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BromoTag® AGB1

Catalog #: 7686 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
7686/5
BromoTag® AGB1 | CAS No. 2776190-62-4 | TAG Degradation Platforms
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Description: Potent and selective Degrader of Brd4BD2 L387A fusion proteins (BromoTag®)

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

Purity: ≥98%

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Biological Activity

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.

Technical Data

M.Wt:
1031.68
Formula:
C51H63ClN8O9S2
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2776190-62-4

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.

Additional Information

Licensing Caveats:
Sold under exclusive licence from the University of Dundee

Product Datasheets

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