Application
Protein degrader building block C5 Lenalidomide-pyridine-PEG1-piperazine 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, a linker with added rigidity, and a pendant amine for reactivity with a carboxylic acid 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 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
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
Molecular Weight: 520.58 (free base basis). Empirical Formula: C27H32N6O5 · xHCl. Quality Level: 100. 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(CC4: CC: C(OCCCN5CCNCC5)N: C4): O): CC: C31.Cl. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.Shipping Information:
Dry Ice Surcharge & Ice Pack Shipments: $40
More Information: https://cenmed.com/shipping-returns
- UPC:
- 12352200
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 920797-50MG
- Temperature Control Device:
- Yes
