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Biological Activity for BromoTag® AGB1
BromoTag® AGB1 is a highly selective and potent "Bump & Hole" TAG Degrader (DC50,6h < 15 nM, t1/2 for protein degradation = 40 min). BromoTag AGB1 comprises a VHL E3 ligase ligand joined by a linker to a (+)-JQ1 (Cat. No. 4499) derivative (the "bump" bearer) that selectively binds the Brd4BD2 L387A variant (the "hole"). In cell lines expressing a fusion of the target protein with the tag, Brd4BD2 L387A, BromoTag AGB1 drives formation of a ternary complex between VHL and the "BromoTagged" protein, leading to ubiquitination of the protein and its subsequent proteasomal degradation. BromoTag AGB1 is highly selective for Brd4BD2 L387A over wild-type, and is broadly selective across the proteome. BromoTag AGB1 exhibits no cytoxicity in several cancer relevant cell lines. BromoTag AGB1 is suitable for in vivo studies.
Negative control BromoTag® cis-AGB1 (Cat. No. 7687) also available.
Brd4BD2 L387A can be expressed as a fusion with a target protein of interest using genome engineering techniques via CRISPR-mediated locus-specific knock-in. See protocol for more information.
A polyclonal antibody targeting Brd4BD2 L387A (Cat. No. NBP3-17999) is available from Bio-Techne sister brand Novus Biologicals.
BromoTag® is a registered trademark of the University of Dundee and is used under license.
Sold under exclusive licence from the University of Dundee
Technical Data for BromoTag® AGB1
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for BromoTag® AGB1
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for BromoTag® AGB1
The following data is based on the product molecular weight 1031.68. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||0.97 mL||4.85 mL||9.69 mL|
|5 mM||0.19 mL||0.97 mL||1.94 mL|
|10 mM||0.1 mL||0.48 mL||0.97 mL|
|50 mM||0.02 mL||0.1 mL||0.19 mL|
References for BromoTag® AGB1
References are publications that support the biological activity of the product.
Bond et al (2021) Development of BromoTag: a 'Bump-and-Hole'-PROTAC system to induce potent, rapid, and selective degradation of tagged target proteins. J.Med.Chem. 64 15477 PMID: 34652918
If you know of a relevant reference for BromoTag® AGB1, please let us know.
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Keywords: BromoTag® AGB1, BromoTag® AGB1 supplier, BromoTagAGB1, TAG, Degrades, Degraders, degradation, target, fusion, protein, BromoTag, Brd4BD2, L387A, Degradation, Platform, 7686, Tocris Bioscience
Citations for BromoTag® AGB1
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Currently there are no citations for BromoTag® AGB1. Do you know of a great paper that uses BromoTag® AGB1 from Tocris? Please let us know.
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Literature in this Area
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Targeted Protein Degradation Research Product GuideUpdated
This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Ubiquitin-Proteasome System Proteins
- Assays for Protein Degradation
Targeted Protein Degradation Poster
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia