VH 032, amine

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Cat.No. 6462 - VH 032, amine | C22H30N4O3S.2HCl | CAS No. 2137142-47-1
Description: Functionalized VHL ligand for PROTACs
Chemical Name: (4R)-3-Methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-L-prolinamide dihydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (1)

Biological Activity

Derivative of the von Hippel-Lindau (VHL) ligand, VH 032; commonly used as a precursor to a PROTAC® that hijacks VHL as the E3 ubiquitin ligase component. Supplied with a primary amine functional handle at a position known not to significantly affect binding to VHL, for ready conjugation to a linker/target protein ligand.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

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Usage guidelines:

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

Technical Data

M. Wt 503.49
Formula C22H30N4O3S.2HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 2137142-47-1
PubChem ID 118864076
InChI Key SADPMNNWFOJMCY-ZNZDOTFASA-N
Smiles CC1=C(C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)N)=O)O)=O)SC=N1.Cl.Cl

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

Certificate of Analysis / Product Datasheet
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References

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

Zengerle et al (2015) Selective small molecule induced degradation of the BET bromodomain protein BRD4. ACS Chem.Biol. 10 1770 PMID: 26035625

Galdeano et al (2014) Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von Hippel-Lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities. J.Med.Chem. 57 8657


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Keywords: VH 032, amine, VH 032, amine supplier, VH032, amine, 2HCl, protein, degrader, 1, VHL, VL, 269, PROTACs, E3, ligase, ligands, Functionalized, Ligase, Ligands, 6462, Tocris Bioscience

1 Citation for VH 032, amine

Citations are publications that use Tocris products. Selected citations for VH 032, amine include:

Smalley et al (2020) PROTAC-mediated degradation of class I histone deacetylase enzymes in corepressor complexes. Chem.Commun.(Camb) 56 4476 PMID: 32201871


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

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Targeted Protein Degradation

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