VH 032 amide-PEG3-BCN

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Description: Functionalized VHL building block for copper-free click chemistry
Chemical Name: ((1R,8S,9s)-Bicyclo[6.1.0]non-4-yn-9-yl)methyl ((S)-14-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidine-1-carbonyl)-15,15-dimethyl-12-oxo-3,6,9-trioxa-13-azahexadecyl)carbamate
Purity: ≥90% (HPLC)
Datasheet
Citations
Reviews
Literature (1)

Biological Activity for VH 032 amide-PEG3-BCN

VH 032 amide-PEG3-BCN is a functionalized von Hippel Lindau (VHL) protein ligand for PROTAC® research and development. Incorporates an E3 ligase ligand plus a PEG3 linker with terminal bicyclooctyne (BCN). It can be used for copper-free strain-promoted azide-alkyne cycloaddition (SPAAC) reaction. Part of a range of functionalized tool molecules for PROTAC R&D.

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.

Usage Guidelines for VH 032 amide-PEG3-BCN

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

Technical Data for VH 032 amide-PEG3-BCN

M. Wt 810.02
Formula C42H59N5O9S
Storage Store at -20°C
Purity ≥90% (HPLC)
CAS Number 2876198-36-4
PubChem ID 169450546
InChI Key WLQVZOBNMRIBKF-LLQRHEORSA-N
Smiles O=C(N1[C@@H](C[C@H](C1)O)C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)[C@H](C(C)(C)C)NC(CCOCCOCCOCCNC(OC[C@H]4[C@]5([H])[C@@]4([H])CCC#CCC5)=O)=O

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 VH 032 amide-PEG3-BCN

References for VH 032 amide-PEG3-BCN

References are publications that support the biological activity of the product.

Liu et al (2021) TF-PROTACs enable targeted degradation of transcription factors. J.Am.Chem.Soc. 143 8902 PMID: 34100597


If you know of a relevant reference for VH 032 amide-PEG3-BCN, please let us know.

Keywords: VH 032 amide-PEG3-BCN, VH 032 amide-PEG3-BCN supplier, PROTACs, degraders, component, VHL, von, Hippel, lindau, E3, ubiquitin, ligase, PEG3, linker, building, block, ligands, targeted, protein, degradation, TPD, BCN, copper, free, strain, promoted, azide, alkyne, cycloaddition, SPAAC, Ligands, Plus, Linkers, 8123, Tocris Bioscience

Citations for VH 032 amide-PEG3-BCN

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Literature in this Area

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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