ZXH-3-26

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ZXH-3-26

CAS No. : 2243076-67-5

MCE 国际站：ZXH-3-26

产品活性：ZXH-3-26 是由Cereblon配体和BRD4配体相连的PROTAC，处理 5 小时后，DC₅₀ 约为 5 nM。

研究领域：PROTAC  |  Epigenetics

作用靶点：PROTACs  |  Epigenetic Reader Domain

In Vitro: ZXH-3-26 represents the first small molecule to allow pharmacologic targeting of BRD4 without significant inhibition or degradation of BRD2/3.
?ZXH-3-26 shows activity exclusively on the first bromodomain of BRD4, and spares degradation of BRD2/3 at concentrations 10 μM. Immunoblot analysis confirms that ZXH-3-26 degrades endogenous BRD4 with comparable efficacy compared to the best pan-BET degrader dBET6, while being inactive on BRD2/3.
?ZXH-3-26 engages CRBN in a conformation distinct.

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