VH 032 amide-PEG4-amine

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Cat.No. 6464 - VH 032 amide-PEG4-amine | C32H49N5O8S.2HCl
Description: VHL ligand with PEG linker and terminal amine for onward chemistry
Alternative Names: VH 032 - linker 2
Chemical Name: (2S,4R)-1-((S)-17-amino-2-(tert-butyl)-4-oxo-6,9,12,15-tetraoxa-3-azaheptadecan-1-oyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide dihydrochloride
Purity: ≥95% (HPLC)
Literature (1)

Biological Activity

Functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC® research and development; incorporates an E3 ligase ligand plus a PEG linker ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D.

This product has been recently renamed. The previous name for this product was VH 032 - linker 2

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

Usage guidelines:

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

Technical Data

M. Wt 736.75
Formula C32H49N5O8S.2HCl
Storage Store at -20°C
Purity ≥95% (HPLC)
PubChem ID 131704498
Smiles O=C(N[C@@H](C(C)(C)C)C(N1C[C@H](O)C[C@H]1C(NCC2=CC=C(C=C2)C3=C(C)N=CS3)=O)=O)COCCOCCOCCOCCN.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

Certificate of Analysis / Product Datasheet
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References are publications that support the biological activity of the product.

Salami et al (2017) Waste disposal-An attractive strategy for cancer therapy. Science 355 1163 PMID: 28302825

Zengerle et al (2015) Selective small molecule induced degradation of the BET bromodomain protein BRD4. ACS Chem.Biol. 10 1770 PMID: 26035625

Chan et al (2018) Impact of target warhead and linkage vector on inducing protein degradation: comparison of bromodomain and extra-terminal (BET) degraders derived from triazolodiazepine (JQ1) and tetrahydroquinoline (I-BET726) BET inhibitor scaffolds. J.Med.Chem. 61 504 PMID: 28595007

If you know of a relevant reference for VH 032 amide-PEG4-amine, please let us know.

Keywords: VH 032 amide-PEG4-amine, VH 032 amide-PEG4-amine supplier, Proteolysis, Targeting, Chimera, PROTACs, VHL, E3, ubiquitin, ligase, PEG, linker, conjugate, PROTAC, polyethene, glycol, von-Hippel-Lindau, protein, ligand, VH032, -, 2, VH, 032, Ligands, Plus, Linkers, 6464, Tocris Bioscience

Citations for VH 032 amide-PEG4-amine

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Targeted Protein Degradation

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