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MDR efflux

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35

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1

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Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N1423
    Glycocholic acid
    3 Publications Verification

    P-glycoprotein Bcl-2 Family G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite Bacterial Apoptosis FXR Caspase MDM-2/p53 LPL Receptor Metabolic Disease Inflammation/Immunology Cancer
    Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA) .
    Glycocholic acid
  • HY-136072
    Xeruborbactam disodium
    Maximum Cited Publications
    6 Publications Verification

    Bacterial Infection
    Xeruborbactam disodium is a potent, ultra-broad-spectrum boronic acid beta-lactamase inhibitor. Xeruborbactam disodium inhibits key serine and metallo beta-lactamases at a nano molar range .
    Xeruborbactam disodium
  • HY-N1423A
    Glycocholic acid sodium
    3 Publications Verification

    P-glycoprotein Bcl-2 Family G protein-coupled Bile Acid Receptor 1 Bacterial Apoptosis FXR Caspase MDM-2/p53 LPL Receptor Endogenous Metabolite Metabolic Disease Cancer
    Glycocholic acid sodium is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid sodium inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid sodium modulates related bile acid receptor signaling. Glycocholic acid sodium suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid sodium can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA) .
    Glycocholic acid sodium
  • HY-N1423S

    Isotope-Labeled Compounds P-glycoprotein Bcl-2 Family G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite Bacterial Apoptosis FXR Caspase MDM-2/p53 LPL Receptor Metabolic Disease Cancer
    Glycocholic acid-d4 is the deuterium labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
    Glycocholic acid-d4
  • HY-101511

    P-glycoprotein Cancer
    TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1 .
    TTT-28
  • HY-17013
    Dofequidar
    2 Publications Verification

    MS-209 free base

    P-glycoprotein Cancer
    Dofequidar (MS-209 free base) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .
    Dofequidar
  • HY-108694
    γ-Tocotrienol
    4 Publications Verification

    Endogenous Metabolite NF-κB Metabolic Disease Inflammation/Immunology
    γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment .
    γ-Tocotrienol
  • HY-17013A
    Dofequidar fumarate
    2 Publications Verification

    MS-209

    P-glycoprotein Cancer
    Dofequidar fumarate (MS-209) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar fumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar fumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .
    Dofequidar fumarate
  • HY-136069

    Bacterial Infection
    Xeruborbactam is a potent, ultra-broad-spectrum boronic acid beta-lactamase inhibitor. Xeruborbactam inhibits key serine and metallo beta-lactamases at a nano molar range .
    Xeruborbactam
  • HY-W013105

    N-Cholylglycine sodium salt, 98%

    Bcl-2 Family Caspase Endogenous Metabolite Bacterial MDM-2/p53 P-glycoprotein LPL Receptor FXR G protein-coupled Bile Acid Receptor 1 Apoptosis Others
    Sodium glycocholate hydrate, 98% is a bile acid derivative. Sodium glycocholate hydrate, 98% downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Sodium glycocholate hydrate, 98% inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Sodium glycocholate hydrate, 98% modulates related bile acid receptor signaling. Sodium glycocholate hydrate, 98% suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Sodium glycocholate hydrate, 98% can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA) .
    Sodium glycocholate hydrate, 98%
  • HY-N1423B
    Glycocholic acid hydrate
    3 Publications Verification

    Endogenous Metabolite Caspase G protein-coupled Bile Acid Receptor 1 LPL Receptor MDM-2/p53 Bcl-2 Family P-glycoprotein FXR Bacterial Apoptosis Metabolic Disease Inflammation/Immunology Cancer
    Glycocholic acid hydrate is a bile acid derivative. Glycocholic acid hydrate downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid hydrate inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid hydrate modulates related bile acid receptor signaling. Glycocholic acid hydrate suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid hydrate can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA) .
    Glycocholic acid hydrate
  • HY-P990196

    P-glycoprotein Cancer
    Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) is an anti-monkey/human MDR-1/CD243 IgG2a monoclonal antibody. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) can efficiently inhibit P-glycoprotein. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) enhances the inhibitory effect on multidrug resistance (MDR) by suppressing drug efflux. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) can be used for research on cancer .
    Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2)
  • HY-175838

    P-glycoprotein Cancer
    P-gp-IN-32 is a P-glycoprotein (P-gp) inhibitor. P-gp-IN-32 exhibits low cytotoxicity and potent multidrug resistance (MDR) reversal activity against Doxorubicin (HY-15142A) in MCF7/ADR cells (IC50 = 0.11 μM, reversal fold (RF) = 215.9). P-gp-IN-32 can bind to P-gp directly, induce a conformation change of P-gp and inhibit the efflux function. P-gp-IN-32 can be used for the research of cancer, such as breast cancer .
    P-gp-IN-32
  • HY-N11697

    P-glycoprotein Cancer
    α-Cryptoxanthin is a natural carotenoid with anticancer effects. α-Cryptoxanthin inhibits multidrug resistance 1 (MDR1) mediated efflux pump .
    α-Cryptoxanthin
  • HY-144366

