BCRP

Elacridar (GG918) (GF120918) is an effective BCRP and P-gp (MDR-1) inhibitor.

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.

YHO-13351 free base is a water-soluble prodrug of YHO-13177, an inhibitor of BCRP.

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

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

CP-100356 hydrochloride is an orally active and low micromolar dual inhibitor of MDR1 (P-gp) and BCRP, a nucleotide-derived substrate analogue with inhibitory effects on MDR1-mediated Calcein-AM transporter and BCRP-mediated Prazosin transporter.CP-100356 Inhibits OATP1B1, 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.

Brevianamide F (Cyclo(L-Pro-L-Trp)), also known as cyclo-(L-Trp-L-Pro), belongs to a class of naturally occurring 2,5-diketopiperazines. Brevianamide F possess interesting breast cancer resistance protein inhibitory activity.

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

YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.

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

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

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

ABCG2-IN-1 (compound K2), an analog of Ko143, constitutes an orally active inhibitor targeting ABCG2 with an inhibitory concentration (IC50) of 0.13 μM. Demonstrating favorable oral pharmacokinetics in mice, ABCG2-IN-1 showcases promise for further research [1].

Triclabendazole sulfoxide (TCBZ-SO) is a main plasma metabolite of Triclabendazole. Triclabendazole sulfoxide inhibits membrane transporter ABCG2/BCRP and exhibits anti-parasite effects.