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PNZ5 是一个有效的、异恶唑类的、BET 的广泛抑制剂,有着类似(+)-JQ1 的高选择性和强效作用,其对BRD4(1) 的KD 值为 5.43 nM。
PNZ5 is a potent and isoxazole-based pan-BET inhibitor with high selectivity and potency similar to the well-established (+)-JQ1, with a KD of 5.43 nM for BRD4(1)[1]. BRD4(1)|5.43 nM (Kd)
[1]. Montenegro RC, et al. BET inhibition as a new strategy for the treatment of gastric cancer. Oncotarget. 2016 Jul 12;7(28):43997-44012.
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