BRD4degraderAT1是基于PROTAC技术的一种高度选择性的Brd4降解剂，在细胞中对Brd4BD2的Kd值为44nM。
CAS：2098836-45-2
分子式：C48H58ClN9O5S3
分子量：972.68
纯度：98%
存储：Store at -20°C

Background:

BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.

BRD4 degrader AT1 is a highly selective Brd4 degrader, with a Kd of 44 nM, for Brd4BD2 in cells. BRD4 degrader AT1 also shows Kds of 38.8 nM for a mutant Brd4BD2 (QVK), 111 ± 14 nM for Brd2BD1, 94 ± 9 nM for Brd2BD2, 35 ± 3 nM for Brd3BD1, 39 ± 8 nM for Brd3BD2, 75 ± 23 nM for Brd4BD1 and 35 ± 4 nM for a Brd2BD1 mutant (KEA). BRD4 degrader AT1 (1-3 μM) causes remarkable Brd4-selective depletion and has no or little activity against Brd2 and Brd3[1].

[1]. Gadd MS, et al. Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 May;13(5):514-521.