A P-glycoprotein inhibitor
Potent P-glycoprotein (P-gp) inhibitor (IC50 = 5.1 nM). Reverses drug resistance in multiple MDR cell lines. Acts as a substrate for breast cancer resistance protein (BCRP) at low concentrations and acts as an inhibitor of BCRP when used at >100 nM concentration. Potentiates the cytotoxic effects of doxorubicin and mitoxantrone in vitro.
Kannan et al (2011) The "specific" P-glycoprotein inhibitor Tariquidar is also a substrate and an inhibitor for breast cancer resistance protein (BCRP/ABCG2). ACS Chem.Neurosci. 2 82 PMID:22778859 |Loo et al (2015) Mapping the binding site of the inhibitor Tariquidar that stabilizes the first transmembrane domain of P-glycoprotein. J.Biol.Chem. 290 29389 PMID:26507655
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