PROTAC PI3K? degrader-1

Product Specifications

Target

PI3K|||Autophagy|||Akt|||PROTACs|||Apoptosis

Related Pathways

Apoptosis|||Autophagy|||Cytoskeletal Signaling|||PROTAC|||PI3K/Akt/mTOR signaling

Bioactivity

PROTACPI3K? degrader-1 is a covalent PI3K?-targeting PROTAC degrader that targets lysine, with a DC50 of 3.98 nM. It exhibits potent antiproliferative activity and selective PI3K? inhibition (IC50: 8 nM) . Additionally, PROTACPI3K? degrader-1 effectively degrades p-AKT, induces cell cycle arrest in the G1 phase, and promotes apoptosis and autophagy. It also significantly suppresses tumor growth in the SU-DHL-6 xenograft mouse model.