BRD4 (BD1) Assay Service
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Target
BRD4 (BD1)
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Description
Screening and/or profiling inhibitor compounds against BRD4 substrate binding in a homogeneous biochemical assay.
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Synonyms
Bromodomain, HUNK1, MCAP, BRD-4
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Example Data
*Example only, final data may vary.
Assay Details
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Assay Format
TR-FRET
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Reference Compounds and IC50
JQ1, 0.07 μM; ABBV-744, 1 μM
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Assay Principle
The BRD4 (BD1) TR-FRET Assay is designed to measure the inhibition of BRD4 (BD1) binding to its substrate in a no-wash homogeneous 384 reaction format, highly suitable for high throughput. The assay procedure is straightforward and simple; a sample containing terbium-labeled donor, dye-labeled acceptor, BRD4, substrate, and an inhibitor is incubated for sixty minutes. Then, the fluorescence intensity is measured using a fluorescence reader.
Target Details
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Protein Family
Bromodomains
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UniProt
O60885
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Background
BRD4 is a protein involved in regulating gene expression by recognizing acetylated histones through its bromodomains, playing critical roles in cell cycle regulation and cancer progression. Its overexpression in certain cancers has made it an attractive therapeutic target. Small molecule inhibitors have been developed to disrupt BRD4's interaction with acetylated histones, thereby inhibiting its transcriptional regulatory activity and potentially suppressing the expression of oncogenes.
Delivery
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Estimated Turnaround
Two to three weeks following delivery of compounds
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Results
Extensive report with raw and analyzed data, graphs, and detailed protocols. Includes positive control for inhibition.