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BCRP(breast cancer resistant protein) is an ATP-binding cassette (ABC) transporter, which together with two other ABC efflux drug pumps, namely P-glycoprotein (P-gp, ABCB1) and multidrug resistance-related protein 1 (MRP1, ABCC1) is the most important multidrug resistance protein found in eukaryotic cells including cells in the testis.

Breast cancer resistance protein (BCRP/ABCG2) is known to localize at the blood-brain barrier (BBB) and can significantly restrict xenobiotic permeability in the brain. The objective of this study is to investigate the regulation of BCRP functional expression by peroxisome proliferator-activated receptor alpha (PPARα), a ligand-activated transcription factor primarily involved in lipid metabolism, in a cerebral microvascular endothelial cell culture system (hCMEC/D3), representative of human BBB.

Cat. No. Product Name CAS No. Information
H4290

YHO-13351 free base

 		912288-64-3

YHO-13351 is an orally available prodrug of YHO-13177, which can specifically reverse BCRP/ABCG2-mediated drug resistance in vitro and in vivo; YHO-13351 is rapidly converted into YHO-13177 after its oral or intravenous administration, significantly increases the survival time of mice inoculated with BCRP-transduced murine leukemia P388 cells and suppressed the tumor growth in an HCT116/BCRP xenograft model coadministration of irinotecan.
H4289

YHO-13351

 		1346753-00-1

YHO-13351 is an orally available prodrug of YHO-13177, which can specifically reverse BCRP/ABCG2-mediated drug resistance in vitro and in vivo; YHO-13351 is rapidly converted into YHO-13177 after its oral or intravenous administration, significantly increases the survival time of mice inoculated with BCRP-transduced murine leukemia P388 cells and suppressed the tumor growth in an HCT116/BCRP xenograft model coadministration of irinotecan.
H4288

YHO-13177

 		912287-56-0

YHO-13177 is a acrylonitrile derivative and active form of YHO-13351 that can specifically reverse BCRP/ABCG2-mediated drug resistance in vitro and in vivo; reverses BCRP-mediated acquired resistance to SN-38 in A549 cells without cytotoxicity, also shows no effect on P-glycoprotein-mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells and multidrug resistance-related protein 1-mediated doxorubicin resistance in MRP1-transfected human epidermoid cancer KB-3-1 cells.
H4287

KS-176

 		1253452-78-6

A potent and selective inhibitor of BCRP multidrug transporter with IC50 of 0.59 and 1.39 uM in Pheo A and Hoechst 33342 assays, respectively; displays no inhibitory activity against P-gp or MRP1.
H4286

Ko-143

 		461054-93-3

A nontoxic analog of fungal toxin fumitremorgin C and potent, orally bioavailable inhibitor of BCRP (ABCG2) with EC90 of 26 nM; shows low activity against P-gp, MRP1 and other known drug transporter; has an effect on the transport activity of both ABCB1 and ABCC1 at >1 uM; reverses Bcrp-mediated drug resistance and markedly increases the oral availability of topotecan in mice.
H4285

Brevianamide F

 		38136-70-8

A naturally occurring 2,5-diketopiperazine that possess interesting breast cancer resistance protein (BCRP) inhibitory activity.; also shows agonism towards Ca(2+)-channel activity at 100 uM, and has potentiation for use in the treatment of cardiovascular dysfunction.

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