VH 032, propargyl

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Description: Alkyne-functionalized VH 032; 'click' VHL ligand for PROTACs
Chemical Name: (2S,4R)-1-((S)-3,3-Dimethyl-2-(2-(prop-2-yn-1-yloxy)acetamido)butanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥95% (HPLC)
Datasheet
Citations
Reviews
Literature (1)

Biological Activity for VH 032, propargyl

VH 032, propargyl is a functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC® research and development; incorporates an E3 ligase ligand with terminal propargyl ready for conjugation to a target protein ligand. 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, propargyl

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

Technical Data for VH 032, propargyl

M. Wt 526.65
Formula C27H34N4O5S
Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 2098799-78-9
Smiles CC1=C(C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(COCC#C)=O)=O)O)=O)SC=N1

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, propargyl

References for VH 032, propargyl

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

Wurz et al (2018) A "click chemistry platform" for the rapid synthesis of bispecific molecules for inducing protein degradation. J.Med.Chem. 61 453 PMID: 28378579


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Keywords: VH 032, propargyl, VH 032, propargyl supplier, VH032,, propargyl, Proteolysis, Targeting, Chimera, PROTACs, VHL, E3, ubiquitin, ligase, conjugate, PROTAC, polyethene, glycol, von-Hippel-Lindau, protein, ligand, terminal, Functionalized, Ligase, Ligands, 6683, Tocris Bioscience

Citations for VH 032, propargyl

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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