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Submit Review(+)-JQ1 maleimide
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)
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.
| 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.
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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
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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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
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
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