(+)-JQ1 bump, acid functionalized

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Description: Functionalized BET bromodomain ligand; precursor for Tag Degraders
Chemical Name: (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)butanoic acid
Purity: ≥98% (HPLC)
Literature (3)

Biological Activity for (+)-JQ1 bump, acid functionalized

(+)-JQ1 bump, acid functionalized is a BET bromodomain binding analog of (+)-JQ1 (Cat. No. 4499) that selectively binds single point mutant form of Brd4 (Brd4BD2 L387A). Functionalized with a carboxylic acid group to enable onward chemistry. The position of the carboxylic acid group represents an 'exit vector' allowing modification without interfering with compound binding ability.

Technical Data for (+)-JQ1 bump, acid functionalized

M. Wt 428.94
Formula C21H21ClN4O2S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2421153-77-5
Smiles CC1=C(C)C(C(C2=CC=C(C=C2)Cl)=N[C@@H]([C@H](C(O)=O)CC)C3=NN=C(C)N43)=C4S1

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 (+)-JQ1 bump, acid functionalized

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 42.89 100

Preparing Stock Solutions for (+)-JQ1 bump, acid functionalized

The following data is based on the product molecular weight 428.94. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.33 mL 11.66 mL 23.31 mL
5 mM 0.47 mL 2.33 mL 4.66 mL
10 mM 0.23 mL 1.17 mL 2.33 mL
50 mM 0.05 mL 0.23 mL 0.47 mL

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Product Datasheets for (+)-JQ1 bump, acid functionalized

Certificate of Analysis / Product Datasheet
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References for (+)-JQ1 bump, acid functionalized

References are publications that support the biological activity of the product.

Bond et al (2021) Development of BromoTag: a 'Bump-and-Hole'-PROTAC system to induce potent, rapid, and selective degradation of tagged target proteins. J.Med.Chem 64 15477 PMID: 34652918

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Citations for (+)-JQ1 bump, acid functionalized

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Targeted Protein Degradation Research Product Guide

Targeted Protein Degradation Research Product Guide

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
Developing Degraders Poster

Developing Degraders Poster

This poster describes the generation of a database of Degraders (PROTACs®) from the literature. The Degraders were profiled according to the constituent ligands, linker type, linker length and physicochemical properties and this information was used to establish a set of guidelines for the design and synthesis of cell-permeable Degrader molecules. Presented at the 20th SCI/RSC Medicinal Chemistry Symposium 2019, Cambridge, UK.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Targeted Protein Degradation Poster

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