SF-153 is a small molecule inhibitor of UHM splicing factor RBM39 and SPF45 with IC50 of 45.8 uM for both, targets U2 Auxiliary Factor Homology Motif (UHM) domains, exerts anti-tumor activities in leukemia cell lines.
SF-153 shows improved inhibitory activity against UHM-containing proteins compared to UHMCP1, especially against RBM39-UHM and SPF45-UHM.
SF-153 is more effective against RBM39 and SPF45 than three other UHM containing proteins.
SF-153 inhibits cell growth in MV4–11, NKM-1, and K562 cells with IC50 of 17-27 uM.
SF-153 altered cell cycle progression and induced apoptosis differently in NKM-1 and K562 cells.
SF-153 down-regulated ribosomal proteins and genes involved with DNA repair, G2/M checkpoint, and replication in NKM-1 cells.
SF-153 reduced lysosome acidification in NKM-1, K562, and MV4–11 cells, synergized with the SREBP1/2 inhibitor to invoke anti-tumor activity.