Proteasome Degrader

PROTAC 20S proteasome subunit β5 degrader 1 is a PROTAC degrader targeting the 20S proteasome subunit β5, with a DC₅₀ of 0.11 μM. PROTAC 20S proteasome subunit β5 degrader 1 forms a ternary complex with the CRBN E3 ligase, induces ubiquitination of the 20S proteasome subunit β5, and promotes its degradation via the proteasomal pathway. PROTAC 20S proteasome subunit β5 degrader 1 disrupts cell cycle progression, promotes apoptosis, and inhibits cell proliferation and migration. PROTAC 20S proteasome subunit β5 degrader 1 exhibits significant proliferation-inhibitory activity against various tumor cells, suppresses tumor growth in in vivo xenograft models, and overcomes the resistance of multiple myeloma cells to Bortezomib (HY-10227). PROTAC 20S proteasome subunit β5 degrader 1 can be used in studies related to pharyngeal cancer and drug-resistant multiple myeloma.

PROTAC 20S proteasome subunit β5 degrader 2 is a PROTAC degrader targeting the 20S proteasome subunit β5, with a DC₅₀ of 0.16 μM. PROTAC 20S proteasome subunit β5 degrader 2 forms a ternary complex with the CRBN E3 ligase, induces ubiquitination of the 20S proteasome subunit β5, and promotes its degradation via the proteasome. PROTAC 20S proteasome subunit β5 degrader 2 exerts antiproliferative effects in cancer cells and exhibits antitumor activity both in vitro and in vivo. It can be used for the research of pharyngeal cancer and drug-resistant multiple myeloma.