XY-06-007

Cat. No. 7669 Submit a Review Datasheet / COA / SDS

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Description: Potent and selective Degrader of Brd4^{BD1 L94V} fusion proteins

Chemical Name: (2R)-2-((S)-6-(4-Chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-(5-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamido)pentyl)propanamide

Purity: ≥98% (HPLC)

Datasheet

Citations

Reviews

Literature (3)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for XY-06-007

XY-06-007 is a highly selective and potent "Bump & Hole" TAG Degrader (DC_50,6h = 10 nM, T_1/2 < 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 Brd4^{BD1 L94V} variant (the "hole"). In cell lines expressing a fusion of the target protein with the tag, Brd4^{BD1 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 Brd4^{BD1 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.

Licensing Information

Sold under license from Dana-Farber Cancer Institute

Technical Data for XY-06-007

M. Wt	809.28
Formula	C₄₁H₄₁ClN₈O₈
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2757045-94-4
PubChem ID	162526515
InChI Key	QTDHGBJLMBQHOW-BPJPHOPQSA-N
Smiles	COC1=CC=C(C2=C1)N3C([C@H]([C@@H](C)C(NCCCCCNC(COC4=CC=CC(C(N5C6C(NC(CC6)=O)=O)=O)=C4C5=O)=O)=O)N=C2C7=CC=C(Cl)C=C7)=NN=C3C

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
Solubility
Solubility	DMSO	80.93	100

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

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Product Datasheets for XY-06-007

Certificate of Analysis / Product Datasheet

Safety Datasheet

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

If you know of a relevant reference for XY-06-007, please let us know.

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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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TPD and Induced Proximity Research Product GuideUpdated

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

Active Degraders
TAG Degradation Platform
Degrader Building Blocks
Assays for Protein Degradation
Induced Proximity Tools

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

Validating Targets for TPD Using dTAG Poster

The dTAG platform offers a generalizable strategy to degrade, in principle, any intracellular protein of interest (POI) and is a useful strategy for exploration and validation of targets. This poster presents a workflow solution for target validation, from custom TAG knock-in cell-lines for your POI, different dTAG Degraders to knockdown you POI, to automated assays for protein degradation using Simple Western^TM instruments. Data are also presented on the use of an antibody that recognizes the TAG domain (FKBP12^F36V) for detection of degradation. Presented at TPD Europe, March 2022, London, UK.