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.
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