VH 101, acid

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Description: VHL ligand, carboxylic acid functionalized at the benzylic position
Chemical Name: (S)-3-[[[(2S,4R)-1-[(S)-2-(1-Fluorocyclopropan-1-ylcarbonylamino)-3,3-dimethylbutanoyl]-4-hydroxypyrrolidin-2-yl]carbonyl]amino]-3-[4-(4-methylthiazol-5-yl)phenyl]propanoic acid
Purity: ≥98% (HPLC)
Literature (1)

Biological Activity for VH 101, acid

VH 101, acid is a functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC® research and development; incorporates an E3 ligase ligand with carboxylic acid handle at the benzylic position 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 101, acid

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

Technical Data for VH 101, acid

M. Wt 574.67
Formula C28H35FN4O6S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2408341-97-7
PubChem ID 156701284
Smiles CC1=C(SC=N1)C2=CC=C([C@H](CC(O)=O)NC([C@@H]3C[C@@H](O)CN3C([C@@H](NC(C4(CC4)F)=O)C(C)(C)C)=O)=O)C=C2

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.

References for VH 101, acid

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

Kofink et al (2022) A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo. ChemRxiv - not yet peer reviewed 13 5969 PMID: 36216795

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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