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).

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.

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.

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

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.

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

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.

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.

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.

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

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].

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.

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.

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.

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].

AZ99 (compound 7) serves as an effective inhibitor of ABCG2. It impedes the transport of estrone-3-sulfate (E1S) to proteoliposomes and inhibits ABCG2 ATPase activity mediated by ABCG2.