1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
  3. BCRP

BCRP

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.

BCRP Related Products (10):

Cat. No. Product Name Effect Purity
  • HY-10010
    Ko 143 Inhibitor 99.79%
    Ko 143 is a potent and selective ATP-binding cassette sub-family G member 2 (ABCG2) inhibitor.
  • HY-50879
    Elacridar Inhibitor 98.47%
    Elacridar is a potent P-glycoprotein (Pgp) and BCRP inhibitor.
  • HY-N2143
    Fumitremorgin C Inhibitor 99.63%
    Fumitremorgin C is a potent and selective ABCG2/BRCP inhibitor.
  • HY-12758
    YHO-13351 Inhibitor
    YHO-13351 is the water-soluble prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
  • HY-19753
    KS176 Inhibitor 99.21%
    KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays respectively). Displays no inhibitory activity against P-gp or MRP1.
  • HY-128685
    FD 12-9 Inhibitor
    FD 12-9 is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively. Anti-glioblastoma activity.
  • HY-106004
    Zamicastat Inhibitor 99.95%
    Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor that could cross the blood-brain barrier (BBB) and cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8 μM and 17.0 μM, respectively. Reduces high blood pressure.
  • HY-12757
    YHO-13177 Inhibitor 98.72%
    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.
  • HY-12758A
    YHO-13351 free base Inhibitor 98.10%
    YHO-13351 (free base) is the water-soluble prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
  • HY-100390
    BCRP-IN-1 Inhibitor 98.13%
    BCRP-IN-1 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
Isoform Specific Products

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