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Merck
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文件

930695

Sigma-Aldrich

4-Aminomethyl-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione hydrochloride

≥95%

别名:

1H-Isoindole-1,3(2H)-dione, 4-(aminomethyl)-2-(2,6-dioxo-3-piperidinyl) hydrochloride

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About This Item

经验公式（希尔记法）:
C14H13N3O4 · xHCl
CAS号:
444287-40-5
分子量:
287.27 (free base basis)
MDL號碼:
MFCD30188072
分類程式碼代碼:
12352101
NACRES:
NA.26

品質等級

100

化驗

≥95%

形狀

powder

反應適用性

reagent type: ligand

官能基

amine

儲存溫度

2-8°C

SMILES 字串

NCC1=C(C(N(C2CCC(NC2=O)=O)C3=O)=O)C3=CC=C1

相关类别

應用

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.

其他說明

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
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
Protein Degrader Building Blocks

法律資訊

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

象形圖

Health hazard
GHS08

訊號詞

Danger

危險聲明

H360D

危險分類

Repr. 1B

儲存類別代碼

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

水污染物質分類（WGK）

WGK 3

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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
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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