MZP-55是基于PROTAC技术的一种选择性的BRD3/4降解剂，对Brd4BD2的Kd值为8nM。
CAS：2010159-48-3
分子式：C57H70ClN7O10S
分子量：1080.72
纯度：98%
存储：Store at -20°C

Background:

MZP-55 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 8 nM for Brd4BD2.

MZP-55 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 8 nM for Brd4BD2. MZP-55 binds to VHL-EloC-EloB protein (VCB) with a Kd of 105 ± 24 nM. MZP-55 shows an inhibitory activity against MV4;11 and HL60 cells, with pEC50s of 7.31 ± 0.03 and 6.57 ± 0.02, respectively[1].

[1]. Chan KH, et al. Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. J Med Chem. 2018 Jan 25;61(2):504-513.