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(+)-JQ1 PA

Cat. No. 6589 Submit a Review Datasheet / COA / SDS
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Description: Functionalized BET bromodomain inhibitor; 'click' target ligand for PROTACs
Chemical Name: (6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-N-2-propyn-1-yl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
Purity: ≥95% (HPLC)
Datasheet
Citations
Reviews
Literature (3)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for (+)-JQ1 PA

(+)-JQ1 PA is a click-activated (alkyne) version of the BET bromodomain inhibitor (+)-JQ1 (Cat. No. 4499). Can be used as a precursor to a PROTAC® targeting 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.

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

Technical Data for (+)-JQ1 PA

M. Wt 437.95
Formula C22H20ClN5OS
Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 2115701-93-2
PubChem ID 134821687
InChI Key ZLSCJWMPQYKVKU-KRWDZBQOSA-N
Smiles O=C(NCC#C)C[C@@H]1N=C(C2=CC=C(Cl)C=C2)C3=C(SC(C)=C3C)N4C1=NN=C4C

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 PA

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 43.8 100
ethanol 43.8 100

Preparing Stock Solutions for (+)-JQ1 PA

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.

Select a batch to recalculate based on the batch molecular weight:
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

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References for (+)-JQ1 PA

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

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

View Related Products by Target

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

Citations for (+)-JQ1 PA

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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