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Merck

901850

Sigma-Aldrich

(S,R,S)-AHPC-PEG5-NH2 hydrochloride

Synonim(y):

(2S,4R)-1-((S)-20-Amino-2-(tert-butyl)-4-oxo-6,9,12,15,18-pentaoxa-3-azaicosanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide hydrochloride, Crosslinker−E3 ligase ligand conjugate, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader, VH032 conjugate

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About This Item

Wzór empiryczny (zapis Hilla):
C34H54ClN5O9S
Masa cząsteczkowa:
744.34
Kod UNSPSC:
12352101
NACRES:
NA.22

ligand

VH032

Postać

crystals

przydatność reakcji

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

grupa funkcyjna

amine

temp. przechowywania

2-8°C

ciąg SMILES

O=C(COCCOCCOCCOCCOCCN)N[C@H](C(N1[C@H](C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O)C(C)(C)C.Cl

Zastosowanie

Protein degrader building block (SRS)-AHPC-PEG5-NH2 (HCl salt) enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a von Hippel–Lindau (VHL)-recruiting ligand and a PEGylated crosslinker with pendant amine for reactivity with a carboxyl group on the target ligand. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target E3 ligase and PROTAC many analogs are prepared to screen for optimal target degradation.When used with other protein degrader building blocks with a pendant amine parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length composition and E3 ligase ligand.

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

Informacje prawne

PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
This page may contain text that has been machine translated.

produkt powiązany

Numer produktu
Opis
Cennik

Kod klasy składowania

11 - Combustible Solids

Klasa zagrożenia wodnego (WGK)

WGK 3

Temperatura zapłonu (°F)

Not applicable

Temperatura zapłonu (°C)

Not applicable


Certyfikaty analizy (CoA)

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Dokumenty związane z niedawno zakupionymi produktami zostały zamieszczone w Bibliotece dokumentów.

Odwiedź Bibliotekę dokumentów

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
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

Produkty

Protein Degrader Building Blocks are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

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