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compounds tc14012  (Tocris)


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    Structured Review

    Tocris compounds tc14012
    (A), (B) and (C): Inhibition of the CXCL12/CXCR4 interaction by (A) the peptide analogs T22, T140, <t>TC14012</t> and CTCE-9908 and the small molecules (B) AMD3100, AMD3465, AMD11070, IT1t and (C) WZ811, Me6TREN and gambogic acid. Jurkat cells were incubated with 2.9 nM CXCL12 AF647 in the presence of different concentrations of compound. Data are represented as % inhibition of maximal CXCL12 binding to CXCR4. Mean ± SEM of three or four independent experiments is shown.
    Compounds Tc14012, supplied by Tocris, used in various techniques. Bioz Stars score: 92/100, based on 15 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/result/compounds tc14012/product/Tocris
    Average 92 stars, based on 15 article reviews
    compounds tc14012 - by Bioz Stars, 2026-05
    92/100 stars

    Images

    1) Product Images from "Comparison of cell-based assays for the identification and evaluation of competitive CXCR4 inhibitors"

    Article Title: Comparison of cell-based assays for the identification and evaluation of competitive CXCR4 inhibitors

    Journal: PLoS ONE

    doi: 10.1371/journal.pone.0176057

    (A), (B) and (C): Inhibition of the CXCL12/CXCR4 interaction by (A) the peptide analogs T22, T140, TC14012 and CTCE-9908 and the small molecules (B) AMD3100, AMD3465, AMD11070, IT1t and (C) WZ811, Me6TREN and gambogic acid. Jurkat cells were incubated with 2.9 nM CXCL12 AF647 in the presence of different concentrations of compound. Data are represented as % inhibition of maximal CXCL12 binding to CXCR4. Mean ± SEM of three or four independent experiments is shown.
    Figure Legend Snippet: (A), (B) and (C): Inhibition of the CXCL12/CXCR4 interaction by (A) the peptide analogs T22, T140, TC14012 and CTCE-9908 and the small molecules (B) AMD3100, AMD3465, AMD11070, IT1t and (C) WZ811, Me6TREN and gambogic acid. Jurkat cells were incubated with 2.9 nM CXCL12 AF647 in the presence of different concentrations of compound. Data are represented as % inhibition of maximal CXCL12 binding to CXCR4. Mean ± SEM of three or four independent experiments is shown.

    Techniques Used: Inhibition, Incubation, Binding Assay

    Fluo-2 AM loaded cells were treated with serial dilutions of compound and subsequently stimulated with 6.25 nM CXCL12. Fluorescence changes were measured over time in all wells simultaneously. (A): The inhibitory effect of different concentrations of AMD11070 on CXCL12-induced calcium release is shown. The red and blue line represent the negative (untreated, without CXCL12 stimulation) and positive (untreated, CXCL12 stimulation) control, respectively. Calcium fluxes are represented as % of baseline ( i . e . mean relative light units in each well during a fixed time interval before CXCL12 addition). One representative experiment out of three is shown with each data point corresponding to the mean fluorescence of three to six replicates. (B), (C) and (D): Inhibitory effect of (B) T22, T140, TC14012, CTCE-9908, (C) AMD3100, AMD3465, AMD11070, IT1t, (D) WZ811, Me6TREN and gambogic acid on CXCL12-induced calcium flux. Data are represented as % inhibition of CXCL12-induced calcium mobilization relative to the positive and negative control. Mean ± SEM of three independent experiments is shown.
    Figure Legend Snippet: Fluo-2 AM loaded cells were treated with serial dilutions of compound and subsequently stimulated with 6.25 nM CXCL12. Fluorescence changes were measured over time in all wells simultaneously. (A): The inhibitory effect of different concentrations of AMD11070 on CXCL12-induced calcium release is shown. The red and blue line represent the negative (untreated, without CXCL12 stimulation) and positive (untreated, CXCL12 stimulation) control, respectively. Calcium fluxes are represented as % of baseline ( i . e . mean relative light units in each well during a fixed time interval before CXCL12 addition). One representative experiment out of three is shown with each data point corresponding to the mean fluorescence of three to six replicates. (B), (C) and (D): Inhibitory effect of (B) T22, T140, TC14012, CTCE-9908, (C) AMD3100, AMD3465, AMD11070, IT1t, (D) WZ811, Me6TREN and gambogic acid on CXCL12-induced calcium flux. Data are represented as % inhibition of CXCL12-induced calcium mobilization relative to the positive and negative control. Mean ± SEM of three independent experiments is shown.

