Thalidomide, propargyl

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说明: Alkyne-functionalized Thalidomide; 'click' cereblon ligand for PROTACs
化学名: 2-(2,6-Dioxo-3-piperidinyl)-4-(2-propyn-1-yloxy)-1H-isoindole-1,3(2H)-dione
纯度: ≥95% (HPLC)
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生物活性 for Thalidomide, propargyl

Thalidomide, propargyl is a click-activated Thalidomide (Cat.No. 0652); can be used as a precursor to a PROTAC® that hijacks cereblon as the E3 ubiquitin ligase component. Supplied with an alkyne functional handle at a position known not to significantly affect binding to cereblon, for ready click conjugation to a linker/target protein ligand.

Please contact us for SD files of our available Degrader Building Blocks.

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

Require a different derivative? Get in touch.

Usage Guidelines for Thalidomide, propargyl

This product is provided for use in onward chemistry. Suitable solvents can be used.

技术数据 for Thalidomide, propargyl

分子量 312.28
公式 C16H12N2O5
储存 Store at -20°C
纯度 ≥95% (HPLC)
CAS Number 2098487-39-7
PubChem ID 132118478
InChI Key NOGQTNDSZFYNTM-UHFFFAOYSA-N
Smiles O=C1N(C(C2=C(C=CC=C12)OCC#C)=O)C3CCC(NC3=O)=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 Thalidomide, propargyl

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参考文献 for Thalidomide, propargyl

参考文献是支持产品生物活性的出版物。

Wurz et al (2018) A "click chemistry platform" for the rapid rynthesis of bispecific molecules for inducing protein degradation. J.Med.Chem. 61 453 PMID: 28378579


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关键词: Thalidomide, propargyl, Thalidomide, propargyl supplier, PROTACs, click-activated, thalidomide, E3, ligase, ligands, cereblon, PROTAC, Toolbox, targeted, protein, degradation, development, Functionalized, Ligase, Ligands, 6685, Tocris Bioscience

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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!

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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