    P-glycoprotein Cancer
    P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel .
    P-gp inhibitor 3
  • HY-108694R

    Reference Standards Endogenous Metabolite NF-κB Metabolic Disease Inflammation/Immunology
    γ-Tocotrienol (Standard) is the analytical standard of γ-Tocotrienol. This product is intended for research and analytical applications. γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a novel radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment .
    γ-Tocotrienol (Standard)
  • HY-N1423S1

    Isotope-Labeled Compounds P-glycoprotein Bcl-2 Family G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite Bacterial Apoptosis FXR Caspase MDM-2/p53 LPL Receptor Metabolic Disease Cancer
    Glycocholic acid-d5 is the deuterium labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
    Glycocholic acid-d5
  • HY-178466

    Microtubule/Tubulin P-glycoprotein Apoptosis Cancer
    Tubulin polymerization/P-gp-IN-1 is a Tubulin polymerization/P-gp dual inhibitor. Tubulin polymerization/P-gp-IN-1 inhibits tubulin polymerization and induces G2/M arrest and apoptosis. Tubulin polymerization/P-gp-IN-1 reverses MDR by inhibiting P-gp efflux function. Tubulin polymerization/P-gp-IN-1 has dual functions: direct antitumor activity and reversal of P-gp-mediated Cisplatin (HY-17394) resistance. Tubulin polymerization/P-gp-IN-1 stable binds to the tubulin CBS (ΔG = −12.4 kcal/mol) and the P-gp hydrophobic lumen (ΔG = −10.8 kcal/mol). Tubulin polymerization/P-gp-IN-1 can be used for the study of drug-resistant cervical cancer .
    Tubulin polymerization/P-gp-IN-1
  • HY-162822

    P-glycoprotein Cancer
    P-gp modulator-5 (compound 25) is a modulator of P-gp and can inhibit the proliferation of multidrug resistant (MDR) tumors. P-gp modulator-5 inhibits the activity of drug efflux pumps in MDR cells, leading to a large accumulation of ROS and altered cell cycle profiles .
    P-gp modulator-5
  • HY-161645

    P-glycoprotein Cancer
    P-gp modulator-4 (compound 4c) inhibits the efflux function of P-glycoprotein (P-gp). P-gp modulator-4 shows multidrug resistance (MDR) in cancer reversal activity (IC50 of Paclitaxel (HY-B0015) = 8.80, reversal fold = 211.8) .
    P-gp modulator-4
  • HY-17013D

    MS-209 sesquifumarate

    P-glycoprotein Cancer
    Dofequidar (MS-209) sesquifumarate is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar sesquifumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar sesquifumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .
    Dofequidar sesquifumarate
  • HY-159085

    P-glycoprotein Cancer
    P-gp inhibitor 24 (Compound 10) is an inhibitor for P-glycoprotein (P-gp)), that inhibits the P-gp mediated fluorescent dye efflux. P-gp inhibitor 24 exhibits multidrug resistance (MDR) reversal effect, enhances the cytotoxicity of Vincristine (HY-N0488) and Etoposide (HY-13629) in cancer cells .
    P-gp inhibitor 24
  • HY-175522

    P-glycoprotein Apoptosis Cancer
    P-gp-IN-31 is a P-glycoprotein (P-gp) inhibitor with IC50 values of 0.42 μM for KB cells and 0.43 μM for MDR KBvin cells. P-gp-IN-31 can pass P-gp-mediated drug efflux mechanisms and shows collateral sensitivity via P-gp downregulation. P-gp-IN-31 inhibits cell proliferation, induces apoptosis and arrests the cell cycle at G2/M phase. P-gp-IN-31 can be used for the research of cancer, such as multidrug-resistant (MDR) malignancies .
    P-gp-IN-31
  • HY-N15297

    P-glycoprotein Cancer
    Isotenulin inhibits the efflux function of P-glycoprotein by stimulation of P-glycoprotein ATPase, thereby overcoming the multidrug resistance (MDR) of cancer cells. Isotenulin exhibits cytotoxicity in multidrug-resistant cancer cell KB-vin and sensitive cancer cell HeLaS3. Isotenulin exhibits synergistic effect with Paclitaxel (HY-B0015), Vinblastine (HY-13780) and Doxorubicin (HY-15142) .
    Isotenulin
  • HY-161260

    P-glycoprotein Cancer
    P-gp inhibitor 20 (compound H27) is a low cytotoxicity P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 20 inhibits the efflux function of P-gp in a dose-dependent manner (without affecting the expression of P-gp), thereby reversing the multidrug resistance (MDR) of MCF-7/ADR cells, with an IC50 value of 46.6 nM. P-gp inhibitor 20 can be used for cancer research .
    P-gp inhibitor 20
  • HY-172771

