BromoTag® AGB3

Tocris Bioscience | Catalog # 7688

Selective Degrader of Brd4BD2 L387A fusion proteins (BromoTag®)
Tocris Bioscience

Key Product Details

Description

Selective Degrader of Brd4BD2 L387A fusion proteins (BromoTag®)
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Product Description

BromoTag® ABG3 is a selective "Bump & Hole" TAG Degrader (DC50 210 - 290 nM, protein degradation t½ = 113 min, Dmax = 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 Brd4BD2 L387A variant (the "hole"). In cell lines expressing a fusion of the target protein with the tag, Brd4BD2 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.

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.

Licensing Information

Sold under exclusive licence from the University of Dundee

Product Specifications for BromoTag® AGB3

Molecular Weight

1030.70

Formula

C51H64ClN9O8S2

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

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.

Solubility

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

Preparing Stock Solutions for BromoTag® AGB3

The following data is based on the product molecular weight 1030.70.

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 9.70 mL
5 mM 0.19 mL 0.97 mL 1.94 mL
10 mM 0.10 mL 0.49 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.

Product Documents for BromoTag® AGB3

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® AGB3

For research use only

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