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Submit ReviewMe 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.
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PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
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This product is provided for use in onward chemistry. Suitable solvents can be used.
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.
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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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