910503
Pomalidomide-PEG2-butyl alkyne
≥95%
别名:
N-(2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)-2-(2-(oct-7-yn-1-yloxy)ethoxy)acetamide, Crosslinker−E3 Ligase ligand conjugate, Pomalidomide conjugate, Pomalidomide-2-2-6-alkyne, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader
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关于此项目
经验公式（希尔记法）:
C25H29N3O7
分子量:
483.51
UNSPSC Code:
51171641
ligand
pomalidomide
assay
≥95%
form
(Liquid or Semi-Solid or Paste or Solid)
reaction suitability
reaction type: click chemistry, reagent type: ligand-linker conjugate
functional group
alkyne
storage temp.
2-8°C
SMILES string
O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NC(COCCOCCCCCCC#C)=O)=O)NC1=O
Application
Protein degrader builiding block Pomalidomide-PEG2-butyl alkyne enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand, a linker with both hydrophobic and hydrophilic moieties, and a pendant alkyne for click chemistry with an azide on the target ligand. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and PROTAC, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a pendant alkyne, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
Other Notes
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
Portal: Building PROTAC® Degraders for Targeted Protein Degradation
Targeted Protein Degradation by Small Molecules
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
Portal: Building PROTAC® Degraders for Targeted Protein Degradation
Targeted Protein Degradation by Small Molecules
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
存储类别
13 - Non Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
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Protein Degrader Building Blocks are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.
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
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