A homo-PROTAC, bivalent small-molecule dimerizer of the VHL E3 ubiquitin ligase to induce self-degradation; induces potent, rapid and proteasome-dependent self-degradation of VHL in different cell lines.

DBCO-S-S-PEG3-biotin is a cleavable reagent for introduction of a biotin moiety to azide-containing biomolecules using copper-free Click Chemistry.?The disulfide bond in this linker can be cleaved using reducing agents such as DTT, BME and TCEP to remove the biotin label.?PEG Linkers can be used in the synthesis of PROTACs.

Gefitinib-based PROTAC 3 is a VHL-recruiting PROTAC that induces the degradation of EGFR and EGFR mutants with DC50 of 11.7 nM and 22.3 nM for HCC827 cell (Exon 19 del) and H3255 cell (L858R).