PROTACPI3Kdelta degrader-1 is a covalent PI3Kdelta-targeting PROTAC degrader that targets lysine, with a DC50 of 3.98 nM. It exhibits potent antiproliferative activity and selective PI3Kdelta inhibition (IC50: 8 nM). Additionally, PROTACPI3Kdelta 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.
Target-Kategorie:
PI3K|||Autophagy|||Akt|||Apoptosis|||PROTACs
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