E3 ligase Ligand-Linker Conjugates 9 Chemical Properties

Boiling point:

963.4±65.0 °C(Predicted)

Density 

1.195±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

Ethanol: 100 mg/mL (120.85 mM); DMSO: ≥ 100 mg/mL (120.85 mM)

pka

13.54±0.46(Predicted)

E3 ligase Ligand-Linker Conjugates 9 Usage And Synthesis

Uses

Protein degrader builiding block (S,R,S)-AHPC-PEG₆-Butyl chloride 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 chloroalkane for reactivity with a nucleophilic group on 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 chloro group, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.