Me VH 032, amine

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说明: Amine functionalized VHL ligand for PROTAC® research
化学名: (4R)-3-Methyl-L-valyl-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-L-prolinamide dihydrochloride
纯度: ≥95% (HPLC)
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生物活性 for Me VH 032, amine

Me VH 032, amine is a derivative of the von Hippel-Lindau (VHL) ligand, VH 032 for use as a precursor to a PROTAC® that hijacks VHL as the E3 ubiquitin ligase component. Me VH 032, amine is supplied with a primary amine functional handle, for ready conjugation to a linker/target protein ligand. Introduction of the methyl group at the benzylic position of VH 032 is associated with improved binding affinity.

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.

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Usage Guidelines for Me VH 032, amine

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

技术数据 for Me VH 032, amine

分子量 517.51
公式 C23H32N4O3S.2HCl
储存 Desiccate at RT
纯度 ≥95% (HPLC)
CAS Number 2504950-56-3
PubChem ID 137319712
InChI Key YTJDUDNKHHNDRD-ARZBPYMHSA-N
Smiles CC1=C(C2=CC=C(C=C2)[C@H](C)NC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)N)=O)O)=O)SC=N1.Cl.Cl

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 Me VH 032, amine

参考文献 for Me VH 032, amine

参考文献是支持产品生物活性的出版物。

Hu et al (2019) Discovery of ERD-308 as a highly potent proteolysis targeting chimera (PROTAC) degrader of estrogen receptor (ER). J.Med.Chem. 62 1420 PMID: 30990042


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关键词: Me VH 032, amine, Me VH 032, amine supplier, MeVH032, methyl, VH032, amine, PROTAC, degraders, building, blocks, functionalized, Von, Hippel-Lindau, VHL, Functionalized, E3, Ligase, Ligands, 7634, Tocris Bioscience

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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