Description
Mal-PEG2-acid is a PEG linker containing a maleimide group with a terminal carboxylic acid. The hydrophilic PEG spacer increases solubility in aqueous media. The maleimide group will react with a thiol group to form a covalent bond, enabling the connection of biomolecule with a thiol. The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond.
Uses
Mal-PEG2-acid can couple with amino-containing target protein ligands to form PROTAC ternary complexes, which mediate ubiquitination and degradation of oncogenic target proteins and are widely used in the medicinal chemistry research and development of degradative agents for tumor and inflammation-related target proteins.
Biological Activity
Mal-PEG2-acid is a non-cleavable ADC linker for the synthesis of antibody-drug conjugates (ADCs). It can bind to Tubulysin (HY-128914) and its cytotoxic derivatives activity. It can also be used as a PROTAC linker for PROTAC synthesis.
in vitro
ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker.
target
| Non-cleavable < span> | PEGs |
