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Results for "

ABCG2 inhibitor

" in MedChemExpress (MCE) Product Catalog:

51

Inhibitors & Agonists

4

Natural
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6

Isotope-Labeled Compounds

1

GMP Molecules

Targets Recommended:
Cat. No. Nombre del producto Target Áreas de investigación Chemical Structure
  • HY-10010
    Ko 143
    45+ Cited Publications

    		 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-101570
    Nedisertib
    25+ 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-10440
    Vismodegib
    Maximum Cited Publications
    53 Publications Verification

    GDC-0449

    		 Hedgehog Autophagy Neurological Disease Inflammation/Immunology Cancer
    Vismodegib (GDC-0449) is a BBB-permeable and 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-101561
    Avapritinib
    10+ 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-109061
    Lazertinib
    3 Publications Verification

    YH25448; GNS-1480

    		 Apoptosis Akt TRP Channel EGFR ERK Infection Neurological Disease Metabolic Disease Cancer
    Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
    Lazertinib
  • 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-12758
    YHO-13351

    		BCRP Cancer
    YHO-13351 is an orally active ABCG2 inhibitor . YHO-13351 modulates the function of ABCG2, blocks BCRP-mediated compound efflux, downregulates the expression of breast cancer resistance protein at the post-transcriptional level, and reverses ABCG2-associated tolerance. YHO-13351 restores the toxicity of SN-38 to SN-38-resistant cancer cells and sensitizes cancer cells to Irinotecan. YHO-13351 is a water-soluble prodrug that is rapidly converted to YHO-13177 (HY-12757) in mice. YHO-13351 prolongs the median survival time of mice bearing cancer cell xenografts when combined with IMMU-132. YHO-13351 extends the survival time of tumor-bearing mice and inhibits the growth of xenograft tumors when combined with Irinotecan. YHO-13351 can be used for the research of breast cancer, gastric cancer, BCRP-mediated drug-resistant cancers, and cervical cancer .
    YHO-13351
  • HY-109061B
    Lazertinib mesylate
    3 Publications Verification

    YH25448 mesylate; GNS-1480 mesylate

    		 TRP Channel EGFR Akt ERK Apoptosis Cancer
    Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
    Lazertinib mesylate
  • 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-136450
    Triclabendazole sulfoxide

    TCBZ-SO

    		 Parasite BCRP Infection Cancer
    Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer .
    Triclabendazole sulfoxide
  • HY-146676
    UR-MB108

    		BCRP Cancer
    UR-MB108 is a selective ABCG2 inhibitor with an IC50 value of 79 nM. UR-MB108 acts as a potent inhibitor of ABCG2 transport and ATPase activity. UR-MB108 can be used in cancer-related research .
    UR-MB108
  • 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-100933
    MY-5445
    1 Publications Verification

    		 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-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-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-101570G
    Nedisertib

    Peposertib; M3814

    		 DNA-PK BCRP Cancer
    Nedisertib (GMP) (Peposertib (GMP)) is Nedisertib (HY-101570) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Nedisertib 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-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-17648
    MBL-II-141

    		BCRP Cancer
    MBL-II-141 is potent ABCG2 inhibitor with an IC50 of 0.11 μM. MBL-II-141 inhibits the transport function of ABCG2 in a non-competitive manner, preventing ABCG2 from pumping substrates (such as Irinotecan (HY-16562)) out of the cells, thereby increasing the accumulation of drugs within the cells. MBL-II-141 has no effect on ABCB1 (P-gp) and ABCC1 (MRP1) and has extremely low cytotoxicity (IG50 > 100 μM). MBL-II-141 can be used for the study of multidrug resistance (MDR) cancers .
    MBL-II-141
  • 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-174435
    ABCB1/ABCG2-IN-1

    		P-glycoprotein Cancer
    ABCB1/ABCG2-IN-1 (Compound (S,Z)-4b) is an inhibitor of ABCB1 and ABCB2 transporters. ABCB1/ABCG2-IN-1 shows moderate activity in SW620M, -V, and –Mito variants (IC50 ≈ 50 μM). ABCB1/ABCG2-IN-1 affects methotrexate resistance in vitro. ABCB1/ABCG2-IN-1 can be studied in anticancer research .
    ABCB1/ABCG2-IN-1
  • 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-178100
    PARP1-IN-45

