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Cat. Number
996837237387516
Chemical Name
BRD4 bromodomain 1 TR-FRET Assay Kit
References
Synonyms
  • MCAP
  • HUNK1
  • Bromodomain containing 4
Stability 6 months
Storage -80°C
Shipping Dry ice in continental US; may vary elsewhere

Background Reading

Hargreaves, D.C., Horng, T., and Medzhitov, R. Control of inducible gene expression by signal-dependent transcriptional elongation. Cell 138(1) 129-45 (2009).

Weidner-Glunde, M., Ottinger, M., and Schulz, T.F. WHAT do viruses BET on? Front Biosci 15 537-549 (2010).

Liu, Y., Wang, X., Zhang, J., et al. Structural basics and binding properties of the second bromodomain of Brd4 with acetylated histone tails. Biochem 47 6403-6417 (2008).

Umehara, T., Nakamura, Y., Wakamori, M., et al. Structural implications for K5/K12-di-acetylated histone H4 recognition by the second bromodomain of BRD2. FEBS Lett 584(18) 3901-3908 (2010).

Dawson, M.A., Prinjha, R.K., Dittmann, A., et al. Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature 478 529-533 (2011).

Florence, B., and Faller, D.V. You bet-cha: A novel family of transcriptional regulators. Front Biosci 6 D1008-D1018 (2011).

Mertz, J.A., Conery, A.R., Bryant, B.M., et al. Targeting MYC dependence in cancer by inhibiting BET bromodomains. Proc Natl Acad Sci USA 108(40) 16669-16674 (2011).

Zhang, J., Chung, T.D.Y., and Oldenburg, K.R. A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 4(2) 67-73 (1999).

Mujtaba, S., Zeng, L., and Zhou, M. Structure and acetyl-lysine recognition of the bromodomain. Oncogene 26 5521-5527 (2011).

LeRoy, G., Rickards, B., and Flint, S.J. The double bromodomain proteins Brd2 and Brd3 couple histone acetylation to transcription. Mol Cell 30(1) 51-60 (2008).

Philpott, M., Yang, J., Tumber, T., et al. Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery. Mol BioSyst 7(10) 2899-2908 (2011).

Delmore, J.E., Issa, G.C., Lemieux, M.E., et al. BET bromodomain inhibition as a therapeutic strategy to target c-Myc. Cell 146(6) 904-917 (2011).

Umehara, T., Nakamura, Y., Jang, M.K., et al. Structural basis for acetylated histone H4 recognition by the human BRD2 bromodomain. J Biol Chem 2855(10) 7610-7618 (2010).

Day, A., Chitsaz, F., Abbasi, A., et al. The double bromodomain protein Brd4 binds to acetylated chromatin during interphase and mitosis. Proc Natl Acad Sci USA 100(15) 8758-8763 (2003).

Filippakopoulos, P., Qi, J., Picaud, S., et al. Selective inhibition of BET bromodomains. Nature 468(7327) 1067-1073 (2010).

Hewings, D.S., Wang, M., Philpott, M., et al. 3,5-Dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands. J Med Chem 1-30 (2011).

Chung, C.W., Coste, H., White, J.H., et al. Discovery and characterization of small molecule inhibitors of the BET family bromodomains. J Med Chem 54(11) 3827-3838 (2011).

Nicodeme, E., Jeffrey, K.L., Schaefer, U., et al. Suppression of inflammation by a synthetic histone mimic. Nature 468(7327) 1119-23 (2010).

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600520-9600well
Foil Plate Covers
384-Well Solid Plate (low volume; black)
TR-FRET Assay Buffer (10X) 5 × 10 mL
TR-FRET Assay Buffer Additive 5 × 1 g
(+)-JQ1 Positive Control 5 × 40 nmol
BRD4 bromodomain 1 Europium Chelate 5 × 2100 Well
BRD4 bromodomain 1 Ligand/APC Acceptor Mixture 5 × 2100 Well
600520-1920well
Foil Plate Covers
384-Well Solid Plate (low volume; black)
TR-FRET Assay Buffer (10X) 10 mL
TR-FRET Assay Buffer Additive 1 g
(+)-JQ1 Positive Control 5 × 8 nmol
BRD4 bromodomain 1 Europium Chelate 5 × 420 Well
BRD4 bromodomain 1 Ligand/APC Acceptor Mixture 5 × 420 Well
600520-384well
Foil Plate Covers
384-Well Solid Plate (low volume; black)
TR-FRET Assay Buffer (10X) 2 mL
TR-FRET Assay Buffer Additive 200 mg
(+)-JQ1 Positive Control 8 nmol
BRD4 bromodomain 1 Europium Chelate 420 Well
BRD4 bromodomain 1 Ligand/APC Acceptor Mixture 420 Well
Size Global Purchasing
384 wells  
1920 wells  
9600 wells  

Description

Bromodomains recognize acetylated lysine residues and recruit regulatory complexes to acetylated nucleosomes, thereby controlling chromatin structure and gene expression. The isolated individual or tandem bromodomains of BRD2 and BRD4 bind acetylated histone tails, which couples histone acetylation marks to the transcriptional regulation of target promoters. Small molecule inhibitors of bromodomain interactions hold promise as useful therapeutics for human disease. Cayman’s BRD4 bromodomain 1 TR-FRET Assay Kit is a homogeneous, Time-Resolved Fluorescence Resonance Energy Transfer assay method amenable to rapid characterization of inhibitors of bromodomain/acetylated peptide interaction in a high throughput format. This screening assay kit is robust, displaying a Z’ >0.6.
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