(S,R,S)-AHPC-PEG2-azide 904813-50MG
Empirical Formula (Hill Notation): | C28H39N7O6S |
CAS Number: | 2010159-45-0 |
Molecular Weight: | 601.72 |
Protein degrader builiding block (
S,
R,
S)-AHPC-PEG2-azide 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 and a PEGylated crosslinker with pendant azide for click chemistry with a 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 azide group, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation,
Portal: Building PROTAC® Degraders for Targeted Protein Degradation,
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds,
Structural basis of PROTAC cooperative recognition for selective 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,
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
assay | 95% |
form | solid |
reaction suitability | reaction type: click chemistry |
storage temp. | 2-8°C |
SMILES string | O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H](C[C@@H](O)C3)N3C([C@H](C(C)(C)C)NC(COCCOCCN=[N+]=[N-])=O)=O, O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H](C[C@@H](O)C3)N3C([C@H](C(C)(C)C)NC(COCCOCCN=[N+]=[N-])=O)=O |
WGK Germany | WGK 3 |
Flash Point F | Not applicable |
Flash Point C | Not applicable |