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astemizole  (Tocris)


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    Structured Review

    Tocris astemizole
    Astemizole, supplied by Tocris, used in various techniques. Bioz Stars score: 93/100, based on 13 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/product/astemizole/Astemizole/10__1093_slash_rpsppr_slash_rqaf014-44-82-84
    Average 93 stars, based on 13 article reviews
    astemizole - by Bioz Stars, 2026-09
    93/100 stars

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    Related Articles

    Positive Control:

    Article Title: Identification of novel EED-EZH2 PPI inhibitors using an in silico fragment mapping method.
    Article Snippet: Enhancer of zeste homolog 2 (EZH2) is a histone lysine methyltransferase that is overexpressed in many cancers.. Numerous EZH2 inhibitors have been developed as anticancer agents, but recent studies have also focused on protein–protein interaction (PPI) between embryonic ectoderm development (EED) and EZH2 as a novel drug discovery target.. Because EED indirectly enhances EZH2 enzymatic activity, EED-EZH2 PPI inhibitors suppress the methyltransferase activity and inhibit cancer growth.

    Comparison:

    Article Title: Identification of novel EED-EZH2 PPI inhibitors using an in silico fragment mapping method.
    Article Snippet: Enhancer of zeste homolog 2 (EZH2) is a histone lysine methyltransferase that is overexpressed in many cancers.. Numerous EZH2 inhibitors have been developed as anticancer agents, but recent studies have also focused on protein–protein interaction (PPI) between embryonic ectoderm development (EED) and EZH2 as a novel drug discovery target.. Because EED indirectly enhances EZH2 enzymatic activity, EED-EZH2 PPI inhibitors suppress the methyltransferase activity and inhibit cancer growth.

    Saline:

    Article Title: An Investigation of Lysosome-Dependent Cell Death in Breast Cancer Cells Treated with Doxorubicin
    Article Snippet: 3.2.4 MATERIALS AND METHODS 3.2.4.1 Materials Trypsin/ EDTA buffer solution, penicillin and streptomycin antibiotic solutions, dimethyl sulfoxide (DMSO), EDTA, DL-Diothiothreitol (DTT) solution, glycerol, HEPES solution (1 M, pH 7.0-7.6), Triton X-100 (TX-100), hydrogen peroxide solution (30% w/w in water), and E64 protease inhibitor (EMD Millipore) were purchased from Sigma-Aldrich (St. Louis, MO). .. Dulbecco’s phosphate buffered saline (DPBS, Gibco), fetal bovine serum (FBS, Gibco), recombinant human insulin (Santa Cruz), trypan blue (Corning), Countess cell counter chamber slides (anitrogen), MTT (3-(4,5-Dimethylthiazol-2-yl)—2,5- Diphenyltetrazolium Bromide, Invitrogen), CTSB substrate 111 (Z-Arg-Arg-AMC, EMD Millipore), CellEventTMCaspase-3/7 green flow cytometry assay kit (Invitrogen), RPMI 1640 (Coming), staurosporine (STS, Enzo Life Sciences), and astemizole (AST, Tocris Bioscience) were purchased from Fisher (Pittsburgh, PA). .. MCF-7 and MDA-MB-231 breast cancer cells were purchased from American Type Culture Collection (ATCC, Manassas, VA) along with Eagle’s minimum essential medium (EMEM).

