bcrp

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].

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

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.

CH-0793076, a hexacyclic camptothecin analog, is an active drug and major metabolite of TP300. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein). CH-0793076 inhibits DNA topoisomerase I (IC50: 2.3 μM).

CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC 50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein) [1] .

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.

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

PF-06273340 is an effective, Selective, and Peripherally Restricted Pan-Trk inhibitor (IC50: Trk-A = 6 nM; Trk-B = 4 nM; Trk-C = 3 nM). PF-06273340 has low metabolic turnover in HLM and hHep is a good substrate for efflux transporters P-gp (ER = 35.7) and BCRP (ER = 4.0) and has moderate passive permeability (RRCK Papp = 5.4 × 10 6 cm s 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.

YHO-13351 is the water-soluble prodrug of YHO-13177, which is a potent and specific BCRP inhibitor.

UR-MB108 is a potent and selective inhibitor of ABCG2 (BCRP), displaying an IC50 value of 79 nM, and exhibits stability in blood plasma.

Ac32Az19 is a potent, non-toxic, and highly selective inhibitor of Breast Cancer Resistance Protein (BCRP), demonstrating an EC50 of 13 nM in BCRP-overexpressed HEK293/R2 cells.

Atiratecan (TP300) is a prodrug of camptothecin analog CH0793076. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models[1]. Atiratecan does not inhibit acetylch

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.

MC-70 hydrochloride is a potent P-gp inhibitor with good selectivity towards BCRP pump (EC50 values 0.05 μM, 0.69 μM, 9.3 μM, and 73 μM for Caco-2, MDR1, MRP1, and BCRP inhibition, respectively).

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.

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

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.

5,7-DIMETHOXYFLAVONE possessed remarkable leishmanicidal potential.

Cefditoren sodium is a cephalosporin antibiotic potentially for the treatment of bacterial infection. The expression levels of Mrp2, Bcrp, Oat2 mRNA were markedly increased, while P-gp and Oct1 mRNA were decreased. In concordance with RT-PCR results, Mrp2

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).

Cefditoren-d3 is a deuterated compound of Cefditoren. Cefditoren has a CAS number of 104146-53-4. Cefditoren sodium is a cephalosporin antibiotic potentially for the treatment of bacterial infection. The expression levels of Mrp2, Bcrp, Oat2 mRNA were markedly increased, while P-gp and Oct1 mRNA were decreased. In concordance with RT-PCR results, Mrp2 expression level increased by Western blotting.

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

Efflux inhibitor-1 is a pyrazolopyrimidine efflux inhibitor. Efflux inhibitor-1 selectively targets toward ABCG2/BCRP over ABCB1 with IC 50 s of 0.45 μM and 2.17 μM, respectively .

'(6R)-ML753286, an isomer of ML753286, is an orally active, selective Breast Cancer Resistance Protein (BCRP) inhibitor, demonstrating an IC50 of 0.6 μM. It exhibits high permeability and low to medium clearance in rodent and human liver S9 fractions, with cross-species plasma stability [1].'

Ceefourin 1 is a highly selective multidrug resistance protein 4 (MRP4) inhibitor.

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

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