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Submit ReviewVH 032, amine
说明： Functionalized VHL ligand for PROTACs
化学名： (4R)-3-Methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-L-prolinamide dihydrochloride
纯度： ≥98% (HPLC)
生物活性 for VH 032, amine
VH 032, amine is a derivative of the von Hippel-Lindau (VHL) ligand, VH 032; commonly used as a precursor to a PROTAC® that hijacks VHL as the E3 ubiquitin ligase component. Supplied with a primary amine functional handle at a position known not to significantly affect binding to VHL, for ready 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 VH 032, amine
This product is provided for use in onward chemistry. Suitable solvents can be used.
技术数据 for VH 032, amine
| 分子量 | 503.49 |
| 公式 | C22H30N4O3S.2HCl |
| 储存 | Desiccate at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2137142-47-1 |
| PubChem ID | 118864076 |
| InChI Key | SADPMNNWFOJMCY-ZNZDOTFASA-N |
| Smiles | CC1=C(C2=CC=C(C=C2)CNC([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 VH 032, amine
参考文献 for VH 032, amine
参考文献是支持产品生物活性的出版物。
Zengerle et al (2015) Selective small molecule induced degradation of the BET bromodomain protein BRD4. ACS Chem.Biol. 10 1770 PMID: 26035625
Galdeano et al (2014) Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von Hippel-Lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities. J.Med.Chem. 57 8657
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关键词: VH 032, amine, VH 032, amine supplier, VH032, amine, 2HCl, protein, degrader, 1, VHL, VL, 269, PROTACs, E3, ligase, ligands, 1448297-52-6, 1448189-80-7, 2230958-14-0, functionalized, Functionalized, Ligase, Ligands, 6462, Tocris Bioscience
1 篇 VH 032, amine 的引用文献
引用文献是使用了 Tocris 产品的出版物。 VH 032, amine 的部分引用包括：
Smalley et al (2020) PROTAC-mediated degradation of class I histone deacetylase enzymes in corepressor complexes. Chem.Commun.(Camb) 56 4476 PMID: 32201871
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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。
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