BromoTag^® AGB3

Cat. No. 7688 Submit a Review Datasheet / COA / SDS

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Description: Selective Degrader of Brd4^{BD2 L387A} fusion proteins (BromoTag^®)

Chemical Name: (2S,4R)-1-((2S,17R)-2-(tert-Butyl)-17-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,16-dioxo-6,9,12-trioxa-3,15-diazanonadecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

Purity: ≥98% (HPLC)

Datasheet

Citations

Reviews

Literature (3)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for BromoTag^® AGB3

BromoTag^® ABG3 is a selective "Bump & Hole" TAG Degrader (DC₅₀ 210 - 290 nM, protein degradation t½ = 113 min, D_max = 92%). BromoTag AGB3 comprises a VHL E3 ligase ligand joined by a linker to a (+)-JQ1 (Cat. No. 4499) derivative (the "bump" bearer) that selectively binds the Brd4^{BD2 L387A} variant (the "hole"). In cell lines expressing a fusion of the target protein with the tag, Brd4^{BD2 L387A}, BromoTag AGB3 drives formation of a ternary complex between VHL and the "BromoTagged" protein, leading to ubiquitination of the protein and its subsequent proteasomal degradation.

BromoTag^® is a registered trademark of the University of Dundee and is used under license.

Brd4^{BD2 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.

Licensing Information

Sold under exclusive licence from the University of Dundee

Technical Data for BromoTag^® AGB3

M. Wt	1030.7
Formula	C₅₁H₆₄ClN₉O₈S₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2776191-07-0
InChI Key	IEUOSJXYLRSZRR-QLMRCLNASA-N
Smiles	ClC1=CC=C(C2=N[C@@H]([C@H](C(NCCOCCOCCOCC(N[C@H](C(N3C[C@@H](C[C@H]3C(NCC4=CC=C(C5=C(N=CS5)C)C=C4)=O)O)=O)C(C)(C)C)=O)=O)CC)C6=NN=C(C)N6C7=C2C(C)=C(S7)C)C=C1

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^® AGB3

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	103.07	100

Preparing Stock Solutions for BromoTag^® AGB3

The following data is based on the product molecular weight 1030.7. 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	9.7 mL
5 mM	0.19 mL	0.97 mL	1.94 mL
10 mM	0.1 mL	0.49 mL	0.97 mL
50 mM	0.02 mL	0.1 mL	0.19 mL

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Product Datasheets for BromoTag^® AGB3

Certificate of Analysis / Product Datasheet

Safety Datasheet

References for BromoTag^® AGB3

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^® AGB3, please let us know.

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Keywords: BromoTag® AGB3, BromoTag® AGB3 supplier, BromoTagAGB3, TAG, Degrades, Degraders, degradation, target, fusion, protein, BromoTag, Brd4BD2, L387A, Degradation, Platform, 7688, Tocris Bioscience

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Literature in this Area

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TPD and Induced Proximity Research Product GuideUpdated

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

Active Degraders
TAG Degradation Platform
Degrader Building Blocks
Assays for Protein Degradation
Induced Proximity Tools

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

Validating Targets for TPD Using dTAG Poster

The dTAG platform offers a generalizable strategy to degrade, in principle, any intracellular protein of interest (POI) and is a useful strategy for exploration and validation of targets. This poster presents a workflow solution for target validation, from custom TAG knock-in cell-lines for your POI, different dTAG Degraders to knockdown you POI, to automated assays for protein degradation using Simple Western^TM instruments. Data are also presented on the use of an antibody that recognizes the TAG domain (FKBP12^F36V) for detection of degradation. Presented at TPD Europe, March 2022, London, UK.