E3 ligase Ligand-Linker Conjugates 7 Free Base Chemical Properties

Boiling point:

901.7±65.0 °C(Predicted)

Density 

1.230±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

Soluble in Water, DMSO, Methanol

pka

13.54±0.46(Predicted)

form 

Solid

color 

White to off-white

Safety Information

HS Code 

2934100090

E3 ligase Ligand-Linker Conjugates 7 Free Base Usage And Synthesis

Description

(S, R, S)-AHPC-PEG4-amine is a PROTAC linker that incorporates an E3 ligase ligand with a PEG4 unit to empower drug research & discovery. The amine group is reactive with NHS ester or carboxylic acid.

Uses

Protein degrader builiding block (S,R,S)-AHPC-PEG₄-NH₂ (HCl salt) 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 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 blocks with 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.

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