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930547

Sigma-Aldrich

Pomalidomide-PEG1-C2-azide

≥95.0%

Synonim(y):

1H-Isoindole-1,3(2H)-dione, 4-[[2-(2-azidoethoxy)ethyl]amino]-2-(2,6-dioxo-3-piperidinyl), 4-((2-(2-Azidoethoxy)ethyl]amino]-2-(2,6-dioxopiperidin-3-yl]isoindoline-1,3-dione, 4-[[2-(2-Azidoethoxy)ethyl]amino]-2-(2,6-dioxo-3-piperidinyl)-1H-isoindole-1,3(2H)-dione

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About This Item

Wzór empiryczny (zapis Hilla):
C17H18N6O5
Numer CAS:
2271036-44-1
Masa cząsteczkowa:
386.36
Numer MDL:
MFCD32693891
Kod UNSPSC:
12352125
NACRES:
NA.21

ligand

pomalidomide

Poziom jakości

100

Próba

≥95.0%

Formularz

powder

grupa funkcyjna

azide

temp. przechowywania

2-8°C

ciąg SMILES

[N-]=[N+]=NCCOCCNC1=CC=CC=2C(=O)N(C(=O)C12)C3C(=O)NC(=O)CC3

Klucz InChI

NJPMWHWTBBYBDY-UHFFFAOYSA-N

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Zastosowanie

Pomalidomide-PEG1-C2-azide is a functionalized cereblon ligand for development of pomalidomide-based PROTACs. Contains an alkyne, allowing for conjugation through click chemistry. A basic building block for development of a protein degrader library.

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

Protein Degrader Building Blocks

Inne uwagi

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
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Kod klasy składowania

11 - Combustible Solids

Klasa zagrożenia wodnego (WGK)

WGK 3

Temperatura zapłonu (°F)

Not applicable

Temperatura zapłonu (°C)

Not applicable

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Certyfikaty analizy (CoA)

Lot/Batch Number
0000204797
0000204797

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Odwiedź Bibliotekę dokumentów

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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