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TRIM24ºÍBRPF1Êǰ©Ö¢µÄDZÔÚÖÎÁưеã ¡£Y08624ÊÇÒ»ÖÖÐÂÐÍTRIM24/BRPF1Ë«ÖØÒÖÖÆ¼Á£¬¾ßÓÐÓÅÒìµÄCaco-2ÉøÍ¸ÐÔ ¡£Caco-2 ÉøÍ¸ÐԲⶨͨ¹ý×ðÁú¿­Ê±¾ÙÐÐ

2023-07-06
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TRIM24 (tripartite motif-containing protein 24) and BRPF1 (bromodomain and PHD finger containing protein 1) are epigenetics ¡°readers¡±and potential therapeutic targets for cancer and other diseases. Y08624 (Compound 20l) is a new TRIM24/BRPF1 dual inhibitor. Y08624 displays reasonable Caco-2 permeability. Caco-2 permeability assay was performed by Medicilon.

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Qiuping Xiang, et al. Discovery, optimization and evaluation of 1-(indolin-1-yl)ethan-1-ones as novel selective TRIM24/BRPF1 bromodomain inhibitors. Eur J Med Chem. 2022 Jun 5;236:114311. doi: 10.1016/j.ejmech.2022.114311. 

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