BCRP

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

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

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.

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.

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

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

Brevianamide F (Cyclo(L-Pro-L-Trp)), also known as cyclo-(L-Trp-L-Pro), is a naturally occurring 2,5-diketopiperazine with notable breast cancer resistance protein inhibitory activity.

YHO-13177 is a potent and specific inhibitor of BCRP, which enhances the cytotoxicity of SN-38 in cancer cells without affecting P-glycoprotein–mediated paclitaxel resistance in [MDR1]-transduced human leukemia [K562] cells.

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

YHO-13351 is an ABCG2 inhibitor, an acrylonitrile derivative, that induces sensitization of cancer stem initiating-like side population cells to irinotecan.GSK1702934A can be used to study diabetes.

PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.

KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter, exhibiting no inhibitory activity against P-gp or MRP1.

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.

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.

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.

5,7,3'-Trihydroxy-4'-methoxy-8-prenylflavanone, a flavonoid, is found in the bark of *Azadirachta indica*.

5-Hydroxy-2′,3,4′,7-tetramethoxyflavone shows weak ABCG2 inhibitory potency with IC50s of 3.27 and 3.89 µM in the Hoechst 33342 and pheophorbide A assays.

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

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-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].

Vedroprevir, also known as GS9451, is a selective hepatitis C virus (HCV) NS3 protease inhibitor in the development of the treatment of genotype 1 (GT1) HCV infection.

CAY10719 is a selective inhibitor of the breast cancer resistance protein ABCG2 (IC50 = 0.23 μM) with little activity at ABCG1. It has been shown to reverse the ABCG2-mediated resistance toward SN 38 and to inhibit ATPase activity.

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.

INCB-056868 is the metabolite M11 of Epacadostat. It serves as a substrate for BCRP and holds potential for use in the study of metabolic diseases.