    Article Title: Lysosome-mediated cytotoxicity in breast cancer subtype cells treated with doxorubicin
    Article Snippet: Dimethyl sulphoxide (DMSO), hydrogen peroxide (H2O2, 30% w/v), E64 cysteine protease inhibitor (EMD Millipore), and MDA-MB-231 cells were purchased from Sigma-Aldrich (St. Louis, MO). .. Dulbecco’s phosphate buffered saline (DPBS, Gibco), trypsin/EDTA, penicillin/streptomycin, fetal bovine serum (FBS, Gibco), recombinant human insulin (Santa Cruz), 3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide (MTT, Invitrogen), LysoTracker Green DND-26 (LTG, Molecular Probes), JC-1 assay kit (Molecular Probes), Hoechst 33342 (20 mM, Thermo Scientific), poly-L-lysine coated glass coverslips (NeuVitro), 10 kDa AlexaFluor488 dextran (Invitrogen), CTSB substrate III (Z-Arg-ArgAMC, EMD Millipore), H2DCFDA/DCFDA (Invitrogen), pifithrin-α (PFT-α, EMD Millipore), tiron (Thermo Scientific), trypan blue (0.4% w/v, Corning), Countess chamber slides (Invitrogen), RPMI 1640 (Corning), staurosporine (STS, Enzo Life Sciences), and astemizole (AST, Tocris Bioscience) were purchased from Fisher Scientific (Pittsburgh, PA). .. MCF-7 cells, MDA-MB-361 cells, Eagle’s minimum essential medium (EMEM), and Leibovitz’s L15 medium were purchased from American Type Culture Collection (ATCC) (Manassas, VA).

    Recombinant:

    Article Title: An Investigation of Lysosome-Dependent Cell Death in Breast Cancer Cells Treated with Doxorubicin
    Article Snippet: 3.2.4 MATERIALS AND METHODS 3.2.4.1 Materials Trypsin/ EDTA buffer solution, penicillin and streptomycin antibiotic solutions, dimethyl sulfoxide (DMSO), EDTA, DL-Diothiothreitol (DTT) solution, glycerol, HEPES solution (1 M, pH 7.0-7.6), Triton X-100 (TX-100), hydrogen peroxide solution (30% w/w in water), and E64 protease inhibitor (EMD Millipore) were purchased from Sigma-Aldrich (St. Louis, MO). .. Dulbecco’s phosphate buffered saline (DPBS, Gibco), fetal bovine serum (FBS, Gibco), recombinant human insulin (Santa Cruz), trypan blue (Corning), Countess cell counter chamber slides (anitrogen), MTT (3-(4,5-Dimethylthiazol-2-yl)—2,5- Diphenyltetrazolium Bromide, Invitrogen), CTSB substrate 111 (Z-Arg-Arg-AMC, EMD Millipore), CellEventTMCaspase-3/7 green flow cytometry assay kit (Invitrogen), RPMI 1640 (Coming), staurosporine (STS, Enzo Life Sciences), and astemizole (AST, Tocris Bioscience) were purchased from Fisher (Pittsburgh, PA). .. MCF-7 and MDA-MB-231 breast cancer cells were purchased from American Type Culture Collection (ATCC, Manassas, VA) along with Eagle’s minimum essential medium (EMEM).

    Article Title: Lysosome-mediated cytotoxicity in breast cancer subtype cells treated with doxorubicin
    Article Snippet: Dimethyl sulphoxide (DMSO), hydrogen peroxide (H2O2, 30% w/v), E64 cysteine protease inhibitor (EMD Millipore), and MDA-MB-231 cells were purchased from Sigma-Aldrich (St. Louis, MO). .. Dulbecco’s phosphate buffered saline (DPBS, Gibco), trypsin/EDTA, penicillin/streptomycin, fetal bovine serum (FBS, Gibco), recombinant human insulin (Santa Cruz), 3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide (MTT, Invitrogen), LysoTracker Green DND-26 (LTG, Molecular Probes), JC-1 assay kit (Molecular Probes), Hoechst 33342 (20 mM, Thermo Scientific), poly-L-lysine coated glass coverslips (NeuVitro), 10 kDa AlexaFluor488 dextran (Invitrogen), CTSB substrate III (Z-Arg-ArgAMC, EMD Millipore), H2DCFDA/DCFDA (Invitrogen), pifithrin-α (PFT-α, EMD Millipore), tiron (Thermo Scientific), trypan blue (0.4% w/v, Corning), Countess chamber slides (Invitrogen), RPMI 1640 (Corning), staurosporine (STS, Enzo Life Sciences), and astemizole (AST, Tocris Bioscience) were purchased from Fisher Scientific (Pittsburgh, PA). .. MCF-7 cells, MDA-MB-361 cells, Eagle’s minimum essential medium (EMEM), and Leibovitz’s L15 medium were purchased from American Type Culture Collection (ATCC) (Manassas, VA).

