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Biological Activity for XY-06-007
XY-06-007 is a highly selective and potent "Bump & Hole" TAG Degrader (DC50,6h = 10 nM, T1/2 < 43.2 min). XY-06-007 comprises a cereblon (CRBN) E3 ligase ligand joined by a linker to a (+)-JQ1 (Cat. No. 4499) derivative (the "bump" bearer) that selectively binds the Brd4BD1 L94V variant (the "hole"). In cell lines expressing a fusion of the target protein with the tag, Brd4BD1 L94V, XY-06-007 drives formation of a ternary complex between CRBN and the tagged protein, leading to ubiquitination and subsequent proteasomal degradation of the entire protein. XY-06-007 is highly selective for Brd4BD1 L94V over wild-type, and is broadly selective across the proteome. XY-06-007 can be combined with the dTAG approach to achieve simultaneous degrader-mediated depletion of their respective protein fusions. XY-06-007 is suitable for in vivo studies.
Sold under license from Dana-Farber Cancer Institute
Technical Data for XY-06-007
|Storage||Store at -20°C|
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 XY-06-007
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for XY-06-007
The following data is based on the product molecular weight 809.28. 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||1.24 mL||6.18 mL||12.36 mL|
|5 mM||0.25 mL||1.24 mL||2.47 mL|
|10 mM||0.12 mL||0.62 mL||1.24 mL|
|50 mM||0.02 mL||0.12 mL||0.25 mL|
References for XY-06-007
References are publications that support the biological activity of the product.
Nowak et al (2021) Structure-guided design of a "Bump-and-Hole" Bromodomain-based degradation tag. J.Med.Chem. 64 11637 PMID: 34279939
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Keywords: XY-06-007, XY-06-007 supplier, XY06007, TAG, Degrades, Degraders, degradation, targets, fusion, proteins, BromoTag, Brd4BD1L94V, Degradation, Platform, 7669, Tocris Bioscience
Citations for XY-06-007
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Literature in this Area
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Targeted Protein Degradation Research Product GuideUpdated
This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Ubiquitin-Proteasome System Proteins
- Assays for Protein Degradation
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