Ceefourin-1 is a highly selective inhibitor of multidrug resistance protein 4 (MRP4/ABCC4), inhibits the efflux of a broad range of MRP4 substrates.
Ceefourin-1 potentiates global cytosolic cAMP accumulation in BE(2)-C neuroblastoma cells following forskolin stimulation.
Ceefourin-1 is relatively non-toxic and well tolerated across a broad range of cell lines with IC50 values typically >50 μM.
Ceefourin-1 reverses 6-MP resistance conferred by MRP4 in HEK293-MRP4 cells, and Ceefourin-1 is more potent than MK-571.
Ceefourin-1 exhibits no activity against cell lines overexpressing P-gp (HEK293-Pgp), ABCG2 (HEK293-ABCG2), and MRP1 (MCF7-VP16).
