BCRP

Breast cancer resistance protein; ABCG2

BCRP

Related Products

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 Inhibitors (44)

BCRP Related Products (49)
Antibodies (2)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

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.

HY-136450

Triclabendazole sulfoxide	Inhibitor	98.78%
Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP.

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.

HY-132934

Ac32Az19	Inhibitor	99.50%
Ac32Az19 is a potent, nontoxic, and highly selective BCRP inhibitor with an EC₅₀ value of 13 nM in the BCRP-overexpressed HEK293/R2 cells.

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-136450S1

Triclabendazole sulfoxide-¹³C,d₃	Inhibitor
Triclabendazole sulfoxide-¹³C,d₃ is the ¹³C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP[1][2].

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.

HY-136450S

Triclabendazole sulfoxide-d₃	Inhibitor
Triclabendazole sulfoxide-d₃ is the deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP[1][2].

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).

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.

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.

HY-155652

ABCG2-IN-1	Inhibitor
ABCG2-IN-1 (compound K2), a Ko143 analog, is an orally active ABCG2 inhibitor with an IC₅₀ of 0.13 μM. ABCG2-IN-1 has favorable oral pharmacokinetic profiles in mice.

HY-129301

CCTA-1523	Inhibitor
CCTA-1523 is a potent, selective, reversible and orally active ABCG2 inhibitor. CCTA-1523 shows cytotoxicity. CCTA-1523 shows anticancer activity.

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.

HY-168041

LRRK2-IN-15	Inhibitor
LRRK2-IN-15 is an LRRK2 inhibitor. The IC₅₀ value for PBMC cells is 5 nM, and the IC₅₀ value for BCRP is 1.5 μM. LRRK2-IN-15 can be used for research on Parkinson's disease.

HY-146676

UR-MB108	Inhibitor
UR-MB108 (Compound 57) is a potent, selective ABCG2 (BCRP) inhibitor with an IC₅₀ of 79 nM. UR-MB108 is stable in blood plasma.

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.

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).

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.

HY-121645

2,4-Dibromoestradiol
2,4-Dibromoestradiol (NSC103054) is a compound that is involved in the function of ABCG2 transporter.

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BCRP

BCRP

BCRP Related Products (49)

Antibodies (2)

BCRP Related Products (49):