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Merck

930717

Sigma-Aldrich

1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-5-(4-piperidinyloxy) hydrochloride

≥95%

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About This Item

Fórmula empírica (notación de Hill):
C18H19N3O5 · xHCl
Número de CAS:
Peso molecular:
357.36 (free base basis)
MDL number:
UNSPSC Code:
12352101
NACRES:
NA.22

Quality Level

assay

≥95%

form

powder

functional group

amine

storage temp.

2-8°C

SMILES string

O=C1NC(C(CC1)N2C(C3=CC=C(C=C3C2=O)OC4CCNCC4)=O)=O

Application

1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-5-(4-piperidinyloxy) 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.


Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation


Protein Degrader Building Blocks

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

signalword

Danger

hcodes

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


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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
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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
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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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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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