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Submit ReviewMe VH 032, amine
Description: Amine functionalized VHL ligand for PROTAC® research
Chemical Name: (4R)-3-Methyl-L-valyl-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-L-prolinamide dihydrochloride
Purity: ≥95% (HPLC)
Biological Activity 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.
Technical Data for Me VH 032, amine
| M. Wt | 517.51 |
| Formula | C23H32N4O3S.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for Me VH 032, amine
References for Me VH 032, amine
References are publications that support the biological activity of the product.
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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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