Aurora Kinase Degrader

PROTAC AURKB Degrader-1 is a selective AURKB PROTAC degrader with a DC₅₀ value of 0.6 nM. PROTAC AURKB Degrader-1 promotes ubiquitination and degradation of AURKB. PROTAC AURKB Degrader-1 downregulates the expression levels of chromosomal passenger complex components Borealin, INCENP, Survivin as well as the transcription factor YY1. PROTAC AURKB Degrader-1 induces G₂/M phase arrest and triggers Apoptosis in cells. PROTAC AURKB Degrader-1 serves as a chemical probe for biological studies of the chromosomal passenger complex. PROTAC AURKB Degrader-1 can be used in research related to acute myeloid leukemia, colorectal cancer, and non-small cell lung cancer.

PROTAC Aurora A Degrader-1 is an orally active and blood-brain barrier-permeable selective Aurora A PROTAC degrader. PROTAC Aurora A Degrader-1 induces AURKA degradation with a DC₅₀ of 6 nM in IMR32 cells (D_max = 95%), eliminates both the kinase catalytic activity and N-Myc stabilizing scaffolding function of Aurora A, induces DNA damage, G2/M arrest and apoptosis, and shows antiproliferative activity. PROTAC Aurora A Degrader-1 is applicable to the research of neuroblastoma and small cell lung cancer.