    MTT Assay:

    Article Title: An Investigation of Lysosome-Dependent Cell Death in Breast Cancer Cells Treated with Doxorubicin
    Article Snippet: 3.2.4 MATERIALS AND METHODS 3.2.4.1 Materials Trypsin/ EDTA buffer solution, penicillin and streptomycin antibiotic solutions, dimethyl sulfoxide (DMSO), EDTA, DL-Diothiothreitol (DTT) solution, glycerol, HEPES solution (1 M, pH 7.0-7.6), Triton X-100 (TX-100), hydrogen peroxide solution (30% w/w in water), and E64 protease inhibitor (EMD Millipore) were purchased from Sigma-Aldrich (St. Louis, MO). .. Dulbecco’s phosphate buffered saline (DPBS, Gibco), fetal bovine serum (FBS, Gibco), recombinant human insulin (Santa Cruz), trypan blue (Corning), Countess cell counter chamber slides (anitrogen), MTT (3-(4,5-Dimethylthiazol-2-yl)—2,5- Diphenyltetrazolium Bromide, Invitrogen), CTSB substrate 111 (Z-Arg-Arg-AMC, EMD Millipore), CellEventTMCaspase-3/7 green flow cytometry assay kit (Invitrogen), RPMI 1640 (Coming), staurosporine (STS, Enzo Life Sciences), and astemizole (AST, Tocris Bioscience) were purchased from Fisher (Pittsburgh, PA). .. MCF-7 and MDA-MB-231 breast cancer cells were purchased from American Type Culture Collection (ATCC, Manassas, VA) along with Eagle’s minimum essential medium (EMEM).

    Article Title: Lysosome-mediated cytotoxicity in breast cancer subtype cells treated with doxorubicin
    Article Snippet: Dimethyl sulphoxide (DMSO), hydrogen peroxide (H2O2, 30% w/v), E64 cysteine protease inhibitor (EMD Millipore), and MDA-MB-231 cells were purchased from Sigma-Aldrich (St. Louis, MO). .. Dulbecco’s phosphate buffered saline (DPBS, Gibco), trypsin/EDTA, penicillin/streptomycin, fetal bovine serum (FBS, Gibco), recombinant human insulin (Santa Cruz), 3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide (MTT, Invitrogen), LysoTracker Green DND-26 (LTG, Molecular Probes), JC-1 assay kit (Molecular Probes), Hoechst 33342 (20 mM, Thermo Scientific), poly-L-lysine coated glass coverslips (NeuVitro), 10 kDa AlexaFluor488 dextran (Invitrogen), CTSB substrate III (Z-Arg-ArgAMC, EMD Millipore), H2DCFDA/DCFDA (Invitrogen), pifithrin-α (PFT-α, EMD Millipore), tiron (Thermo Scientific), trypan blue (0.4% w/v, Corning), Countess chamber slides (Invitrogen), RPMI 1640 (Corning), staurosporine (STS, Enzo Life Sciences), and astemizole (AST, Tocris Bioscience) were purchased from Fisher Scientific (Pittsburgh, PA). .. MCF-7 cells, MDA-MB-361 cells, Eagle’s minimum essential medium (EMEM), and Leibovitz’s L15 medium were purchased from American Type Culture Collection (ATCC) (Manassas, VA).

