Breast cancer resistance protein (BCRP/ABCG2/MXR/ABCP) is a member of the G subfamily of the large ATP-binding cassette (ABC) transporter family found on cell membranes. It is an ATP-dependent efflux transporter. Xenobiotic efflux transporter BCRP is expressed in a variety of healthy cells. Cancer chemotherapeutic resistance and BCRP are frequently linked. Multidrug resistance (MDR) is conferred by BCRP to a number of antitumor drugs, including Mitoxantrone, Daunorubicin, SN-38, and Topotecan, and frequently reduces the effectiveness of chemotherapy.

BCRP is a physiological component of the organism's self-defense system. It facilitates the removal of harmful substances and toxic xenobiotics from the body through the blood-brain, placental, and possibly blood-testis barriers, as well as in the gut and biliary tract.Numerous anticancer medications, including traditional chemotherapeutics and targeted small therapeutic molecules that are still relatively new in clinical use, are recognized and transported by BCRP. Therefore, BCRP expression in cancer cells directly contributes to MDR through active anticancer drug efflux. The expression of BCRP in cancer cells may be a manifestation of metabolic and signaling pathways that confer multiple mechanisms of drug resistance, self-renewal (stemness), and invasiveness (aggressiveness), and thereby impart a poor prognosis. BCRP is also known to be a stem cell marker. Therefore, inhibiting BCRP-mediated active efflux might be useful as a cancer treatment.

BCRP related products

Structure Cat No. Product Name CAS No. Product Description
3,7,2',4'-Tetramethoxy-5-hydroxyflavone V74161 3,7,2',4'-Tetramethoxy-5-hydroxyflavone 19056-75-8 BCRP/ABCG2-IN-1 is an inhibitor (blocker/antagonist) of breast cancer resistance protein (BCRP/ABCG2) with IC50 of 5.98 μM and can be used for multidrug resistance research in breast cancer.
5,7,3'-Trihydroxy-4'-Methoxy-8-prenylflavanone V74162 5,7,3'-Trihydroxy-4'-Methoxy-8-prenylflavanone 1268140-15-3 5,7,3'-Trihydroxy-4'-Methoxy-8-prenylflavanone (compound 1) is a flavonoid and a potent ABCG2 inhibitor (antagonist) with IC50 of 6.6 μM.
ABCG2-IN-1 V74157 ABCG2-IN-1 2559759-40-7 ABCG2-IN-1 (Compound K2), a Ko143 analogue, is an orally bioactive ABCG2 inhibitor (antagonist) with IC50 of 0.13 μM.
ABCG2-IN-2 V74160 ABCG2-IN-2 2559759-59-8 ABCG2-IN-2 is a potent ABCG2 inhibitor (antagonist) with good oral pharmacokinetics in mice.
Ac32Az19 V74159 Ac32Az19 2760674-72-2 Ac32Az19 is a potent, nontoxic, and selective BCRP inhibitor (antagonist) with EC50 of 13 nM in BCRP-overexpressing HEK293/R2 cells.
Efflux inhibitor-1 V74158 Efflux inhibitor-1 1776055-29-8 Efflux inhibitor-1 (compound 2) is a pyrazoline[1,5-a] pyrimidine efflux inhibitor.
KS176 V3037 KS176 1253452-78-6 KS176 is a novel potent and highly selective/specific inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter with IC50 values of 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays respectively.
RG 14620 V13718 RG 14620 136831-49-7 RG 14620 (RG-14620),a non-phenolic tyrphostin analog, is a novel and potent EGFR inhibitor (IC50 = 3 μM) with anticancer activity.
YHO-13177 V28371 YHO-13177 912287-56-0 YHO-13177 is a highly active breast cancer resistance protein multidrug transport channel (BCRP) inhibitor that can enhance the activity of SN-38 and has no effect on P-gp.
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