Catalog No.: PC-23133Not For Human Use, Lab Use Only.
SMARCA2 PROTAC YD23 is a potent and selective proteolysis targeting chimera (PROTAC) targeting SMARCA2 with DC50 of 64 nM in H1792 cells and Dmax of 88%.
SMARCA2 PROTAC YD23 is a potent and selective proteolysis targeting chimera (PROTAC) targeting SMARCA2 with DC50 of 64 nM in H1792 cells and Dmax of 88%. YD23 selectively degrades SMARCA2 and inhibits the growth of SMARCA4-mutant lung cancer cell lines. YD23 exhibits DC50 of 297 nM and a Dmax of 95% in H1975 SMARCA4-WT cells, minimal impact on SMARCA4 up to 10 μM. YD23 potently degraded SMARCA2 with a median DC50 of 92.8 nM and achieving a Dmax of 90% on an additional panel of ten SMARCA4-WT cell lines. YD23 selectively inhibits growth of SMARCA4-mutant lung cancer cell lines with IC50 of 0.11 uM (SMARCA4-WT cells, IC50=6 uM). SMARCA2 degradation disrupts chromatin accessibility at enhancers to disable cell cycle transcriptional programs. YD23 (12.5 mg/kg) inhibits growth of SMARCA4-mutant xenograft models of lung cancer.
