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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)
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.
Product Datasheets for (+)-JQ1 PA
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
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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
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
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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