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.


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Ko 143

Ko 143 is a potent and selective ATP-binding cassette sub-family G member 2 (ABCG2) inhibitor.

  • CAS Number: 461054-93-3
  • MF: C26H35N3O5
  • MW: 469.573
  • Catalog: BCRP
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 689.8±55.0 °C at 760 mmHg
  • Melting Point: 147ºC
  • Flash Point: 371.0±31.5 °C

(S)-ML753286

BCRP-IN-1 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.

  • CAS Number: 1699720-85-8
  • MF: C20H25N3O3
  • MW: 355.43
  • Catalog: BCRP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ABCG2-IN-2

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)[1].

  • CAS Number: 2559759-59-8
  • MF: C25H34N4O4
  • MW: 454.56
  • Catalog: BCRP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Triclabendazole sulfoxide

Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP[1][2].

  • CAS Number: 100648-13-3
  • MF: C14H9Cl3N2O2S
  • MW: 375.65700
  • Catalog: BCRP
  • Density: 1.69
  • Boiling Point: 547.6ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 285ºC

FD 12-9

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[1].

  • CAS Number: 1451741-22-2
  • MF: C51H47N3O11
  • MW: 877.93
  • Catalog: BCRP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

elacridar

Elacridar is a potent P-glycoprotein (Pgp) and BCRP inhibitor.

  • CAS Number: 143664-11-3
  • MF: C34H33N3O5
  • MW: 563.643
  • Catalog: BCRP
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 701.6±60.0 °C at 760 mmHg
  • Melting Point: 216-218℃
  • Flash Point: 378.1±32.9 °C

ABCG2-IN-1

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[1].

  • CAS Number: 2559759-40-7
  • MF: C26H36N4O4
  • MW: 468.59
  • Catalog: BCRP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

YHO-13351 free base

YHO-13351 (free base) is the water-soluble prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.IC50 value:Target: BCRP inhibitorin vitro: YHO-13177 potentiates the cytotoxicity of SN-38, mitoxantrone, and topotecan in both BCRP-transduced human colon cancer HCT116 (HCT116/BCRP) cells and SN-38-resistant human lung cancer A549 (A549/SN4) cells that express BCRP, but had little effect in the parental cells. In addition, YHO-13177 potentiates the cytotoxicity of SN-38 in human lung cancer NCI-H460 and NCI-H23, myeloma RPMI-8226, and pancreatic cancer AsPC-1 cells that intrinsically expressed BCRP. YHO-13177 increases the intracellular accumulation of Hoechst 33342, a substrate of BCRP, at 30 minutes and partially suppresses the expression of BCRP protein at more than 24 hours after its treatment in both HCT116/BCRP and A549/SN4 cells [1].in vivo: In mice, YHO-13351 is rapidly converted into YHO-13177 after its oral or intravenous administration. Coadministration of irinotecan with YHO-13351 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, whereas irinotecan alone has little effect in these tumor models [1].

  • CAS Number: 912288-64-3
  • MF: C26H33N3O4S
  • MW: 483.623
  • Catalog: BCRP
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 627.1±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 333.1±31.5 °C

CP-100356 hydrochloride

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)[1].

  • CAS Number: 142715-48-8
  • MF: C31H37ClN4O6
  • MW: 597.10200
  • Catalog: BCRP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ML753286

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[1].

  • CAS Number: 1699720-89-2
  • MF: C20H25N3O3
  • MW: 355.43
  • Catalog: BCRP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

UR-MB108

UR-MB108 (Compound 57) is a potent, selective ABCG2 (BCRP) inhibitor with an IC50 of 79 nM. UR-MB108 is stable in blood plasma[1].

  • CAS Number: 2412461-98-2
  • MF: C40H38N6O4
  • MW: 666.77
  • Catalog: BCRP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CCTA-1523

CCTA-1523 is a potent, selective, reversible and orally active ABCG2 inhibitor. CCTA-1523 shows cytotoxicity. CCTA-1523 shows anticancer activity[1].

  • CAS Number: 1616271-41-0
  • MF: C16H15Cl2NO3
  • MW: 340.20
  • Catalog: BCRP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Efflux inhibitor-1

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[1].

  • CAS Number: 1776055-29-8
  • MF: C28H25N5O3
  • MW: 479.53
  • Catalog: BCRP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fumitremorgin C

Fumitremorgin C is a potent and selective ABCG2/BRCP inhibitor.

  • CAS Number: 118974-02-0
  • MF: C22H25N3O3
  • MW: 379.452
  • Catalog: BCRP
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 642.9±55.0 °C at 760 mmHg
  • Melting Point: 259.5-260.5℃
  • Flash Point: 342.6±31.5 °C

3,7,2',4'-Tetramethoxy-5-hydroxyflavone

BCRP/ABCG2-IN-1 is the inhibitor of breast cancer resistance protein (BCRP/ABCG2), with IC50 of 5.98 μM, that can be used in multidrug resistance of breast cancer[1].

