(+)-JQ1 maleimide

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Description: JQ1-maleimide functionalized probe; induces proteasomal degradation of BRD4
Chemical Name: (S)-N-(2-(2-(2-(2-(4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamido)ethoxy)ethoxy)ethyl)-6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanamide
Purity: ≥95% (HPLC)
Datasheet
Citations
Reviews
Literature (3)

Biological Activity for (+)-JQ1 maleimide

(+)-JQ1 maleimide is a probe that comprises a cysteine-reactive maleimide connected to the BRD4 ligand, JQ1, via a PEG2 linker. It can be used in the COFFEE method (COvalent Functionalization Followed by E3 Electroporation) in which (+)-JQ1 maleimide is covalently attached to VHL followed by electroporation into live cells. The E3 ligase forms a complex with BRD4 intracellularly and induces its degradation.

Technical Data for (+)-JQ1 maleimide

M. Wt 724.27
Formula C35H42ClN7O6S
Storage Store at -20°C
Purity ≥95% (HPLC)
InChI Key SGQDAIFBYPRIDQ-MHZLTWQESA-N
Smiles ClC1=CC=C(C2=N[C@@H](CC(NCCOCCOCCNC(CCCCCN3C(C=CC3=O)=O)=O)=O)C4=NN=C(C)N4C5=C2C(C)=C(C)S5)C=C1

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 maleimide

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 72.43 100

Preparing Stock Solutions for (+)-JQ1 maleimide

The following data is based on the product molecular weight 724.27. 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 1.38 mL 6.9 mL 13.81 mL
5 mM 0.28 mL 1.38 mL 2.76 mL
10 mM 0.14 mL 0.69 mL 1.38 mL
50 mM 0.03 mL 0.14 mL 0.28 mL

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Product Datasheets for (+)-JQ1 maleimide

References for (+)-JQ1 maleimide

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

Pinch et al (2022) A strategy to assess the cellular activity of E3 ligase components against neo-substrates using electrophilic probes. Cell Chem.Biol. 29 57 PMID: 34499862


If you know of a relevant reference for (+)-JQ1 maleimide, please let us know.

Keywords: (+)-JQ1 maleimide, (+)-JQ1 maleimide supplier, TPD, targeted, protein, degradation, maleimide, probe, 2-PEG, linker, COFFEE, COvalent, Functionalization, Followed, E3, Electroporation, BRD4, VHL, Degraders, degrades, Functionalized, Warhead, Ligands, Bromodomains, 7576, Tocris Bioscience

Citations for (+)-JQ1 maleimide

Citations are publications that use Tocris products.

Currently there are no citations for (+)-JQ1 maleimide. Do you know of a great paper that uses (+)-JQ1 maleimide from Tocris? Please let us know.

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Literature in this Area

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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