Application
Protein degrader building block 6F,C5-Pomalidomide-4-piperidine-C1-piperazine hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC® (proteolysis-targeting chimeras) research. This conjugate contains a Cereblon (CRBN) recruiting ligand, a rigid linker, 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 degrader, 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 degrader libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
Protein Degrader Building Blocks
Other Notes
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: 457.50 (free base basis). Empirical Formula: C23H28FN5O4 · xHCl. reaction suitability: reactivity: carboxyl reactive, reagent type: ligand-linker conjugate. Quality Level: 100. functional group: amine. storage temp.: 2-8°C. SMILES string: O: C1C(N2C(C(C: C(F)C(N(CC3)CCC3CN4CCNCC4): C5): C5C2: O): O)CCC(N1): O.Cl. Pictograms: GHS08. Signal Word: Danger. Hazard Statements: H360D. Precautionary Statements: P201 - P202 - P280 - P308 + P313 - P405 - P501. Hazard Classifications: Repr. 1B. Storage Class Code: 6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51453013
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 923958-50MG
