(+)-JQ1 PA

Discontinued Product

(+)-JQ1 PA (Cat. No. 6589) has been withdrawn from sale for commercial reasons.
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)
Citations (1)
Literature (3)

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
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.

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

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

1 Citation for (+)-JQ1 PA

Citations are publications that use Tocris products. Selected citations for (+)-JQ1 PA include:

Sophia Y et al (2020) Small molecule JQ1 promotes prostate cancer invasion via BET-independent inactivation of FOXA1. J Clin Invest 130 1782-1792 PMID: 31874106

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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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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