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Sigma Aldrich (S R S)-Ahpc-Pyridine-Peg1-Piperazine Hydrochloride

Catalog No. 92143250MG Shop All MilliporeSigma Sigma Organic Chemistry Products
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92-143-250MG 250 mg
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Description

MilliporeSigma Sigma Organics products encompass a wide range of quality reagents, solvents, catalysts, and building blocks for organic synthesis. From benchtop discovery to process development and scale-up, Sigma Organics solutions are built to meet the needs of synthetic chemists.

Protein degrader building block (S,R,S)-AHPC-pyridine-PEG1-piperazine hydrochloride 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, 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 terminal amine, 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 DegradationPortal: Building PROTAC™ Degraders for Targeted Protein DegradationTargeted Protein Degradation by Small MoleculesSmall-Molecule PROTACS: New Approaches to Protein DegradationTargeted Protein Degradation: from Chemical Biology to Drug DiscoveryImpact of linker length on the activity of PROTACsPROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license

Specifications

CAS 8778-1-9-8
Quantity 250 mg
Synonym (2S,4R)-N-{[2-(2-{[2-(2-aminoethoxy)ethyl](methyl)amino}ethoxy)-4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}-4-hydroxy-1-[(2S)-3-methyl-2-(1-oxo-2,3-dihydro-1H-isoindol-2-yl)butanoyl]pyrrolidine-2-carboxamide; Crosslinker-E3 Ligase ligand conjugate; VHL protein degrader building block for PROTAC(R) research
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