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Click-activated (alkyne) version of the BET bromodomain inhibitor (+)-JQ1 (Cat. No. 4499). Can be used as a precursor to PROTACs that target BET bromodomains. Supplied with an alkyne functionalized handle for click conjugation to a linker/E3 ligase ligand. Can also be conjugated to fluorescent dyes for imaging aplications.
|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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 437.95. 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||2.28 mL||11.42 mL||22.83 mL|
|5 mM||0.46 mL||2.28 mL||4.57 mL|
|10 mM||0.23 mL||1.14 mL||2.28 mL|
|50 mM||0.05 mL||0.23 mL||0.46 mL|
References are publications that support the biological activity of the product.
Tyler et al (2017) Click chemistry enables preclinical evaluation of targeted epigenetic therapies. Science 356 1397 PMID: 28619718
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Keywords: (+)-JQ1 PA, (+)-JQ1 PA supplier, (+)-JQ1PA, PROTACs, click-activated, Tools, for, R&D, BET, bromodomain, inhibitors, inhibits, Bromodomains, Functionalized, Warhead, Ligands, 6589, Tocris Bioscience
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Literature in this Area
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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.