VH032-OH is a potent and selective ligand for the von Hippel-Lindau (VHL) E3 ubiquitin ligase, commonly used in the development of PROTACs (Proteolysis Targeting Chimeras). Categorized as an E3 Ligase Ligand, VH032-OH provides a functional handle for attaching linkers, enabling the recruitment of VHL to target proteins and inducing their ubiquitination and subsequent degradation via the proteasome. This compound plays a crucial role in targeted protein degradation strategies, facilitating research into new therapeutics for cancer, neurodegenerative diseases, and other conditions driven by disease-related proteins.
Structure of 2244684-42-0
* For research and manufacturing use only. Not for human or clinical use.
| Size | Price | Stock | Quantity |
|---|---|---|---|
| -- | $-- | In stock |
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Background Introduction
VH032-OH is a crucial derivative of VH032, a well-characterized ligand that specifically binds the von Hippel-Lindau (VHL) E3 ubiquitin ligase complex. As an essential building block in the design and synthesis of PROTACs (Proteolysis Targeting Chimeras), VH032-OH features a hydroxyl functional group, allowing facile conjugation to various linkers and target ligands. This structure supports the creation of highly effective heterobifunctional molecules aimed at precision protein degradation.
Mechanism
VH032-OH operates by binding directly to the VHL E3 ligase component, thus facilitating the recruitment of VHL to the PROTAC molecule. When linked to a ligand targeting a protein of interest, VH032-OH enables the formation of a ternary complex that brings the target protein into proximity with the VHL E3 ligase. This interaction drives the ubiquitination and subsequent proteasomal degradation of the target protein, resulting in selective and potent protein knockdown.
Applications
VH032-OH is widely utilized in the design and synthesis of VHL-based PROTACs to achieve targeted and efficient protein degradation. Its reactive hydroxyl moiety is ideal for linker attachment, enabling versatile PROTAC architectures. Key applications include:
• Synthesis of VHL-based PROTAC molecules for drug discovery pipelines| ConcentrationVolumeMass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.05 mL | 10.23 mL | 20.47 mL |
| 5 mM | 0.41 mL | 2.05 mL | 4.09 mL |
| 10 mM | 0.2 mL | 1.02 mL | 2.05 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
* 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
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