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

BCRP

Breast cancer resistance protein; ABCG2

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-10010
    Ko 143
    Inhibitor 99.97%
    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.
    Ko 143
  • HY-50879
    Elacridar
    Inhibitor 99.94%
    Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on agent distribution to brain and the research of cancer.
    Elacridar
  • HY-108347
    CP-100356 hydrochloride
    Inhibitor 99.68%
    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).
    CP-100356 hydrochloride
  • HY-N2143
    Fumitremorgin C
    Inhibitor 99.20%
    Fumitremorgin C is a potent and selective ABCG2/BRCP inhibitor.
    Fumitremorgin C
  • HY-50880
    Elacridar hydrochloride
    Inhibitor 99.93%
    Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on agent distribution to brain and it can be used for the research of cancer.
    Elacridar hydrochloride
  • HY-B0777R
    Moxidectin (Standard)
    Moxidectin (Standard) is the analytical standard of Moxidectin. This product is intended for research and analytical applications. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk.
    Moxidectin (Standard)
  • HY-157876
    Anticancer agent 191
    Inhibitor
    Anticancer agent 191 (Compound 2) is a derivative of probenecid (HY-B0545). As a cancer cell efflux inhibitor, Anticancer agent 191 is designed to inhibit P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and/or multiple multidrug resistance proteins (MRPs). Anticancer agent 191 increases the accumulation of vinblastine in cancer cells, which is used for cancer research.
    Anticancer agent 191
  • HY-119724
    ABCG2-IN-3
    Inhibitor
    ABCG2-IN-3 (Compound 52) is a selective inhibitor for breast cancer resistance protein (ABCG2), with an IC50 of 0.238 µM. ABCG2-IN-3 reverses the ABCG2-mediated resistance toward SN-38 and inhibit the ATPase activity.
    ABCG2-IN-3
  • HY-B0777
    Moxidectin
    98.03%
    Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk.
    Moxidectin
  • HY-12758A
    YHO-13351 free base
    Inhibitor 99.00%
    YHO-13351 free base is the prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
    YHO-13351 free base
  • HY-12757
    YHO-13177
    Inhibitor 98.45%
    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.
    YHO-13177
  • HY-18010
    PCI 29732
    Inhibitor 99.86%
    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.
    PCI 29732
  • HY-19753
    KS176
    Inhibitor 99.09%
    KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.
    KS176
  • 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.
    Zamicastat
  • HY-112505
    Efflux inhibitor-1
    Inhibitor ≥98.0%
    Efflux inhibitor-1 (compound 2) is a pyrazolo[1,5-a]pyrimidine efflux inhibitor. Efflux inhibitor-1 selectively targets toward ABCG2/BCRP over ABCB1 with IC50s of 0.45 μM and 2.17 μM, respectively.
    Efflux inhibitor-1
  • HY-100390
    (S)-ML753286
    Inhibitor 99.25%
    (S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
    (S)-ML753286
  • HY-116494
    ML753286
    Inhibitor
    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.
    ML753286
  • HY-118144
    PD166326
    Inhibitor 99.99%
    PD166326 is a pyridopyrimidine-type inhibitor of receptor tyrosine kinases, with IC50s of 6 nM and 8 nM for Src and Abl, respectively. PD166326 exhibits antileukemic activity.
    PD166326
  • HY-111678
    ML230
    Inhibitor 99.60%
    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.
    ML230
  • HY-12758
    YHO-13351
    Inhibitor
    YHO-13351 is the prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
    YHO-13351
Cat. No. Product Name / Synonyms Application Reactivity