BromoTag^® AGB1

BromoTag^® AGB1 is a highly selective and potent "Bump & Hole" TAG Degrader (DC_50,6h < 15 nM, t_1/2 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 Brd4^{BD2 L387A} variant (the "hole"). In cell lines expressing a fusion of the target protein with the tag, Brd4^{BD2 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 Brd4^{BD2 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.

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.

A polyclonal antibody targeting Brd4^{BD2 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