Application
Protein degrader builiding block (S,R,S)-AHPC-PEG2-butyl CO2H enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a von Hippel-Lindau (VHL)-recruiting ligand, a linker with both hydrophobic and hydrophilic moieties, and a pendant carboxylic acid for reactivity with an amine 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 carboxyl group, 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: Partial PROTACs for Targeted Protein Degradation
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: 660.82. Empirical Formula: C33H48N4O8S. Assay: ≥. 95%. form: crystals. reaction suitability: reactivity: amine reactive, reagent type: ligand-linker conjugate. functional group: carboxylic acid. storage temp.: 2-8°C. SMILES string: O: C(N[C@H](C(N1[C@H](C(NCC2: CC: C(C3: C(C)N: CS3)C: C2): O)C[C@@H](O)C1): O)C(C)(C)C)COCCOCCCCCCC(O): O.Cl. Storage Class Code: 10 - Combustible liquids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 12352306
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 910600-50MG
