1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
  3. BCRP

BCRP

Breast cancer resistance protein (BCRP/ABCG2/MXR/ABCP) is an ATP-dependent efflux transporter, which belongs to the large ATP-binding cassette (ABC) transporter family present on cell membranes, and it is classified into the G subfamily of these transporters. BCRP is expressed in a variety of normal cells and acts as a xenobiotic efflux transporter. BCRP is often associated with cancer chemotherapeutic resistance. BCRP confers multidrug resistance (MDR) to a series of antitumor agents such as Mitoxantrone, Daunorubicin, SN-38, and Topotecan, and often limits the efficacy of chemotherapy.

BCRP physiologically functions as a part of a self-defense mechanism for the organism. It enhances elimination of toxic xenobiotic substances and harmful agents in the gut and biliary tract, as well as through the blood-brain, placental, and possibly blood-testis barriers. BCRP recognizes and transports numerous anticancer drugs including conventional chemotherapeutic and targeted small therapeutic molecules relatively new in clinical use. Thus, BCRP expression in cancer cells directly causes MDR by active efflux of anticancer drugs. Because BCRP is also known to be a stem cell marker, its expression in cancer cells could 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. Therefore, blocking BCRP-mediated active efflux may provide a therapeutic benefit for cancers.

BCRP Related Products (15):

Cat. No. Product Name Effect Purity
  • HY-10010
    Ko 143
    Inhibitor 99.83%
    Ko 143 is a potent and selective ATP-binding cassette subfamily G member 2 (ABCG2/BCRP) inhibitor. Ko 143 displays >200-fold selectivity over P-gp and MRP-1 transporters.
  • HY-50879
    Elacridar
    Inhibitor ≥98.0%
    Elacridar (GF120918) is a potent P-glycoprotein (Pgp) and BCRP inhibitor.
  • HY-N2143
    Fumitremorgin C
    Inhibitor 98.26%
    Fumitremorgin C is a potent and selective ABCG2/BRCP inhibitor.
  • HY-106004
    Zamicastat
    Inhibitor ≥98.0%
    Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8 μM and 17.0 μM, respectively. Zamicastat reduces high blood pressure.
  • HY-18010
    PCI 29732
    Inhibitor 99.68%
    PCI 29732 is a potent, orally active, reversible BTK inhibitor with Kiapp values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2.
  • HY-19753
    KS176
    Inhibitor 98.01%
    KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays respectively). Displays no inhibitory activity against P-gp or MRP1.
  • HY-108347
    CP-100356 hydrochloride
    Inhibitor ≥98.0%
    CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC50=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC50>15 µM).
  • HY-100390
    (S)-ML753286
    Inhibitor 98.90%
    (S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
  • HY-12758A
    YHO-13351 free base
    Inhibitor 98.10%
    YHO-13351 free base is the prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
  • HY-12757
    YHO-13177
    Inhibitor 98.40%
    YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.
  • HY-111678
    ML230
    Inhibitor ≥98.0%
    ML230 (CID44640177; SID 88095709) is a selective inhibitor of ATP-binding cassette (ABC) transporter ABCG2, and 36-fold selective for ABCG2 over ABCB1 with EC50s values of 0.13 μM and 4.65 μM, respectively.
  • HY-116494
    ML753286
    Inhibitor 99.79%
    ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species.
  • HY-12758
    YHO-13351
    Inhibitor
    YHO-13351 is the prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
  • HY-128685
    FD 12-9
    Inhibitor
    FD 12-9 is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively. Anti-glioblastoma activity.
  • HY-136450
    Triclabendazole sulfoxide
    Inhibitor
    Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP.
Isoform Specific Products

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