PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells.In Vitro: PROTAC-O4I2 introduces Thalidomide to ubiquitin E3 ligase cereblon (CRBN), which selectively degrades SF3B1 and inhibits tumor growth in cells.
PROTAC-O4I2 degrades and inhibits SF3B1 in K562 cells. PROTAC-O4I2 exhibits anti-proliferation effects on SF3B1 WT, SF3B1 OE, and SF3B1 K700E cells with IC50s of 228, 63, and 90 nM, respectively.
PROTAC-O4I2 induces FLAG-SF3B1 degradation in a concentration-dependent manner with a half maximal inhibitory concentration (IC50) value of 0.244 μM in K562 cells.In Vivo: PROTAC-O4I2 (10 μM) significantly increases survival by interference with the maintenance and proliferation of tumor in a Drosophila intestinal tumor model.