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Sigma-Aldrich

Pomalidomide-methylamino-PEG1-NH2 hydrochloride

Synonim(y):

3-((2-(2-Aminoethoxy)ethyl)(methyl)amino)-N-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)propanamide hydrochloride, Crosslinker–E3 Ligase l, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrade

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About This Item

Wzór empiryczny (zapis Hilla):
C21H27N5O6 · xHCl
Masa cząsteczkowa:
445.47 (free base basis)
Kod UNSPSC:
12352101
NACRES:
NA.22

ligand

pomalidomide

Poziom jakości

100

Postać

(Powder or Crystals or Solid or Chunks)

przydatność reakcji

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

grupa funkcyjna

amine

temp. przechowywania

2-8°C

ciąg SMILES

O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NC(CCN(C)CCOCCN)=O)=O)NC1=O.Cl

Zastosowanie

Protein degrader builiding block Pomalidomide-methylamino-PEG1-NH2 hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand, a linker, and a pendant amine for reactivity with a carboxylic acid 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 terminal 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 CRBN-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.

Piktogramy

Health hazard
GHS08

Hasło ostrzegawcze

Warning

Zwroty wskazujące rodzaj zagrożenia

H361d

Zwroty wskazujące środki ostrożności

P201 - P202 - P280 - P308 + P313 - P405 - P501

Klasyfikacja zagrożeń

Repr. 2

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

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
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
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

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