VH 032, thiol

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Description: Functionalized VHL ligand for PROTAC® development
Chemical Name: (2S,4R)-1-((R)-2-Acetamido-3-mercapto-3-methylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥95% (HPLC)
Literature (1)

Biological Activity for VH 032, thiol

VH 032, thiol is a functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC® research and development; incorporates an E3 ligase ligand with thiol group 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, thiol

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

Technical Data for VH 032, thiol

M. Wt 490.64
Formula C23H30N4O4S2
Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 2098836-54-3
PubChem ID 124201834
Smiles CC(N[C@@H](C(C)(S)C)C(N1[C@@H](C[C@H](C1)O)C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)=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, thiol

References for VH 032, thiol

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

Gadd et al (2017) Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat.Chem.Biol. 13 514 PMID: 28288108

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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