Chemical Name: Methyl (6S)-4-(4-chlorophenyl)-2-[[[5-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]pentyl]amino]carbonyl]-3,9-dimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetate
Biological ActivityPotent and selective BRD4 degrader (DC50 ~ 5 nM). Exhibits no significant degradation of BRD2 and BRD3. Whole proteome mass spectometry shows significant downregulation of BRD4 only. Active intracellularly.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Plasticity in binding confers selectivity in ligand-induced protein degradation.
Nowak et al.
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