dBET6是一种高效的，选择性的，细胞透过的基于PROTAC技术的BET降解剂，IC50值为14nM，具有抗肿瘤活性。
CAS：1950634-92-0
分子式：C42H45ClN8O7S
分子量：841.37
纯度：98%
存储：Store at -20°C

Background:

dBET6 is a highly potent, selective and cell-permeable degrader of BET based on PROTAC, with an IC50 of 14 nM, and has antitumor activity.

dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM. dBET6 (100 nM) exhibits antitumor activity against T cell acute lymphoblastic leukemia (T-ALL) lines via degradation of BRD4[1].

dBET6 (7.5 mg/kg, p.o., BID) reduces the leukemic burden in a disseminated mouse model of T-ALL[1].

[1]. Winter GE, et al. BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment. Mol Cell. 2017 Jul 6;67(1):5-18.e19.