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WDR5-IN-4TFA是一种染色质相关WD重复结构域5蛋白(WDR5)的WIN位点抑制剂,Kd值为0.1nM。WDR5-IN-4TFA能够从染色质中取代WDR5,并降低相关基因的表达,引起翻译抑制和核仁应激。具有抗癌作用。
WDR5-IN-4 TFA is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 TFA displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity[1].
[1]. Aho ER, et al. Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity. Cell Rep. 2019 Mar 12;26(11):2916-2928.e13.
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