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-111678
    ML230
    		Inhibitor 99.65%
    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-B0777S
    Moxidectin-d3
    Moxidectin-d3 (CL-301423-d3) is deuterium labeled Moxidectin. 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-d<sub>3</sub>
  • HY-132934
    Ac32Az19
    		Inhibitor 98.12%
    Ac32Az19 is a potent, nontoxic, and highly selective BCRP inhibitor with an EC50 value of 13 nM in the BCRP-overexpressed HEK293/R2 cells.
    Ac32Az19
  • HY-100390
    (S)-ML753286
    		Inhibitor 99.39%
    (S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
    (S)-ML753286
  • HY-50879R
    Elacridar (Standard)
    		Inhibitor
    Elacridar (Standard) is the analytical standard of Elacridar. This product is intended for research and analytical applications. 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 (Standard)
  • 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-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-W777317
    Elacridar-d4(Major)
    Elacridar-d4(Major) is the deuterium labeled Elacridar (HY-50879). 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-d<sub>4</sub>(Major)
  • 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.
    FD 12-9
  • HY-136450S1
    Triclabendazole sulfoxide-13C,d3
    		Inhibitor
    Triclabendazole sulfoxide-13C,d3 is the 13C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer.
    Triclabendazole sulfoxide-<sup>13</sup>C,d<sub>3</sub>
  • HY-122416
    6,8-Diprenylnaringenin
    		Inhibitor
    6,8-Diprenylnaringenin (Lonchocarpol A; Senegalensin), a hop prenylflavonoid, is a inhibitor of breast cancer resistance protein (BCRP/ABCG2). 6,8-Diprenylnaringenin inhibits ABCG2-mediated efflux of Mitoxantrone, and 3H-Methotrexate transport (IC50=0.41 μM) in HEK293 cells. 6,8-Diprenylnaringenin exhibits some estrogenicity, but its potency is less than 1% of that of 8-Prenylnaringenin.
    6,8-Diprenylnaringenin
  • HY-101570G
    Nedisertib (GMP)
    Nedisertib (GMP) (Peposertib (GMP)) is Nedisertib (HY-101570) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Nedisertib is an orally active selective DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of less than 3 nM. Nedisertib also acts as a modulator of ABCG2, capable of reversing ABCG2-mediated multidrug resistance (MDR), thus providing new strategies for combination therapy. By inhibiting DNA double-strand break repair, Nedisertib can enhance the efficacy of chemotherapy and radiotherapy. Nedisertib exhibits antitumor activity.
    Nedisertib (GMP)
  • HY-136450S
    Triclabendazole sulfoxide-d3
    		Inhibitor
    Triclabendazole sulfoxide-d3 is the deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer.
    Triclabendazole sulfoxide-d<sub>3</sub>
  • HY-W007771R
    Acridone (Standard)
    		Inhibitor
    Acridone (Standard) is the analytical standard of Acridone. This product is intended for research and analytical applications. Acridone is an organic compound based on the acridine skeleton. Acridone has antibacterial, antimalarial, antiviral and anti neoplastic activities.
    Acridone (Standard)
  • HY-178100
    PARP1-IN-45
    PARP1-IN-45 (Compound 15) is a PARP1 inhibitor with an IC50 of 17  nM. PARP1-IN-45 effectively stimulates ATPase activity of ABCG2. PARP1-IN-45 can be used for cancers like ovarian cancer research.
    PARP1-IN-45
  • HY-155653
    ABCG2-IN-2
    		Inhibitor
    ABCG2-IN-2 is a potent ABCG2 inhibitor with favorable oral pharmacokinetic profiles in mice. ABCG2-IN-2 can be used for the research of tumor multidrug resistance (MDR) and erythropoietic protoporphyria (EPP).
    ABCG2-IN-2
  • HY-136940
    Ac22(Az8)2
    		Inhibitor
    Ac22(Az8)2​ is a selective BCRP inhibitor (EC50: 1-2 nM). Ac22(Az8)2 can restore the drug sensitivity of BCRP-overexpressing cells by inhibiting BCRP-ATPase activity, blocking drug efflux, and increasing intracellular drug accumulation. Ac22(Az8)2 can be used in the research of BCRP-mediated multidrug-resistant cancers.
    Ac22(Az8)2
  • HY-17648
    MBL-II-141
    		Inhibitor
    MBL-II-141 is potent ABCG2 inhibitor with an IC50 of 0.11 μM. MBL-II-141 inhibits the transport function of ABCG2 in a non-competitive manner, preventing ABCG2 from pumping substrates (such as Irinotecan (HY-16562)) out of the cells, thereby increasing the accumulation of drugs within the cells. MBL-II-141 has no effect on ABCB1 (P-gp) and ABCC1 (MRP1) and has extremely low cytotoxicity (IG50 > 100 μM). MBL-II-141 can be used for the study of multidrug resistance (MDR) cancers.
    MBL-II-141
  • HY-16278A
    Pradigastat sodium
    		Inhibitor
    Pradigastat sodium (LCQ 908 sodium) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC50 at 0.157 µM. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC50 of 5 µM, 1.66µM, 3.34µM and 0.973µM, respectively. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro.
    Pradigastat sodium
  • HY-156092
    Antitumor photosensitizer-4
    		Inhibitor
    Antitumor photosensitizer-4 (compound 10b) is a potent tyrosine kinase inhibitor (TKI) targeting ABCG2. Antitumor photosensitizer-4 is a photosensitizer (PS) consisting of a conjugate of dasatinib (HY-10181) and imatinib (HY-15463). Antitumor photosensitizer-4 induces apoptosis and ROS production and exhibits strong phototoxicity to HepG2 and B16-F10 cells.
    Antitumor photosensitizer-4
Cat. No. Product Name / Synonyms Application Reactivity