    PI3K DNA-PK P-glycoprotein Cancer
    Multi-target kinase inhibitor 4 (Compound 2) is a PI3K/DNA-PK inhibitor and potent chemosensitizer that can increase the amount of DNA double strand breaks induced by Doxorubicin (HY-15142A). Multi-target kinase inhibitor 4, is an efficient inhibitor of multidrug resistance (MDR) that exhibits inhibitory activity toward P-glycoprotein-mediated drug efflux. Multi-target kinase inhibitor 4 can be loaded into PEG-coated LNPs .
    Multi-target kinase inhibitor 4
  • HY-N1423AR

    Reference Standards P-glycoprotein Bcl-2 Family G protein-coupled Bile Acid Receptor 1 Bacterial Apoptosis FXR Caspase MDM-2/p53 LPL Receptor Endogenous Metabolite Metabolic Disease Cancer
    Glycocholic acid (sodium) (Standard) is the analytical standard of Glycocholic acid sodium (HY-N1423A). This product is intended for research and analytical applications. Glycocholic acid sodium is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid sodium inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid sodium modulates related bile acid receptor signaling. Glycocholic acid sodium suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid sodium can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
    Glycocholic acid sodium (Standard)
  • HY-168921

    P-glycoprotein Apoptosis Cancer
    ABCB1-IN-3 (Compound K27) is an orally active inhibitor of ABCB1, and induces apoptosis. ABCB1-IN-3 directly binds to ABCB1 to inhibit efflux function, ensuring stable intracellular concentration of Paclitaxel (PTX) (HY-B0015) without affecting ABCB1 normal expression. ABCB1-IN-3 significantly increases the sensitivity of ABCB1-mediated multidrug resistance (MDR) to Paclitaxel in vitro, enhances cell cycle arrest, and inhibits proliferation. BCB1-IN-3 combined with Paclitaxel exhibits potent tumor suppression in vivo without generating toxicity .
    ABCB1-IN-3
  • HY-W754548

    Isotope-Labeled Compounds Endogenous Metabolite P-glycoprotein Bcl-2 Family G protein-coupled Bile Acid Receptor 1 Bacterial Apoptosis FXR Caspase MDM-2/p53 LPL Receptor Metabolic Disease Cancer
    Glycocholic acid- 13C2,d4 is the deuterium labeled and 13C-labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
    Glycocholic acid-13C2,d4
  • HY-179640

    PROTACs Aurora Kinase Cancer
    SK4454 is a selective AURKA PROTAC degrader degrading AURKA with IC50 = 8 nM. MYCN levels in MYCN-amplified neuroblastoma cells and limited by MDR1-mediated efflux. SK4454 efficiently reduced AURKA levels in vivo. SK4454 can be used for neuroblastoma research .
    SK4454
  • HY-181404

    Fungal P-glycoprotein Infection
    PA36-2 is an Mdr1 inhibitor and azole resistance reversal agent, with a IC50 of 1.0 μg/mL and a Kd of 4.209 μM against Candida albicans Mdr1. By effectively inhibiting the activity of the Mdr1 efflux pump, PA36-2 prevents the pumping of substrates out of cells, enhances the intracellular accumulation of azole antibiotics, and exerts a synergistic effect with antifungal agents such as Fluconazole (FLC) (HY-B0101). PA36-2 can be used in the research of azole-resistant candidiasis .
    PA36-2
  • HY-179641

    PROTACs Aurora Kinase Cancer
    SK5527 is a selective AURKA PROTAC degrader degrading AURKA with DC50 = 2 nM. SK5527 bind to NanoLuc-AURKA with an IC50 of 20 nM. SK5527 effectively reduces MYCN levels in MYCN-amplified neuroblastoma cells and limited by MDR1-mediated efflux. SK5527 efficiently reduced AURKA levels in vivo. SK5527 can be used for neuroblasto2ma research .
    SK5527
  • HY-101511R

    P-glycoprotein Reference Standards Cancer
    TTT-28 (Standard) is the analytical standard of TTT-28 (HY-101511). This product is intended for research and analytical applications. TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1 .
    TTT-28 (Standard)
  • HY-N16684

    P-glycoprotein Cancer
    Clausarin is a selective inhibitor of P-glycoprotein (P-gp), inhibiting P-gp-mediated drug efflux. Clausarin significantly inhibits Daunorubicin (HY-13062A) efflux in K562/R7 human leukemia cells overexpressing P-gp (with Cyclosporin A (HY-B0579) as a positive control). Clausarin can be naturally extracted from the roots of Citrus sinensis (sweet orange) and can be used in research related to overcoming multidrug resistance (MDR) in tumors .
    Clausarin
  • HY-17013AR

    MS-209 (Standard)

    P-glycoprotein Reference Standards Cancer
    Dofequidar (fumarate) (Standard) is the analytical standard of Dofequidar (fumarate). This product is intended for research and analytical applications. Dofequidar fumarate (MS-209) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar fumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar fumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .
    Dofequidar fumarate (Standard)

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