is inactive on BRD4BD2[1]. BRD4 (BD1)|500 nM (DC50)

[1]. Nowak RP, et al. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol. 2018 Jul;14(7):706-714.