A potent and selective inhibitor of the breast cancer resistance protein multidrug transporter (BCRP/ABCG2). Reverses resistance of MTX and topotecan at 25 nM in human and mouse cell lines. Also inhibits ABCB1 and ABCC1 at concentrations >1 μM. Prevents the export of the FAAH inhibitor URB937...
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A potent and selective inhibitor of the breast cancer resistance protein multidrug transporter (BCRP/ABCG2). Reverses resistance of MTX and topotecan at 25 nM in human and mouse cell lines. Also inhibits ABCB1 and ABCC1 at concentrations >1 μM. Prevents the export of the FAAH inhibitor URB937 from the CNS. Forces prostate stem cells to undergo and AR-modulated differentiation to an androgen deprivation therapy-sensitive luminal phenotype. Active in vivo
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ATP binding cassette subfamily G member 2 (ABCG2), also called breast cancer resistance protein (BCRP) or CD338, is a broad-substrate ATP-dependent efflux transporter represented in the ABMIUM catalogue.
Biological function: ABCG2/BCRP is a broad-substrate ATP-dependent transporter that exports physiological compounds, dietary toxins and xenobiotics from cells. It contributes to multidrug resistance and also participates in transport of porphyrins, heme and urate.
