生物活性 | |||
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描述 | AT1 is a highly selective Brd4 degrader with a modified VHL ligand retained binding to VHL (Kd = 330 nM). Treatment with 1μM or 3μM AT1 for 24h significantly degraded Brd4 in HeLa cells. Compared with the previous Brd4 degrader MZ1, AT1 exhibited much more selectivity as it had no effect on Brd2, 3 protein while MZ1 exerted a broader and more profound effect across all BET proteins at the same concentration[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.03mL 0.21mL 0.10mL |
5.14mL 1.03mL 0.51mL |
10.28mL 2.06mL 1.03mL |
参考文献 |
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