SJPYT-195 is a cytotoxic GSPT1 degrader and can be used for PROTAC synthesis.
体内研究:
SJPYT-195 (24 h) potently and efficaciously reduces endogenous PXR (pregnane X receptor) protein in the colorectal SNU-C4 cell line (SNU-C4 3xFLAG-PXR KI cells), with a half maximal degradation concentration (DC50) of 310 ± 130 nM and maximum degradation efficacy (DMax) of 85 ± 1%. SJPYT-195 reduces PXR protein through the degradation of GSPT1.