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Results for "

ABCG2 inhibitor

" in MedChemExpress (MCE) Product Catalog:

35

Inhibitors & Agonists

4

Natural
Products

5

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N2143
    Fumitremorgin C
    3 Publications Verification

    12α-Fumitremorgin C

    		 BCRP Bacterial Antibiotic Infection Cancer
    Fumitremorgin C is a potent and selective ABCG2/BRCP inhibitor.
    Fumitremorgin C
  • HY-111678
    ML230

    CID44640177; SID 88095709

    		 BCRP Cancer
    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 .
    ML230
  • HY-101570
    Nedisertib
    15+ Cited Publications

    Peposertib; M3814

    		 DNA-PK BCRP Cancer
    Nedisertib (Peposertib) is an orally active selective DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of less than 3 nM. Nedisertib also acts as a modulator of ABCG2, capable of reversing ABCG2-mediated multidrug resistance (MDR), thus providing new strategies for combination therapy. By inhibiting DNA double-strand break repair, Nedisertib can enhance the efficacy of chemotherapy and radiotherapy. Nedisertib exhibits antitumor activity .
    Nedisertib
  • HY-136450
    Triclabendazole sulfoxide

    TCBZ-SO

    		 Parasite BCRP Infection
    Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP .
    Triclabendazole sulfoxide
  • HY-155652
    ABCG2-IN-1

    		BCRP Cancer
    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 .
    ABCG2-IN-1
  • HY-119724
    ABCG2-IN-3

    		BCRP Cancer
    ABCG2-IN-3 (Compound 52) is a selective inhibitor for breast cancer resistance protein (ABCG2), with an IC50 of 0.238 µM. ABCG2-IN-3 reverses the ABCG2-mediated resistance toward SN-38 and inhibit the ATPase activity .
    ABCG2-IN-3
  • HY-155653
    ABCG2-IN-2

    		BCRP Cancer
    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) .
    ABCG2-IN-2
  • HY-168573
    AZ99

    		BCRP Cancer
    AZ99 (compound 7) is a potent ABCG2 inhibitor. AZ99 inhibits ABCG2-mediated transport of estrone-3-sulfate (E1S) into proteoliposomes and ABCG2 ATPase activity .
    AZ99
  • HY-170396
    ABCG2-IN-4

    		BCRP Inflammation/Immunology
    ABCG2-IN-4 (Compound K31) is an orally active inhibitor for ABCG2, which reduces the release of Protoporphyrin IX (PPIX) (HY-B1247) from erythrocytes into plasma, and prevents the reduces phototoxicity. ABCG2-IN-4 exhibits anti-inflammatory and antioxidant activity in mouse models .
    ABCG2-IN-4
  • HY-149469
    3,7,2',4'-Tetramethoxy-5-hydroxyflavone

    		BCRP Cancer
    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 .
    3,7,2',4'-Tetramethoxy-5-hydroxyflavone
  • HY-18010
    PCI 29732
    3 Publications Verification

    		 Btk BCRP Inflammation/Immunology
    PCI 29732 is a potent, orally active, reversible BTK inhibitor with Ki app 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 .
    PCI 29732
  • HY-122416
    6,8-Diprenylnaringenin

    Lonchocarpol A; Senegalensin

    		 BCRP Metabolic Disease Cancer
    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 .
    6,8-Diprenylnaringenin
  • HY-156092
    Antitumor photosensitizer-4

    		BCRP Apoptosis Cancer
    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 .
    Antitumor photosensitizer-4
  • HY-146676
    UR-MB108

    		BCRP Cancer
    UR-MB108 (Compound 57) is a potent, selective ABCG2 (BCRP) inhibitor with an IC50 of 79 nM. UR-MB108 is stable in blood plasma .
    UR-MB108
  • HY-10010
    Ko 143
    Maximum Cited Publications
    40 Publications Verification

    		 BCRP Cancer
    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 .
    Ko 143
  • HY-129301
    CCTA-1523

    		BCRP Cancer
    CCTA-1523 is a potent, selective, reversible and orally active ABCG2 inhibitor. CCTA-1523 shows cytotoxicity. CCTA-1523 shows anticancer activity .
    CCTA-1523
  • HY-136450S
    Triclabendazole sulfoxide-d3

    TCBZ-SO-d3

    		 Isotope-Labeled Compounds Parasite BCRP Infection
    Triclabendazole sulfoxide-d3 is the deuterium labeled 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 .
    Triclabendazole sulfoxide-d3
  • HY-N2651
    5,7,3'-Trihydroxy-4'-Methoxy-8-prenylflavanone

    		BCRP Cancer
    5,7,3'-Trihydroxy-4'-Methoxy-8-prenylflavanone (compound 1), a flavonoid, is a potent ABCG2 inhibitor with an IC50 of 6.6 μM .
    5,7,3'-Trihydroxy-4'-Methoxy-8-prenylflavanone
  • HY-112505
    Efflux inhibitor-1