    Flow Cytometry:

    Article Title: An Investigation of Lysosome-Dependent Cell Death in Breast Cancer Cells Treated with Doxorubicin
    Article Snippet: 3.2.4 MATERIALS AND METHODS 3.2.4.1 Materials Trypsin/ EDTA buffer solution, penicillin and streptomycin antibiotic solutions, dimethyl sulfoxide (DMSO), EDTA, DL-Diothiothreitol (DTT) solution, glycerol, HEPES solution (1 M, pH 7.0-7.6), Triton X-100 (TX-100), hydrogen peroxide solution (30% w/w in water), and E64 protease inhibitor (EMD Millipore) were purchased from Sigma-Aldrich (St. Louis, MO). .. Dulbecco’s phosphate buffered saline (DPBS, Gibco), fetal bovine serum (FBS, Gibco), recombinant human insulin (Santa Cruz), trypan blue (Corning), Countess cell counter chamber slides (anitrogen), MTT (3-(4,5-Dimethylthiazol-2-yl)—2,5- Diphenyltetrazolium Bromide, Invitrogen), CTSB substrate 111 (Z-Arg-Arg-AMC, EMD Millipore), CellEventTMCaspase-3/7 green flow cytometry assay kit (Invitrogen), RPMI 1640 (Coming), staurosporine (STS, Enzo Life Sciences), and astemizole (AST, Tocris Bioscience) were purchased from Fisher (Pittsburgh, PA). .. MCF-7 and MDA-MB-231 breast cancer cells were purchased from American Type Culture Collection (ATCC, Manassas, VA) along with Eagle’s minimum essential medium (EMEM).

    AST Assay:

    Article Title: An Investigation of Lysosome-Dependent Cell Death in Breast Cancer Cells Treated with Doxorubicin
    Article Snippet: 3.2.4 MATERIALS AND METHODS 3.2.4.1 Materials Trypsin/ EDTA buffer solution, penicillin and streptomycin antibiotic solutions, dimethyl sulfoxide (DMSO), EDTA, DL-Diothiothreitol (DTT) solution, glycerol, HEPES solution (1 M, pH 7.0-7.6), Triton X-100 (TX-100), hydrogen peroxide solution (30% w/w in water), and E64 protease inhibitor (EMD Millipore) were purchased from Sigma-Aldrich (St. Louis, MO). .. Dulbecco’s phosphate buffered saline (DPBS, Gibco), fetal bovine serum (FBS, Gibco), recombinant human insulin (Santa Cruz), trypan blue (Corning), Countess cell counter chamber slides (anitrogen), MTT (3-(4,5-Dimethylthiazol-2-yl)—2,5- Diphenyltetrazolium Bromide, Invitrogen), CTSB substrate 111 (Z-Arg-Arg-AMC, EMD Millipore), CellEventTMCaspase-3/7 green flow cytometry assay kit (Invitrogen), RPMI 1640 (Coming), staurosporine (STS, Enzo Life Sciences), and astemizole (AST, Tocris Bioscience) were purchased from Fisher (Pittsburgh, PA). .. MCF-7 and MDA-MB-231 breast cancer cells were purchased from American Type Culture Collection (ATCC, Manassas, VA) along with Eagle’s minimum essential medium (EMEM).

    Article Title: Lysosome-mediated cytotoxicity in breast cancer subtype cells treated with doxorubicin
    Article Snippet: Dimethyl sulphoxide (DMSO), hydrogen peroxide (H2O2, 30% w/v), E64 cysteine protease inhibitor (EMD Millipore), and MDA-MB-231 cells were purchased from Sigma-Aldrich (St. Louis, MO). .. Dulbecco’s phosphate buffered saline (DPBS, Gibco), trypsin/EDTA, penicillin/streptomycin, fetal bovine serum (FBS, Gibco), recombinant human insulin (Santa Cruz), 3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide (MTT, Invitrogen), LysoTracker Green DND-26 (LTG, Molecular Probes), JC-1 assay kit (Molecular Probes), Hoechst 33342 (20 mM, Thermo Scientific), poly-L-lysine coated glass coverslips (NeuVitro), 10 kDa AlexaFluor488 dextran (Invitrogen), CTSB substrate III (Z-Arg-ArgAMC, EMD Millipore), H2DCFDA/DCFDA (Invitrogen), pifithrin-α (PFT-α, EMD Millipore), tiron (Thermo Scientific), trypan blue (0.4% w/v, Corning), Countess chamber slides (Invitrogen), RPMI 1640 (Corning), staurosporine (STS, Enzo Life Sciences), and astemizole (AST, Tocris Bioscience) were purchased from Fisher Scientific (Pittsburgh, PA). .. MCF-7 cells, MDA-MB-361 cells, Eagle’s minimum essential medium (EMEM), and Leibovitz’s L15 medium were purchased from American Type Culture Collection (ATCC) (Manassas, VA).

