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Submit Review(+)-JQ1 carboxylic acid
说明： Carboxylic acid-functionalized BET bromodomain inhibitor; target ligand for PROTACs
化学名： (6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid
纯度： ≥98% (HPLC)
生物活性 for (+)-JQ1 carboxylic acid
(+)-JQ1 carboxylic acid is a BET bromodomain inhibitor (+)-JQ1 (Cat. No. 4499) with a carboxylic acid functional group for conjugation reactions. Can be used as a precursor to PROTAC® Degraders that targets BET bromodomains after conjugation to a linker and E3 ligase ligand.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
技术数据 for (+)-JQ1 carboxylic acid
| 分子量 | 400.88 |
| 公式 | C19H17ClN4O2S |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 202592-23-2 |
| PubChem ID | 66828107 |
| InChI Key | LJOSBOOJFIRCSO-AWEZNQCLSA-N |
| Smiles | OC(C[C@@H]1N=C(C2=CC=C(Cl)C=C2)C3=C(SC(C)=C3C)N4C1=NN=C4C)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for (+)-JQ1 carboxylic acid
参考文献 for (+)-JQ1 carboxylic acid
参考文献是支持产品生物活性的出版物。
Winter et al (2015) DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science 348 1376 PMID: 25999370
Zengerle et al (2015) Selective small molecule induced degradation of the BET bromodomain protein BRD4. ACS Chem Biol. 10 1770 PMID: 26035625
Gadd et al (2017) Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat.Chem.Biol. 13 514 PMID: 28288108
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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