| 靶点 |
Kd: 44 nM (Brd4BD2, cell assay), 38.8 nM (Brd4BD2 QVK, cell assay), 111 nM (Brd2BD1, cell assay), 94 nM (Brd2BD2, cell assay), 35 nM (Brd3BD1, cell assay), 39 nM (Brd3BD2, cell assay), 75 nM (Brd4BD1, cell assay), 35 nM (Brd2BD1 KEA, cell assay)[1]
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| 体外研究 |
BRD4降解剂AT1是高选择性Brd4降解剂,Kd为44 nM,用于细胞中的Brd4BD2。 BRD4降解物AT1对突变体Brd4BD2(QVK)的Kds为38.8 nM,Brd2BD1为111±14 nM,Brd2BD2为94±9 nM,Brd3BD1为35±3 nM,Brd3BD2为39±8 nM,75±23 nM Brd4BD1和35±4nM的Brd2BD1突变体(KEA)。 BRD4降解剂AT1(1-3μM)引起显着的Brd4选择性消耗,对Brd2和Brd3没有或几乎没有活性[1]。
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