A potent and selective inhibitor of the breast cancer resistance protein multidrug transporter (BCRP/ABCG2)1. Reverses resistance of MTX and topotecan at 25 nM in human and mouse cell lines.1 Also inhibits ABCB1 and ABCC1 at concentrations >1 μM.2 Restores the sensitivity of triple negative breast cancer cells to photodynamic therapy.3 Prevents the export of the FAAH inhibitor URB937 from the CNS.4 Forces prostate stem cells to undergo and AR-modulated differentiation to an androgen deprivation therapy-sensitive luminal phenotype.5 Active in vivo.
1) Allen et al. (2002), Potent and specific inhibition of breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C; Mol. Cancer Ther., 1 417
2) Weidner et al. (2015), The Inhibitor Ko143 Is Not Specific for ABCG2; J. Pharmacol. Exp. Ther., 354 384
3) Palasuberniam et al. (2015), ABCG2 transporter inhibitor restores the sensitivity of triple negative breast cancer cells to aminolevulinic acid-mediated photodynamic therapy; Sci. Rep., 5 13298
4) Moreno-Sanz et al. (2011), The ABC membrane transporter ABCG2 prevents access of FAAH inhibitor URB937 to the central nervous system; Pharmacol. Res., 64 359
5) Sabnis et al. (2017), The Effulx Transporter ABCG2 Maintains Prostate Stem Cells; Mol. Cancer Res., 15 128