WCF-598 is a RXRgamma (Kd: 234.2 nM) PROTAC degrader. WCF-598 induces RXRgamma degradation via the ubiquitin-proteasome pathway and binds directly to RXRgamma. WCF-598 indirectly induces AR-V7 degradation, impairs the stability of the RXRgamma-AR-V7 complex, downregulates AR-V7 levels, and inhibits the transcription of downstream target genes of AR-V7. WCF-598 induces tumor cell apoptosis, inhibits cell proliferation, activates the p53 signaling pathway, and suppresses cell cycle progression. WCF-598 can be used for the research of prostate cancer[1].
