ligand
C5 Lenalidomide
Quality Level
assay
≥95%
form
powder or crystals
reaction suitability
reactivity: carboxyl reactive, reagent type: ligand-linker conjugate
functional group
amine
storage temp.
2-8°C
SMILES string
O=C1N(C2CCC(NC2=O)=O)CC3=CC(NC(CCCCCCN)=O)=CC=C31.Cl
InChI key
BQPYHWPMMOFXIA-UHFFFAOYSA-N
Application
Protein degrader builiding block C5 Lenalidomide-C6-NH2 hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand with alternative exit vector and an alkyl-chain crosslinker with pendant amine for reactivity with an acid on the target warhead. Because even slight alterations in ligands, warheads, 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 terminal amine, 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
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
Legal Information
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
signalword
Warning
hcodes
Hazard Classifications
Repr. 2 - STOT RE 2
target_organs
Blood
存储类别
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
商品
Protein Degrader Building Blocks are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| 911712-2.1MG-KC | 04065272328098 |
| 911712-50MG | 04061841752608 |
