BromoTag® AGB1

Tocris Bioscience | Catalog # 7686

Potent and selective Degrader of Brd4BD2 L387A fusion proteins (BromoTag®)
Tocris Bioscience

Key Product Details

Description

Potent and selective Degrader of Brd4BD2 L387A fusion proteins (BromoTag®)
View all TAG Degradation Platforms »

Product Description

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.

Licensing Information

Sold under exclusive licence from the University of Dundee

Product Specifications for BromoTag® AGB1

Molecular Weight

1031.68

Formula

C51H63ClN8O9S2

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

(S)-13-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidine-1-carbonyl)-14,14-dimethyl-11-oxo-3,6,9-trioxa-12-azapentadecyl (R)-2-((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)butanoate

CAS Number

2776190-62-4

PubChem ID

162641704

InChI Key

ILEZCIMECSOYKF-QLMRCLNASA-N

SMILES

ClC1=CC=C(C2=N[C@@H]([C@H](C(OCCOCCOCCOCC(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.

Solubility

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 103.17 100

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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 0.10 mL 0.48 mL 0.97 mL
50 mM 0.02 mL 0.10 mL 0.19 mL

Calculators

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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 8 publications citing the usage of this product.

Product Documents for BromoTag® AGB1

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for BromoTag® AGB1

For research use only

Citations for BromoTag® AGB1

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