PROTAC-O4I2, a PROTAC ligand targeting splicing factor 3B1 (SF3B1), induced FLAG-SF3B1 degradation in K562 cells with an IC50 value of 0.244 μM. PROTAC-O4I2 induced apoptosis in K562 WT cells.

PROTAC-O4I2 introduces thalidomide into the ubiquitin E3 ligase cereblon (CRBN), thereby selectively degrading SF3B1 and inhibiting tumor growth in cells.[1]
PROTAC-O4I2 degrades and inhibits SF3B1 in K562 cells. PROTAC-O4I2 has anti-proliferative effects on SF3B1 WT, SF3B1 OE, and SF3B1 K700E cells with IC50 of 228, 63, and 90 nM, respectively.[1]
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.[1]

Flies were fed on a round filter paper loaded with PROTAC-O4I2 (10 μM) in a 5% sucrose solution, maintained at 18℃, and flipped into a freshly prepared vial every 2 days. PROTAC-O4I2 significantly improves Drosophila survival in a Drosophila intestinal tumor model by interfering with tumor maintenance and proliferation.[1]