General Description
A cell-permeable benzimidazolyl-benzimidazolothione that targets the BD1 domain of the BET family member BRD2 (
Kd = 28 μM), making it inaccessible for acetylated H4K12 (histone H4 Lys12) binding. Shown to effectively inhibit TSA- (Cat. No.
647925; 1 h 1 μM) induced BRD2 BD1-H4K12 association in COS7 cells (100% inhibition by 60 μM BIC1) and greatly suppress active Ras-induced SV40 promoter transcription activity in HeLa cells (70% inhibition by 5 μM BIC1), while being much less effective against BRDT BD1 binding to acetylated H4K5/K8.
