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930512

Sigma-Aldrich

VH 032 amide-PEG3-acid

≥95.0%

Synonym(e):

(S, R, S)-AHPC-PEG3-acid, 3-Dimethyl-1-oxobutan-2-yl]carbamoyl}ethoxy)ethoxy]ethoxy}propanoic acid, 3-{2 -[2-(2-{[(2S)-1-[(2S,4R)-4-Hydroxy-2-({[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}carbamoyl)pyrrolidin-1-yl]-3, N-[3-[2-[2-(2-Carboxyethoxy)ethoxy]ethoxy]-1-oxopropyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, L-Prolinamide

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About This Item

Empirische Formel (Hill-System):
C32H46N4O9S
CAS-Nummer:
2140807-42-5
Molekulargewicht:
662.79
MDL-Nummer:
MFCD32693314
UNSPSC-Code:
12352106

ligand

VH032

Qualitätsniveau

100

Assay

≥95.0%

Form

powder

Funktionelle Gruppe

carboxylic acid

Lagertemp.

2-8°C

SMILES String

OC(CCOCCOCCOCCC(N[C@@H](C(C)(C)C)C(N1[C@@H](C[C@H](C1)O)C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)=O)=O)=O

Anwendung

VH 032 amide-PEG3-acid is a functionalized von-Hippel-Lindau (VHL) ligand with a terminal carboxyl group, allowing rapid conjugation of amine containing linkers. A basic building block for development of a protein degrader library.

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation


Protein Degrader Building Blocks

Automate your VHL-PEG based PROTACs with Synple Automated Synthesis Platform (SYNPLE-SC002)

Sonstige Hinweise

Targeted Protein Degradation by Small Molecules

Destruction of DNA-Binding Proteins by Programmable Oligonucleotide PROTAC (O′PROTAC): Effective Targeting of LEF1 and ERG

Small-Molecule PROTACS: New Approaches to Protein Degradation

Targeted Protein Degradation: from Chemical Biology to Drug Discovery

Impact of linker length on the activity of PROTACs

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

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Jingwei Shao et al.
Advanced science (Weinheim, Baden-Wurttemberg, Germany), 8(20), e2102555-e2102555 (2021-08-17)
DNA-binding proteins, including transcription factors (TFs), play essential roles in various cellular processes and pathogenesis of diseases, deeming to be potential therapeutic targets. However, these proteins are generally considered undruggable as they lack an enzymatic catalytic site or a ligand-binding
Daniel P Bondeson et al.
Annual review of pharmacology and toxicology, 57, 107-123 (2016-10-13)
Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Whereas therapeutics have been developed to disrupt protein homeostasis, more recently identified techniques have been used to repurpose homeostatic networks to effect degradation of
Kedra Cyrus et al.
Molecular bioSystems, 7(2), 359-364 (2010-10-06)
Conventional genetic approaches have provided a powerful tool in the study of proteins. However, these techniques often preclude selective manipulation of temporal and spatial protein functions, which is crucial for the investigation of dynamic cellular processes. To overcome these limitations
Momar Toure et al.
Angewandte Chemie (International ed. in English), 55(6), 1966-1973 (2016-01-13)
The current inhibitor-based approach to therapeutics has inherent limitations owing to its occupancy-based model: 1) there is a need to maintain high systemic exposure to ensure sufficient in vivo inhibition, 2) high in vivo concentrations bring potential for off-target side effects, and 3) there is
Philipp M Cromm et al.
Cell chemical biology, 24(9), 1181-1190 (2017-06-27)
Traditional pharmaceutical drug discovery is almost exclusively focused on directly controlling protein activity to cure diseases. Modulators of protein activity, especially inhibitors, are developed and applied at high concentration to achieve maximal effects. Thereby, reduced bioavailability and off-target effects can

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