A cell-permeable benzimidazolyl-benzimidazolothione compound that directly interacts with BRD2-BD1 bromodomain reversibly (=28uM) and blocks the transcriptional activity of BRD2 in COS7 cells expressing Histac-K12 (<10uM). Shown to selectively disrupt BRD2 bromodomain-acetylated histone H4K12 association without modulating H4K12 acetylation; only weakly affect the interaction between the BRDT bromodomain (testis-specific bromodomain-containing protein) and acetylated histone H4.
Formula:C17H16N4S2
Molecular Weight:340.5
Solubility:DMSO (50mg/ml)
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.