    other:

    Article Title: Migraine-provoking substances evoke periorbital allodynia in mice
    Article Snippet: CGRP, amylin, PACAP, VIP, PGF 2α , olcegepant, astemizole, ER819762 and Ro1138452 were from Tocris Bioscience (Bristol, UK); adrenomedullin, PACAP6-38, PGE 2 , PGI 2 and histamine were from Sigma Aldrich (Milan, Italy); the mouse monoclonal anti-CGRP antibody (clone [4901]) and the inactive immunoglobulin (mouse monoclonal IgG2a) were from Abcam (Cambridge, UK)



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    Image Search Results


    Pharmacological agents astemizole and celastrol rescue S100P-induced epithelial barrier disfunction. ( A ) Heatmap visualization of calculated binding energies (kcal/mol) for S100P-ligand interactions. ( B-C ) Molecular docking and Molecular dynamics simulations (100 ns) results of S100P with astemizole or celastrol. ( D ) Effects of astemizole and celastrol on the viability of 16HBE cells were assessed by CCK-8 assay for 24 h ( n = 3). ( E , F ) Immunofluorescence analysis of tight junction proteins in 16HBE cells treated with S100P and candidate compound (astemizole 1000 nM and celastrol 500 nM), (Magnification: 200×; scale bar: 50 μm), ( n = 4). ( G ) Measurement of TEER in 16HBE cells treated with S100P and candidate compound at 0, 6, 12, 24 h post-treatment ( n = 4). Data are presented as mean ± SEM. * P < 0.05: S100P vs. Control, # P < 0.05: S100P vs. S100P+astemizole/celastrol, ns: S100P vs. S100P+DMSO

    Journal: Journal of Translational Medicine

    Article Title: S100P mediates IL-13/ATF4-driven epithelial barrier dysfunction in eosinophilic asthma: a potential biomarker and therapeutic target

    doi: 10.1186/s12967-026-08132-y

    Figure Lengend Snippet: Pharmacological agents astemizole and celastrol rescue S100P-induced epithelial barrier disfunction. ( A ) Heatmap visualization of calculated binding energies (kcal/mol) for S100P-ligand interactions. ( B-C ) Molecular docking and Molecular dynamics simulations (100 ns) results of S100P with astemizole or celastrol. ( D ) Effects of astemizole and celastrol on the viability of 16HBE cells were assessed by CCK-8 assay for 24 h ( n = 3). ( E , F ) Immunofluorescence analysis of tight junction proteins in 16HBE cells treated with S100P and candidate compound (astemizole 1000 nM and celastrol 500 nM), (Magnification: 200×; scale bar: 50 μm), ( n = 4). ( G ) Measurement of TEER in 16HBE cells treated with S100P and candidate compound at 0, 6, 12, 24 h post-treatment ( n = 4). Data are presented as mean ± SEM. * P < 0.05: S100P vs. Control, # P < 0.05: S100P vs. S100P+astemizole/celastrol, ns: S100P vs. S100P+DMSO

    Article Snippet: Once ~ 70% confluence was attained, cells were subjected to a starvation for a period of 6–8 h. Thereafter, the cells were treated with IL-13 (Novoprotein, Shanghai, China), ATF4-IN-2 (MedChemExpress, Monmouth Junction, NJ, USA), astemizole (MedChemExpress, Monmouth Junction, NJ, USA), and celastrol (MedChemExpress, Monmouth Junction, NJ, USA) for 24 h. Subsequently, 10 μL of CCK-8 reagent, mixed with 90 μL of complete medium, was added to each well, followed by incubation for 1–2 h incubation at 37 °C.

    Techniques: Binding Assay, CCK-8 Assay, Immunofluorescence, Control