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Submit ReviewVH 101, thiol
Description: Thiol functionalized VHL ligand
Chemical Name: (2S,4R)-1-[(2R)-2-[[(1-Fluorocyclopropyl)carbonyl]amino]-3-methyl-3-sulfanyl-butanoyl]-4-hydroxy-N-[[4-(4-methylthiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide
Purity: ≥95% (HPLC)
Biological Activity for VH 101, thiol
VH 101, thiol is a functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC® research and development; incorporates an E3 ligase ligand with terminal thiol 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, thiol
This product is provided for use in onward chemistry. Suitable solvents can be used.
Technical Data for VH 101, thiol
| M. Wt | 534.67 |
| Formula | C25H31FN4O4S2 |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 2358775-81-0 |
| InChI Key | RCVHBJGYHDKFGZ-WSTZPKSXSA-N |
| Smiles | O=C(C1(CC1)F)N[C@@H](C(C)(S)C)C(N2[C@@H](C[C@H](C2)O)C(NCC3=CC=C(C4=C(N=CS4)C)C=C3)=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 101, thiol
References for VH 101, thiol
References are publications that support the biological activity of the product.
Liu et al (2022) Discovery of XL01126: a potent, fast, cooperative, selective, orally bioavailable, and blood-brain barrier penetrant PROTAC degrader of leucine-rich repeat kinase 2. J.Am.Chem.Soc. 144 16930 PMID: 36007011
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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