BCRP

Elacridar (GG918) is a potent inhibitor of P-glycoprotein and BCRP.

Zamicastat (BIA 5-1058) is an inhibitor of dopamine β-hydroxylase (DBH) and a concentration-dependent dual inhibitor of P-gp and BCRP, with IC50 values of 73.8 μM and 17.0 μM, respectively.

Fumitremorgin C (12α-Fumitremorgin C) is a mycotoxin and inhibits ABCG2 BRCP.

BCRP-IN-2 is a compound with BCRP inhibitory activity, exhibiting enhanced inhibition of BCRP upon UV activation. It serves as a valuable probe for studying interactions between quinazoline amine derivatives and BCRP, and it stimulates ATP hydrolysis of the BCRP transporter, leading to increased mitoxantrone accumulation in BCRP-overexpressing H460 MX20 cells.

Triclabendazole sulfoxide (TCBZ-SO), a primary plasma metabolite of Triclabendazole, inhibits the membrane transporter ABCG2/BCRP and demonstrates anti-parasite effects.

6,8-Diprenylnaringenin (Senegalensin) is a natural product from hop Humulus lupulus. 6,8-Diprenylnaringenin is a breast cancer resistance protein(BCRP) inhibitor with some estrogenicity.

Ko 143 is a selective inhibitor of ATP-binding cassette sub-family G member 2 (ABCG2; BCRP).

GS-9191 PM is a novel antitumorviral compound, a bis-amide prodrug of the nucleotide analog 9-(2-phosphonomethoxyethyl)-N6-cyclopropyl-2,6-diaminopurine (cPrPMEDAP).GS-9191 PM is a potent inhibitor of MDR1 and BCRP.GS-9191 PM exhibits both antiproliferative and antitumorviral activities.

P-gp BCRP-IN-1 (compound 19) is a relatively safe, orally active, and efficient inhibitor of the efflux transporters P-gp and BCRP, which reverses resistance and enhances the oral bioavailability of Paclitaxel (PTX) [1].

P-gp BCRP-IN-2 (compound 15), an oxadiazole derivative, functions as a dual inhibitor targeting both the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). Additionally, it bolsters the anti-proliferative impact of Doxorubicin in the drug-resistant HT29 DX and MDCK-MDR1 human adenocarcinoma colon cancer cell lines [1].

33-BCRP inhibitor is a compound that blocks the action of breast cancer resistance protein (BCRP), enhancing the susceptibility of mitoxantrone-resistant H460/MX20 lung cancer cells to the cytotoxic effects of mitoxantrone, both individually and when combined with UV radiation. Additionally, it enhances the sensitivity of KB-C2 epidermal carcinoma cells, which overexpress P-glycoprotein (P-gp) or multidrug resistance protein (MDR), to colchicine-induced apoptosis. Furthermore, at a concentration of 5 µM, it boosts the intracellular accumulation of mitoxantrone in H460/MX20 cells.

Butein tetramethyl ether (Compound 20) is a potent and selective inhibitor of breast cancer resistance protein ATP-binding cassette sub-family G member 2 (BCRP ABCG2). It inhibits MCF-7 MX and MDCKBCRP cells with IC50 values of 2.2 μM and 1.03 μM, respectively. Butein tetramethyl ether holds potential for cancer research.

ABCG2-IN-4 (Compound K31) is an orally active ABCG2 inhibitor that reduces the release of Protoporphyrin IX (PPIX) from red blood cells into the plasma and prevents phototoxicity. In mouse models, ABCG2-IN-4 also demonstrates anti-inflammatory and antioxidant properties.

ABCG2-IN-1 (compound K2), an analog of Ko143, is an orally active inhibitor of ABCG2 with an IC50 of 0.13 μM, demonstrating favorable oral pharmacokinetics in mice and showing promise for further research [1].

ABCG2-IN-2 is a potent inhibitor of ABCG2, showing favorable oral pharmacokinetic profiles in mice, and is applicable for investigating tumor multidrug resistance (MDR) and erythropoietic protoporphyria (EPP) [1].

YHO-13351 free base, the water-soluble prodrug of YHO-13177, is an inhibitor of BCRP (breast cancer resistance protein).

CCTA-1523 is an efflux function of ABCG2 inhibitor. CCTA-1523 selectively reverses ABCG2-mediated MDR in cancer cells.

Moxidectin (CL301423) is an anthelmintic drug which kills parasitic worms, and is used for the prevention and control of heartworm and intestinal worms. It can be found in treatments prescribed for animals such as dogs, cats, horses, cattle and sheep. Application methods for moxidectin vary by treatment, and include oral, topical, and injectable solutions. Cydectin Pour On is a trade name for a formulation for use on cattle and red deer.

(S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on the BCRP efflux transporter.

FD 12-9, Anti-glioblastoma activity. is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively.

ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions. ML753286 is an orally active and selective inhibitor of BCRP (IC50: 0.6 μM). It is also stable in plasma across species.

LRRK2-IN-15 is an inhibitor of LRRK2. It exhibits an IC50 value of 5 nM in PBMC cells and 1.5 μM for BCRP. This compound is utilized in the research of Parkinson's disease.

MZ82, a derivative of Ko 143, is a potent inhibitor of ATP-binding cassette sub-family G member 2 (ABCG2 BCRP), with an IC50 of approximately 23 nM. Compared to Ko 143, MZ82 exhibits significantly enhanced metabolic stability in liver microsomes and shows marked improvement in mice, along with the ability to penetrate the brain.

CP-100356 hydrochloride is an orally active, low micromolar dual inhibitor of MDR1 (P-gp) and BCRP, a nucleotide-derived substrate analogue that inhibits MDR1-mediated Calcein-AM and BCRP-mediated Prazosin transporters. Additionally, CP-100356 inhibits OATP1B1 and induces stomatal opening in the dark.