PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
Storage Temp
Store at 2-8°C
Shipped In
Wet ice
Product Description
Description
Protein degrader builiding block (S,R,S)-AHPC-PEG4-NH2(HCl salt) enables the synthesis of molecules fortargeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a von Hippel-Lindau (VHL)-recruiting ligand and a PEGylated crosslinker with pendant amine for reactivity with a carboxyl group 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 blockswith 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.
1.Kedra Cyrus, Marie Wehenkel, Eun-Young Choi, Hyeong-Jun Han, Hyosung Lee, Hollie Swanson, Kyung-Bo Kim,. (2010-10-06) Impact of linker length on the activity of PROTACs.. Molecular bioSystems, 7 ((2)):( 359-364 ). [PMID:20922213]
2.Momar Toure, Craig M Crews,. (2016-01-13) Small-Molecule PROTACS: New Approaches to Protein Degradation.. Angewandte Chemie (International ed. in English), 55 ((6)):( 1966-1973 ). [PMID:26756721]
3.Philipp M Cromm,Craig M Crews. (2017-06-27) Targeted Protein Degradation: from Chemical Biology to Drug Discovery.. Cell chemical biology, 24 ((9)):(1181-1190). [PMID:28648379]
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