  • CAS Number: 19056-75-8
  • MF: C19H18O7
  • MW: 358.34200
  • Catalog: BCRP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5,7,3'-Trihydroxy-4'-methoxy-8-prenylflavanone

5,7,3'-Trihydroxy-4'-Methoxy-8-prenylflavanone (compound 1), a flavonoid, is a potent ABCG2 inhibitor with an IC50 of 6.6 μM[1].

  • CAS Number: 1268140-15-3
  • MF: C21H22O6
  • MW: 370.396
  • Catalog: BCRP
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 616.0±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 219.1±25.0 °C

YHO-13177

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.IC50 value:Target: BCRP inhibitorin vitro: YHO-13177 potentiated the cytotoxicity of SN-38, mitoxantrone, and topotecan in both BCRP-transduced human colon cancer HCT116 (HCT116/BCRP) cells and SN-38–resistant human lung cancer A549 (A549/SN4) cells that express BCRP, but had little effect in the parental cells. In addition, YHO-13177 potentiated the cytotoxicity of SN-38 in human lung cancer NCI-H460 and NCI-H23, myeloma RPMI-8226, and pancreatic cancer AsPC-1 cells that intrinsically expressed BCRP. In contrast, it had 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. YHO-13177 increased the intracellular accumulation of Hoechst 33342, a substrate of BCRP, at 30 minutes and partially suppressed the expression of BCRP protein at more than 24 hours after its treatment in both HCT116/BCRP and A549/SN4 cells [1].in vivo: In mice, YHO-13351 was rapidly converted into YHO-13177 after its oral or intravenous administration. Coadministration of irinotecan with YHO-13351 significantly increased the survival time of mice inoculated with BCRP-transduced murine leukemia P388 cells and suppressed the tumor growth in an HCT116/BCRP xenograft model, whereas irinotecan alone had little effect in these tumor models [1].

  • CAS Number: 912287-56-0
  • MF: C20H22N2O3S
  • MW: 370.46500
  • Catalog: BCRP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

6,8-diprenylnaringenin

6,8-Diprenylnaringenin (Lonchocarpol A; Senegalensin), a hop prenylflavonoid, is a inhibitor of breast cancer resistance protein (BCRP/ABCG2). 6,8-Diprenylnaringenin inhibits ABCG2-mediated efflux of Mitoxantrone, and 3H-Methotrexate transport (IC50=0.41 μM) in HEK293 cells. 6,8-Diprenylnaringenin exhibits some estrogenicity, but its potency is less than 1% of that of 8-Prenylnaringenin[1][2].

  • CAS Number: 68236-11-3
  • MF: C25H28O5
  • MW: 408.48700
  • Catalog: BCRP
  • Density: 1.22g/cm3
  • Boiling Point: 639.245°C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 218.297°C

Zamicastat

Zamicastat is a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8±7.2 μM and 17.0±2.7 μM, respectively.

  • CAS Number: 1080028-80-3
  • MF: C21H21F2N3OS
  • MW: 401.47300
  • Catalog: BCRP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

YHO-13351

YHO-13351 is the water-soluble prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.IC50 value:Target: BCRP inhibitorin vitro: YHO-13177 potentiated the cytotoxicity of SN-38, mitoxantrone, and topotecan in both BCRP-transduced human colon cancer HCT116 (HCT116/BCRP) cells and SN-38–resistant human lung cancer A549 (A549/SN4) cells that express BCRP, but had little effect in the parental cells. In addition, YHO-13177 potentiated the cytotoxicity of SN-38 in human lung cancer NCI-H460 and NCI-H23, myeloma RPMI-8226, and pancreatic cancer AsPC-1 cells that intrinsically expressed BCRP. In contrast, it had 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. YHO-13177 increased the intracellular accumulation of Hoechst 33342, a substrate of BCRP, at 30 minutes and partially suppressed the expression of BCRP protein at more than 24 hours after its treatment in both HCT116/BCRP and A549/SN4 cells [1].in vivo: In mice, YHO-13351 was rapidly converted into YHO-13177 after its oral or intravenous administration. Coadministration of irinotecan with YHO-13351 significantly increased the survival time of mice inoculated with BCRP-transduced murine leukemia P388 cells and suppressed the tumor growth in an HCT116/BCRP xenograft model, whereas irinotecan alone had little effect in these tumor models [1].

  • CAS Number: 1346753-00-1
  • MF: C27H37N3O7S2
  • MW: 579.729
  • Catalog: BCRP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KS 176

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.IC50 value: 0.59( in Pheo A assay), 1.39 μM (in Hoechst 33342 assay).Target: BCRPThe more detailed information please refer to Compound 9 in the reference.

  • CAS Number: 1253452-78-6
  • MF: C22H19N3O5
  • MW: 405.40300
  • Catalog: BCRP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A