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

BCRP

Breast cancer resistance protein; ABCG2

BCRP

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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-116494A
    (6R)-ML753286
    		Inhibitor ≥98.0%
    (6R)-ML753286 is an isomer of ML753286 (HY-116494). 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.
    (6R)-ML753286
  • HY-155152
    P-gp/BCRP-IN-2
    		Inhibitor
    P-gp/BCRP-IN-2 (compound 15) is an oxadiazole derivative and a dual inhibitor of the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). P-gp/BCRP-IN-2 also enhances the anti-proliferative effects of Doxorubicin (HY-15142A) in drug-resistant human adenocarcinoma colon cancer cell lines HT29/DX and MDCK-MDR1 cells.
    P-gp/BCRP-IN-2
  • HY-144393
    P-gp/BCRP-IN-1
    		Inhibitor
    P-gp/BCRP-IN-1 (compound 19) is a potential, relatively safe, orally active and efficient efflux transporter (P-gp and BCRP) inhibitor. P-gp/BCRP-IN-1 exerts resistance reversal by inhibiting the efflux function of P-gp and BCRP. P-gp/BCRP-IN-1 can overcome the resistance and improve the oral bioavailability of PTX (Paclitaxel).
    P-gp/BCRP-IN-1
  • 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-121645
    2,4-Dibromoestradiol
    2,4-Dibromoestradiol (NSC103054) is a compound that is involved in the function of ABCG2 transporter.
    2,4-Dibromoestradiol
  • HY-172233
    INCB-056868
    		Substrate
    INCB-056868 is the metabolite M11 of Epacadostat (HY-15689). INCB-056868 can also serve as a substrate for BCRP. INCB-056868 is promising for research of metabolic diseases.
    INCB-056868
  • HY-136450R
    Triclabendazole sulfoxide (Standard)
    		Inhibitor
    Triclabendazole sulfoxide (Standard) is the analytical standard of Triclabendazole sulfoxide. This product is intended for research and analytical applications. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP.
    Triclabendazole sulfoxide (Standard)
  • HY-169860
    BCRP-IN-2
    		Inhibitor
    BCRP-IN-2 has BCRP inhibitory activity and shows even greater inhibition of BCRP after activation by ultraviolet light. BCRP-IN-2 can be a valuable probe for studying the interactions of quinazolinamine derivatives with BCRP, as it stimulates ATP hydrolysis of the BCRP transport protein, increasing the accumulation of mitoxantrone (HY-13502) in H460/MX20 cells with BCRP overexpression.
    BCRP-IN-2
  • HY-W740060
    Dipyridamole Mono-O-β-D-glucuronide
    		Inhibitor
    Dipyridamole Mono-O-β-D-glucuronide (compound M4) is a derivative of the phosphodiesterase (PDE) and BCRP inhibitor Dipyridamole (HY-B0312) and is an O-glucuronide.
    Dipyridamole Mono-O-β-D-glucuronide
  • HY-149469
    3,7,2',4'-Tetramethoxy-5-hydroxyflavone
    		Inhibitor
    BCRP/ABCG2-IN-1 is the inhibitor of breast cancer resistance protein (BCRP/ABCG2), with IC50 of 5.98 μM, that can be used in multidrug resistance of breast cancer.
    3,7,2',4'-Tetramethoxy-5-hydroxyflavone
  • HY-168572
    MZ82
    		Inhibitor
    MZ82, Ko 143 (HY-10010) derivative, is a ATP-binding cassette subfamily G member 2 (ABCG2/BCRP) inhibitor with the IC50 of ~23 nM. MZ82 not only shows greatly improved metabolic stability over Ko 143 (HY-10010) in liver microsomes but also in mice, and is able to penetrate into the brain.
    MZ82
  • 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-123526
    NSC265473
    NSC 265473 is an ABCG2 substrate.
    NSC265473
  • HY-N2651
    5,7,3'-Trihydroxy-4'-Methoxy-8-prenylflavanone
    		Inhibitor
    5,7,3'-Trihydroxy-4'-Methoxy-8-prenylflavanone (compound 1), a flavonoid, is a potent ABCG2 inhibitor with an IC50 of 6.6 μM.
    5,7,3'-Trihydroxy-4'-Methoxy-8-prenylflavanone
  • HY-16773
    Vedroprevir
    		Inhibitor
    Vedroprevir (GS-9451) is an inhibitor for HCV NS3/4A protease with an IC50 of 3.2 nM. Vedroprevir is also an inhibitor for breast cancer resistant protein (BCRP) with an IC50 of 1.4 μM. Vedroprevir inhibits P-gp, MRP1 and MRP2 with IC50 of 34, 14.9 and 12 μM, respectively. Vedroprevir exhibits good pharmacokinetic characteristics in rats and dogs.
    Vedroprevir
  • HY-129037
    BCRP-IN-1
    		Inhibitor
    BCRP-IN-1 (compound 48) is a potent inhibitor of breast cancer resistance protein (BCRP), with IC50s of 2.92 μM and 2.46 μM in Hoechst 33342 assay and Pheophorbide A assay, respectively.
    BCRP-IN-1
Cat. No. Product Name / Synonyms Application Reactivity