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Documentos

934275

Sigma-Aldrich

Pomalidomide-piperazine

≥ 95.0%

Sinónimos:

1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-(1-piperazinyl)-2-(2,6-Dioxopiperidin-3-yl)-4-(piperazin-1-yl)isoindole-1,3-dione

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About This Item

Fórmula empírica (notación de Hill):
C17H18N4O4
Número de CAS:
2154342-57-9
Peso molecular:
342.35
MDL number:
MFCD32898791
UNSPSC Code:
12352200
NACRES:
NA.21

ligand

pomalidomide

Quality Level

100

assay

≥ 95.0%

form

powder or crystals

color

faint yellow to dark yellow

storage temp.

2-8°C

SMILES string

O=C1NC(=O)C(N2C(=O)C3=CC=CC(=C3C2=O)N4CCNCC4)CC1

Application

A functionalized cereblon ligand for development of Pomalidomide based PROTACs. Allows rapid conjugation with carboxyl linkers due to presence of amine group via peptide coupling reactions. Amenable for linker attachement via reductive amination; and a basic building block for making protein degrader library.

Technology Spotlight:

Degrader Building Blocks for Targeted Protein Degradation

Protein Degrader Building Blocks

Other Notes

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

Legal Information

PROTAC® is a registered trademark of Arvinas Operations; Inc.; and is used under license.
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license

pictograms

Health hazard
GHS08

signalword

Danger

hcodes

H360D

Hazard Classifications

Repr. 1B

Storage Class

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

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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
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
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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