    		BCRP Cancer
    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 .
    Efflux inhibitor-1
  • HY-136450R
    Triclabendazole sulfoxide (Standard)

    		Parasite BCRP Infection
    Triclabendazole sulfoxide (Standard) is the analytical standard of Triclabendazole sulfoxide. This product is intended for research and analytical applications. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP .
    Triclabendazole sulfoxide (Standard)
  • HY-10440
    Vismodegib
    35+ Cited Publications

    GDC-0449

    		 Hedgehog Autophagy Cancer
    Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively .
    Vismodegib
  • HY-136450S1
    Triclabendazole sulfoxide-13C,d3

    TCBZ-SO-13C,d3

    		 Isotope-Labeled Compounds Parasite BCRP Infection
    Triclabendazole sulfoxide- 13C,d3 is the 13C- and deuterium labeled 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 .
    Triclabendazole sulfoxide-13C,d3
  • HY-113805
    MC70

    		P-glycoprotein Cancer
    MC70 is a potent and non-selective P-glycoprotein (P-gp) inhibitor with an EC50 of 0.69 µM. MC70 is an ABC transporters inhibitor and anticancer agent. MC70 interacts with ABCB1, ABCG2 and ABCC1 .
    MC70
  • HY-168572
    MZ82

    		BCRP Cancer
    MZ82, Ko 143 (HY-10010) derivative, is a ATP-binding cassette subfamily G member 2 (ABCG2/BCRP) inhibitor with the IC50 of ~23 nM. MZ82 not only shows greatly improved metabolic stability over Ko 143 (HY-10010) in liver microsomes but also in mice, and is able to penetrate into the brain .
    MZ82
  • HY-W716916
    Vismodegib-d7

    		Isotope-Labeled Compounds Cancer
    Vismodegib-d7 is deuterium labeled Vismodegib. Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively .
    Vismodegib-d7
  • HY-W705354
    Vismodegib-d4

    		Isotope-Labeled Compounds Hedgehog Autophagy Cancer
    Vismodegib-d4 is deuterium labeled Vismodegib. Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively .
    Vismodegib-d4
  • HY-10440R
    Vismodegib (Standard)

    		Hedgehog Autophagy Cancer
    Vismodegib (Standard) is the analytical standard of Vismodegib. This product is intended for research and analytical applications. Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively .
    Vismodegib (Standard)
  • HY-100933
    MY-5445

    		Phosphodiesterase (PDE) Cardiovascular Disease Inflammation/Immunology Cancer
    MY-5445 is a specific inhibitor of the cyclic GMP phosphodiesterase, phosphodiesterase type 5 (PDE5), with a Ki of 1.3 μM. MY-5445 inhibits human platelet aggregation. MY-5445 is a selective modulator of ATP-binding cassette (ABC) transporter ABCG2, with anti-proliferative effect .
    MY-5445
  • HY-103439
    GW583340 dihydrochloride

    		EGFR Cancer
    GW 583340 dihydrochloride is a potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50: 0.01 and 0.014 μM respectively). GW 583340 dihydrochloride reverses ABCG2- and ABCB1-mediated drug resistance. GW 583340 dihydrochloride has anti-cancer activity .
    GW583340 dihydrochloride
  • HY-144305
    KPH2f

    		URAT1 GLUT Infection
    KPH2f is a safe, orally active, and effective dual URAT1/GLUT9 inhibitor with IC50s of 0.24 μM and 9.37 μM for URAT1 and GLUT9, respectively. KPH2f shows little effects on OAT1 and ABCG2 (IC50=32.14 and 26.74 μM) .
    KPH2f
  • HY-W082856A
    Butein tetramethyl ether

    		BCRP Cancer
    Butein tetramethyl ether (Compound 20) is a potent and selective breast cancer resistance protein/ATP-binding cassette subfamily G member 2 (BCRP/ABCG2) inhibitor. Butein tetramethyl ether has inhibitory potencies against MCF-7 MX and MDCK BCRP cells with IC50 values of 2.2 and 1.03 μM, respectively. Butein tetramethyl ether is promising for research of cancers .
    Butein tetramethyl ether
  • HY-12757
    YHO-13177
    2 Publications Verification

    		 BCRP Cancer
    YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model .
    YHO-13177
  • HY-101561
    Avapritinib
    5+ Cited Publications

    BLU-285

    		 c-Kit PDGFR Cancer
    Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
    Avapritinib
  • HY-101561R
    Avapritinib (Standard)

    BLU-285 (Standard)

    		 Reference Standards c-Kit PDGFR Cancer
    Avapritinib (Standard) is the analytical standard of Avapritinib. This product is intended for research and analytical applications. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
    Avapritinib (Standard)
  • HY-W754911
    Avapritinib-d3

    BLU-285-d3

    		 Isotope-Labeled Compounds PDGFR c-Kit Cancer
    Avapritinib-d3 (BLU-285-d3) is deuterium labeled Avapritinib. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
    Avapritinib-d3

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