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安全性情報

930512

Sigma-Aldrich

VH 032 amide-PEG3-acid

≥95.0%

別名:

(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

実験式（ヒル表記法）:
C32H46N4O9S
CAS番号:
2140807-42-5
分子量:
662.79
MDL番号:
MFCD32693314
UNSPSCコード:
12352106

ligand

VH032

品質水準

100

アッセイ

≥95.0%

形状

powder

官能基

carboxylic acid

保管温度

2-8°C

SMILES記法

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

アプリケーション

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)

その他情報

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

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable

適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

Jan Code

930512-BULK:
930512-VAR:
930512-50MG:

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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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