The SWI/SNF family of ATP-dependent chromatin remodeling enzymes catalyzes structural changes that allow proteins to access the nucleosomal DNA, alter the position of the nucleosomes on the DNA, or eject the histone octamer from the template. Mammalian SWI/SNF remodelers contain either BRM or BRG1 as their catalytic subunit. These subunits also contain a C-terminal bromodomain that binds to acetylated residues on histone tails. Stereotypical inhibitors of BET family bromodomains (JQ-1 and I-BET) do not inhibit the interaction of BRG1 with peptide binding partners (IC50 >100µM). Several subunits of the SWI/SNF complex exhibit tumor suppressor activity and BRG1 is mutated or expression is absent in a significant number of non-small-cell lung cancer samples. The BRG1 bromodomain TR-FRET Assay Kit is a homogeneous, TR-FRET assay method amenable to rapid characterization of inhibitors of bromodomain/acetylated peptide interaction in a high throughput format. This screening assay is robust, displaying a Z >0.7.
BRG1 bromodomain Europium Chelate: 1 vial/420 wells; 5 vials/420 wells; 5 vials/2,100 wells; -80°CBRG1 bromodomain Ligand/APC Acceptor Mixture: 1 vial/420 wells; 5 vials/420 wells; 5 vials/ 2,100 wells; -80°CTR-FRET Assay Buffer (10X): 1 vial/2 ml; 1 vial/10 ml; 5 vials/10 ml; -20°CTR-FRET Assay Buffer Additive: 1 vial/200 mg; 1 vial/1 g; 5 vials/1 g; -20°CH3 Positive Control: 1 vial/2.5 nmol; 5 vials/2.5 nmol; 5 vials/12.5 nmol; -80°C384-Well Solid Plate (low volume; black): 1 plate; 5 plates; 25 plates; Room temperatureFoil Plate Covers: 1 cover; 5 covers; 25 covers; Room temperature