930695
4-Aminomethyl-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione hydrochloride
≥95%
Sinonimo/i:
1H-Isoindole-1,3(2H)-dione, 4-(aminomethyl)-2-(2,6-dioxo-3-piperidinyl) hydrochloride
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About This Item
Formula empirica (notazione di Hill):
C14H13N3O4 · xHCl
Numero CAS:
Peso molecolare:
287.27 (free base basis)
Numero MDL:
Codice UNSPSC:
12352101
NACRES:
NA.26
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Livello qualitativo
Saggio
≥95%
Forma fisica
powder
Impiego in reazioni chimiche
reagent type: ligand
Gruppo funzionale
amine
Temperatura di conservazione
2-8°C
Stringa SMILE
NCC1=C(C(N(C2CCC(NC2=O)=O)C3=O)=O)C3=CC=C1
Applicazioni
4-Aminomethyl-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione hydrochloride is a functionalized Cereblon ligand used for development of protein degrader building blocks. Contains a terminal amine group, allowing rapid conjugation of carboxyl containing linkers. A basic building block for development of a protein degrader library.
Altre note
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
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
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
Protein Degrader Building Blocks
Protein Degrader Building Blocks
Note legali
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
Avvertenze
Danger
Indicazioni di pericolo
Consigli di prudenza
Classi di pericolo
Repr. 1B
Codice della classe di stoccaggio
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
Classe di pericolosità dell'acqua (WGK)
WGK 3
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I documenti relativi ai prodotti acquistati recentemente sono disponibili nell’Archivio dei documenti.
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
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
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
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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