E3 ligase Ligand-Linker Conjugates 6 Chemical Properties

storage temp. 

2-8°C

form 

Solid

color 

White to yellow

InChIKey

SYAOHFUUVWFWJH-ZBXLSASTSA-N

SMILES

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)=O)=O.Cl

Safety Information

WGK Germany 

WGK 3

Storage Class

11 - Combustible Solids

Hazard Classifications

Acute Tox. 4 Oral
Eye Irrit. 2
Skin Irrit. 2

E3 ligase Ligand-Linker Conjugates 6 Usage And Synthesis

Uses

Protein degrader builiding block (S,R,S)-AHPC-PEG₂-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.

reaction suitability

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

IC 50

VHL

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