BCRP

BCRP inhibitors block breast cancer resistance protein (BCRP), a drug efflux pump in cell membranes. BCRP is ATP-binding cassette (ABC) subfamily G member 2 (ABCG2), a half transporter that works as a homodimer. It was first cloned from drug-selected breast cancer cells, where it conferred resistance to mitoxantrone and anthracyclines. In normal tissues it lines the intestine, bile canaliculi, placenta and blood-brain barrier and limits the entry of many xenobiotics. Inhibitors are used to study drug transport, oral absorption and multidrug resistance in cell and animal models. Ko-143, an analog of the fungal toxin fumitremorgin C, inhibits BCRP selectively. Elacridar blocks both BCRP and P-glycoprotein, listed under P-gp, while YHO-13177 and ML230 are further BCRP inhibitors.

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  • INCB-056868
    Cat. No.
    A65966

    INCB-056868

    INCB-056868 is a metabolite of Epacadostat (M11) that acts as a substrate for the Breast Cancer Resistance Protein (BCRP). This compound is valuable for investigating the mechanisms underlying metabolic diseases and the transport processes mediated by BCRP. Its role in examining drug metabolism and resistance mechanisms makes it a significant reagent for biochemical research.

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