VH032-PEG5-C6-Cl

 CAS No.: 1799506-06-1  Cat No.: BP-400039 4.5  

VH032-PEG5-C6-Cl is a high-purity E3 ligase ligand-linker conjugate designed for advanced PROTAC (Proteolysis Targeting Chimera) drug discovery and targeted protein degradation research. This compound features the VHL-based ligand VH032, a well-characterized small molecule that selectively engages the Von Hippel-Lindau (VHL) E3 ubiquitin ligase, tethered through a flexible PEG5 (polyethylene glycol, 5 units) linker and finished with a C6-chloride functional group for easy payload conjugation.

VH032-PEG5-C6-Cl

Structure of 1799506-06-1

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Category
E3 Ligase Ligand-Linker Conjugate
Molecular Formula
C38H59ClN4O9S
Molecular Weight
783.41

* For research and manufacturing use only. Not for human or clinical use.

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Solubility
DMSO : ≥ 50 mg/mL
Storage
-20°C, protect from light<br/>*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Shipping
Room temperature in continental US; may vary elsewhere
Synonyms
VH032-PEG5-C6-Cl; HaloPROTAC 2; N-[2-[[2-[2-[2-[2-[2-(6-chlorohexoxy)ethoxy]ethoxy]ethoxy]ethoxy]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-1-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide
InChI Key
XWSLAICADDJNNG-UHFFFAOYSA-N
InChI
InChI=1S/C38H59ClN4O9S/c1-28-34(53-27-40-28)30-11-9-29(10-12-30)24-43-25-31(44)23-32(43)36(46)42-37(47)35(38(2,3)4)41-33(45)26-52-22-21-51-20-19-50-18-17-49-16-15-48-14-8-6-5-7-13-39/h9-12,27,31-32,35,44H,5-8,13-26H2,1-4H3,(H,41,45)(H,42,46,47)
Canonical SMILES
CC1=C(SC=N1)C2=CC=C(C=C2)CN3CC(CC3C(=O)NC(=O)C(C(C)(C)C)NC(=O)COCCOCCOCCOCCOCCCCCCCl)O

Background Introduction

VH032-PEG5-C6-Cl is a versatile E3 ligase ligand-linker conjugate commonly used in the design and synthesis of PROTACs (Proteolysis Targeting Chimeras). Leveraging the recognized VH032 moiety, which is a potent ligand for the von Hippel-Lindau (VHL) E3 ubiquitin ligase, this conjugate features a PEG5 (polyethylene glycol, five units) spacer and a reactive C6-chloride tail ready for further chemical modification. This optimized composition facilitates robust and modular PROTAC assembly for targeted protein degradation research in chemical biology and drug discovery.

Mechanism

The mechanism of VH032-PEG5-C6-Cl centers on its function as a bifunctional E3 ligase recruiter. The VH032 moiety binds specifically and tightly to the VHL E3 ligase complex. The PEG5 linker imparts flexibility and spatial separation, critical for effective ternary complex formation in PROTACs. The terminal C6-chloride functions as a reactive handle for covalent conjugation to a ligand that binds the target protein of interest. Once incorporated into a PROTAC molecule, VH032-PEG5-C6-Cl facilitates the recruitment of the VHL E3 ligase to the target protein, promoting its ubiquitination and subsequent degradation by the proteasome.

Applications

VH032-PEG5-C6-Cl is broadly utilized in PROTAC research and development. It serves as an essential building block for synthesizing VHL-based PROTACs designed to selectively degrade disease-related proteins. Researchers use this conjugate to craft custom degrader molecules against challenging targets in oncology, neurodegeneration, immunology, and other therapeutic areas. Owing to its modular design, VH032-PEG5-C6-Cl streamlines the rapid generation and optimization of PROTAC libraries, accelerating hit identification and lead optimization in drug discovery pipelines.

• Flexible PEG5 and C6 linker enables optimal spatial arrangement for efficient target protein degradation.
• Chloride-functionalized VH032 ligand ensures high specificity and reliable binding to VHL E3 ligase in PROTAC design.

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L

* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2

* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
g/mol
g

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