GNE-375 是一种有效且高度选择性的 BRD9 抑制剂，IC50 为 5 nM。GNE-375 对 BRD9 的选择性比 BRD4、TAF1 和 CECR2 高 100 倍以上。GNE-375 降低 BRD9 与染色质的结合。
| 产品描述 | GNE-375 is a potent and highly selective BRD9 inhibitor with an IC50 of 5 nM. GNE-375 shows >100-fold selective for BRD9 over BRD4, TAF1, and CECR2. GNE-375 decreases BRD9 binding to chromatin[1]. [1]. Terry D Crawford, et al. Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance. Bioorg Med Chem Lett. 2017 Aug 1;27(15):3534-3541. |
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