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

BCRP Inhibitor

BCRP Inhibitors (32):

Cat. No. Product Name Effect Purity
  • HY-10010
    Ko 143
    Inhibitor 99.97%
    Ko 143 is a potent and selective ATP-binding cassette subfamily G member 2 (ABCG2/BCRP) inhibitor. Ko 143 displays >200-fold selectivity over P-gp and MRP-1 transporters.
  • HY-50879
    Elacridar
    Inhibitor 99.94%
    Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on agent distribution to brain and the research of cancer.
  • HY-108347
    CP-100356 hydrochloride
    Inhibitor 99.68%
    CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC50=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC50>15 µM).
  • HY-N2143
    Fumitremorgin C
    Inhibitor 99.20%
    Fumitremorgin C is a potent and selective ABCG2/BRCP inhibitor.
  • HY-50880
    Elacridar hydrochloride
    Inhibitor 99.93%
    Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on agent distribution to brain and it can be used for the research of cancer.
  • HY-155653
    ABCG2-IN-2
    Inhibitor
    ABCG2-IN-2 is a potent ABCG2 inhibitor with favorable oral pharmacokinetic profiles in mice. ABCG2-IN-2 can be used for the research of tumor multidrug resistance (MDR) and erythropoietic protoporphyria (EPP).
  • HY-156092
    Antitumor photosensitizer-4
    Inhibitor
    Antitumor photosensitizer-4 (compound 10b) is a potent tyrosine kinase inhibitor (TKI) targeting ABCG2. Antitumor photosensitizer-4 is a photosensitizer (PS) consisting of a conjugate of dasatinib (HY-10181) and imatinib (HY-15463). Antitumor photosensitizer-4 induces apoptosis and ROS production and exhibits strong phototoxicity to HepG2 and B16-F10 cells.
  • HY-155652
    ABCG2-IN-1
    Inhibitor
    ABCG2-IN-1 (compound K2), a Ko143 analog, is an orally active ABCG2 inhibitor with an IC50 of 0.13 μM. ABCG2-IN-1 has favorable oral pharmacokinetic profiles in mice.
  • HY-12758A
    YHO-13351 free base
    Inhibitor 99.00%
    YHO-13351 free base is the prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
  • HY-12757
    YHO-13177
    Inhibitor 98.45%
    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-18010
    PCI 29732
    Inhibitor 99.86%
    PCI 29732 is a potent, orally active, reversible BTK inhibitor with Kiapp values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2.
  • HY-19753
    KS176
    Inhibitor 98.01%
    KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.
  • HY-106004
    Zamicastat
    Inhibitor ≥98.0%
    Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to 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. Zamicastat reduces high blood pressure.
  • HY-112505
    Efflux inhibitor-1
    Inhibitor ≥98.0%
    Efflux inhibitor-1 (compound 2) is a pyrazolo[1,5-a]pyrimidine efflux inhibitor. Efflux inhibitor-1 selectively targets toward ABCG2/BCRP over ABCB1 with IC50s of 0.45 μM and 2.17 μM, respectively.
  • HY-100390
    (S)-ML753286
    Inhibitor 99.25%
    (S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
  • HY-116494
    ML753286
    Inhibitor
    ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species.
  • HY-111678
    ML230
    Inhibitor 99.60%
    ML230 (CID44640177; SID 88095709) is a selective inhibitor of ATP-binding cassette (ABC) transporter ABCG2, and 36-fold selective for ABCG2 over ABCB1 with EC50s values of 0.13 μM and 4.65 μM, respectively.
  • HY-118144
    PD166326
    Inhibitor 99.99%
    PD166326 is a pyridopyrimidine-type inhibitor of receptor tyrosine kinases, with IC50s of 6 nM and 8 nM for Src and Abl, respectively. PD166326 exhibits antileukemic activity.
  • HY-12758
    YHO-13351
    Inhibitor
    YHO-13351 is the prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
  • HY-132934
    Ac32Az19
    Inhibitor 99.50%
    Ac32Az19 is a potent, nontoxic, and highly selective BCRP inhibitor with an EC50 value of 13 nM in the BCRP-overexpressed HEK293/R2 cells.