Bromodomain Inhibitor, BIC1

BRD2 Inhibitor II, BIC1
1-(2-(1H-Benzimidazol-2-ylsulfanyl)ethyl)-3-methyl-1,3-dihydro-2H-benzimidazole-2-thione, 1-(2-(1H-Benzo[d]imidazol-2-ylthio)ethyl)-3-methyl-1H-benzo[d]imidazole-2(3H)-thione, BRD2 Bromodomain-Interactive Compound, BIC1
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.
产品信息
Form  Off-white solid
Molar mass  340.5
Protect from Light  是的
Packaged under inert gas  是的
Purity  ≥95% by HPLC
Solubility  DMSO
Chemical formula  C17H16N4S2
商店和运输信息
Storage  -20°C
Ship  Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Regulatory Review