AT6,2098836-50-9

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AT6

CAS No. : 2098836-50-9

MCE 国际站：AT6

产品活性：AT6 是一种 PROTAC AT1 类似物，PROTAC AT1 由von Hippel-Lindau配体和BRD4配体相连，是一种高度选择性的溴结构域蛋白 (Brd4) 降解剂。

研究领域：PROTAC

作用靶点：PROTACs

In Vitro: PROTACs (proteolysis-targeting chimaeras) are bifunctional molecules that recruit a target protein in proximity to an E3 ubiquitin ligase to trigger protein degradation. Structural elucidation of the key ternary ligase: PROTAC: target species and how this impacts target degradation selectivity remains elusive. The ligand folds into itself to allow formation of specific intermolecular interactions in the ternary complex. Isothermal titration calorimetry studies, supported by surface mutagenesis and proximity assays, are consistent with pronounced cooperative formation of ternary complexes with Brd4^BD2. Structure-based-designed compound AT1 exhibits highly selective depletion of Brd4 in cells.

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