    		PARP BCRP Cancer
    PARP1-IN-45 (Compound 15) is a PARP1 inhibitor with an IC50 of 17  nM. PARP1-IN-45 effectively stimulates ATPase activity of ABCG2. PARP1-IN-45 can be used for cancers like ovarian cancer research .
    PARP1-IN-45
  • HY-10440R
    Vismodegib (Standard)

    GDC-0449 (Standard)

    		 Reference Standards Hedgehog Autophagy Cancer
    Vismodegib (Standard) is the analytical standard of Vismodegib. This product is intended for research and analytical applications. Vismodegib (GDC-0449) is a BBB-permeable and 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-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-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-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-178386
    ABCG2-IN-5

    		BCRP Cancer
    ABCG2-IN-5 (Compound 10) is a is a selective ABCG2 inhibitor, with an IC50 of 0.34 µM. ABCG2-IN-5 can be used for the study of ABCG2-overexpressing tumors such as non-small cell lung cancer (NSCLC) .
    ABCG2-IN-5
  • 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
  • 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-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-136450R
    Triclabendazole sulfoxide (Standard)

    TCBZ-SO (Standard)

    		 Reference Standards 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 an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer .
    Triclabendazole sulfoxide (Standard)
  • 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 an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer .
    Triclabendazole sulfoxide-d3
  • 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-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 an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer .
    Triclabendazole sulfoxide-13C,d3
  • 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-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-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-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-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-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-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-181803
    MRS8432

    		BCRP Cancer
    MRS8432 is an ABCG2 modulator with an EC50 of 7.5 nM against human ABCG2. MRS8432 activates ABCG2 ATPase activity. MRS8432 partially inhibits ABCG2-mediated substrate transport. MRS8432 is applicable to research related to cancer multidrug resistance .
    MRS8432
  • HY-181802
    MRS8431

    		BCRP Cancer
    MRS8431 is an ABCG2 inhibitor with a IC50 of 160 nM against human ABCG2. MRS8432 partially inhibits ABCG2-mediated substrate transport. MRS8432 is applicable to research related to cancer multidrug resistance .
    MRS8431
  • HY-181804
    MRS8288

    		BCRP P-glycoprotein Cancer
    MRS8288 is a ABCG2 and P-glycoprotein inhibitor, with an IC50 of 0.96 μM against ABCG2 and an IC50 of 1.39 μM against P-glycoprotein. MRS8288 inhibits the ATPase activity of ABCG2 and P-glycoprotein, and suppresses ABCG2-mediated substrate transport. MRS8288 is applicable for cancer research .
    MRS8288
  • HY-181731S
    (R,S,R)-Altenuene-13C15

    		Isotope-Labeled Compounds Others
    (R,S,R)-Altenuene- 13C15 is the 13C-labeled (R,S,R)-Altenuene. Fumitremorgin C is a potent and selective ABCG2/BRCP inhibitor.
    (R,S,R)-Altenuene-13C15
  • HY-101570R
    Nedisertib (Standard)

    Peposertib (Standard); M3814 (Standard)

    		 DNA-PK Reference Standards BCRP Cancer
    Nedisertib (Standard) is the analytical standard of Nedisertib (HY-101570). This product is intended for research and analytical applications. 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 (Standard)
  • HY-109061A
    Lazertinib mesylate hydrate

    YH25448 mesylate hydrate; GNS-1480 mesylate hydrate

    		 Apoptosis Akt TRP Channel EGFR ERK Cancer
    Lazertinib (YH25448; GNS-1480) mesylate hydrate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate hydrate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate hydrate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate hydrate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate hydrate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
    Lazertinib mesylate hydrate
  • HY-10010R
    Ko 143 (Standard)

    		BCRP Reference Standards Cancer
    Ko 143 (Standard) is the analytical standard of Ko 143 (HY-10010). This product is intended for research and analytical applications. 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 (Standard)
  • HY-118083
    Pentamethoxymorin

    MRS923

    		 BCRP Cancer
    Pentamethoxymorin (MRS923) is a selective breast cancer resistance protein (BCRP/ABCG2) inhibitor. Pentamethoxymorin shows selectivity for BCRP over P-gp and MRP1. Pentamethoxymorin inhibits MDCK BCRP cells with IC50 vaues of 5.98 μM and 5.94 μM in Hoechst 33342 (HY-15559) assay and Pheophorbide A (HY-125665) assay, respectively. Pentamethoxymorin can be used for the study of ccancer .
    Pentamethoxymorin

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