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901860

Sigma-Aldrich

(S,R,S)-AHPC-PEG6-NH2 hydrochloride

≥95%

Synonim(y):

(2S,4R)-1-((S)-23-Amino-2-(tert-butyl)-4-oxo-6,9,12,15,18,21-hexaoxa-3-azatricosanoyl)-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):
C36H58ClN5O10S
Masa cząsteczkowa:
788.39
Kod UNSPSC:
12352101
NACRES:
NA.22

ligand

VH032

Próba

≥95%

Postać

powder or crystals

przydatność reakcji

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

grupa funkcyjna

amine

temp. przechowywania

2-8°C

ciąg SMILES

O=C(COCCOCCOCCOCCOCCOCCN)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 (S,R,S)-AHPC-PEG6-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)

Inne uwagi

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

Portal: Building PROTAC® Degraders for Targeted Protein Degradation

Targeted Protein Degradation by Small Molecules

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

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.

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(S,R,S)-VL285 Phenol-C2-NH2 hydrochloride

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(S,R,S)-VL285 Phenol-PEG1-piperazine hydrochloride

920827

(S,R,S)-AHPC-methylamino-PEG1-NH2 hydrochloride

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(S,R,S)-VL285 Phenol

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(S,R,S)-VL285 Phenol-PEG4-NH2 hydrochloride

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(S,R,S)-VL285 Phenol-PEG2-NH2 hydrochloride

921432

(S,R,S)-AHPC-pyridine-PEG1-piperazine hydrochloride

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(S,R,S)-VL285 Phenol-C6-NH2 hydrochloride

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(S,R,S)-VL285 Phenol-C3-piperazine hydrochloride

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(S,R,S)-VL285 Phenol-methylamino-PEG1-NH2 hydrochloride

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920835

(S,R,S)-VL285 Phenol-piperazine-pyridine-alkyne-NH2 hydrochloride

Piktogramy

Exclamation mark
GHS07

Hasło ostrzegawcze

Warning

Zwroty wskazujące rodzaj zagrożenia

H302,H315,H319

Klasyfikacja zagrożeń

Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2

Kod klasy składowania

11 - Combustible Solids

Klasa zagrożenia wodnego (WGK)

WGK 3

Temperatura zapłonu (°F)

Not applicable

Temperatura zapłonu (°C)

Not applicable

Wybierz jedną z najnowszych wersji:

Certyfikaty analizy (CoA)

Lot/Batch Number
MKCH3419

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Odwiedź Bibliotekę dokumentów

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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
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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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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

Produkty

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