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
(Cat. No. 2252) and mitoxantrone
(Cat. No. 4250) in vitro
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The "specific" P-glycoprotein inhibitor Tariquidar is also a substrate and an inhibitor for breast cancer resistance protein (BCRP/ABCG2).
Kannan et al.
ACS Chem.Neurosci., 2011;2:82
Mapping the binding site of the inhibitor Tariquidar that stabilizes the first transmembrane domain of P-glycoprotein.
Loo et al.