    Techniques Used: Fluorescence, Control, Inhibition, Negative Control

    SUP-T1 cells were stained with a mAb targeting the N-terminus of CXCR4 (clone 1D9) and then treated with different concentrations of compound. CXCR4 internalization was induced by stimulating samples with CXCL12 at 37°C and quantified by flow cytometry. (A): Flow cytometric analysis of the negative (untreated, no CXCL12 stimulation; red histogram) and positive (untreated, CXCL12 stimulation; dark blue histogram) control and TC14012-treated samples (50 nM to 0.5 nM; light blue, green and orange histogram, respectively). (B), (C) and (D): Inhibitory effect of (B) T22, T140, TC14012, CTCE-9908, (C) AMD3100, AMD3465, AMD11070, IT1t, (D) WZ811, Me6TREN and gambogic acid on CXCR4 endocytosis. Data are represented as % of CXCR4 internalization relative to the positive and negative control. Mean ± SEM of at least two independent experiments is shown.
    Figure Legend Snippet: SUP-T1 cells were stained with a mAb targeting the N-terminus of CXCR4 (clone 1D9) and then treated with different concentrations of compound. CXCR4 internalization was induced by stimulating samples with CXCL12 at 37°C and quantified by flow cytometry. (A): Flow cytometric analysis of the negative (untreated, no CXCL12 stimulation; red histogram) and positive (untreated, CXCL12 stimulation; dark blue histogram) control and TC14012-treated samples (50 nM to 0.5 nM; light blue, green and orange histogram, respectively). (B), (C) and (D): Inhibitory effect of (B) T22, T140, TC14012, CTCE-9908, (C) AMD3100, AMD3465, AMD11070, IT1t, (D) WZ811, Me6TREN and gambogic acid on CXCR4 endocytosis. Data are represented as % of CXCR4 internalization relative to the positive and negative control. Mean ± SEM of at least two independent experiments is shown.

    Techniques Used: Staining, Flow Cytometry, Control, Negative Control

    (A), (B) and (C): Effect of (A) T22, T140, TC14012, CTCE-9908, (B) AMD3100, AMD3465, AMD11070, IT1t, (C) WZ811, Me6TREN and gambogic acid on chemotaxis of CXCR4-positive Jurkat cells. After compound treatment, cells were allowed to migrate towards 6.25 nM CXCL12, present in the lower compartment of the insert, for two hours. The migrated cells were counted by flow cytometry. Data are represented as % inhibition of migration relative to the negative and positive control (spontaneously migrated cells and cells migrated towards CXCL12, respectively). ± SEM of two to three independent experiments, each performed in triplicate.
    Figure Legend Snippet: (A), (B) and (C): Effect of (A) T22, T140, TC14012, CTCE-9908, (B) AMD3100, AMD3465, AMD11070, IT1t, (C) WZ811, Me6TREN and gambogic acid on chemotaxis of CXCR4-positive Jurkat cells. After compound treatment, cells were allowed to migrate towards 6.25 nM CXCL12, present in the lower compartment of the insert, for two hours. The migrated cells were counted by flow cytometry. Data are represented as % inhibition of migration relative to the negative and positive control (spontaneously migrated cells and cells migrated towards CXCL12, respectively). ± SEM of two to three independent experiments, each performed in triplicate.

    Techniques Used: Chemotaxis Assay, Flow Cytometry, Inhibition, Migration, Positive Control

    Anti-HIV-1 (X4) activity of CXCR4 compounds evaluated in CD4-positive MT-4 cells and PHA-stimulated PBMCs.
    Figure Legend Snippet: Anti-HIV-1 (X4) activity of CXCR4 compounds evaluated in CD4-positive MT-4 cells and PHA-stimulated PBMCs.

    Techniques Used: Activity Assay



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    Tocris compounds tc14012
    (A), (B) and (C): Inhibition of the CXCL12/CXCR4 interaction by (A) the peptide analogs T22, T140, <t>TC14012</t> and CTCE-9908 and the small molecules (B) AMD3100, AMD3465, AMD11070, IT1t and (C) WZ811, Me6TREN and gambogic acid. Jurkat cells were incubated with 2.9 nM CXCL12 AF647 in the presence of different concentrations of compound. Data are represented as % inhibition of maximal CXCL12 binding to CXCR4. Mean ± SEM of three or four independent experiments is shown.
    Compounds Tc14012, supplied by Tocris, used in various techniques. Bioz Stars score: 92/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/result/compounds tc14012/product/Tocris
    Average 92 stars, based on 1 article reviews
    compounds tc14012 - by Bioz Stars, 2026-05
    92/100 stars
      Buy from Supplier

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    (A), (B) and (C): Inhibition of the CXCL12/CXCR4 interaction by (A) the peptide analogs T22, T140, TC14012 and CTCE-9908 and the small molecules (B) AMD3100, AMD3465, AMD11070, IT1t and (C) WZ811, Me6TREN and gambogic acid. Jurkat cells were incubated with 2.9 nM CXCL12 AF647 in the presence of different concentrations of compound. Data are represented as % inhibition of maximal CXCL12 binding to CXCR4. Mean ± SEM of three or four independent experiments is shown.

    Journal: PLoS ONE

    Article Title: Comparison of cell-based assays for the identification and evaluation of competitive CXCR4 inhibitors

    doi: 10.1371/journal.pone.0176057

    Figure Lengend Snippet: (A), (B) and (C): Inhibition of the CXCL12/CXCR4 interaction by (A) the peptide analogs T22, T140, TC14012 and CTCE-9908 and the small molecules (B) AMD3100, AMD3465, AMD11070, IT1t and (C) WZ811, Me6TREN and gambogic acid. Jurkat cells were incubated with 2.9 nM CXCL12 AF647 in the presence of different concentrations of compound. Data are represented as % inhibition of maximal CXCL12 binding to CXCR4. Mean ± SEM of three or four independent experiments is shown.

    Article Snippet: The compounds TC14012 (MW: 2,066.4 g/mol) [ ], CTCE-9908 (MW: 1,927.3 g/mol) [ ], IT1t (MW: 479.6 g/mol) [ ] and AMD3465 Hexahydrobromide (MW: 896.1 g/mol) [ ] were obtained from Tocris (Bristol, UK).

    Techniques: Inhibition, Incubation, Binding Assay

    Fluo-2 AM loaded cells were treated with serial dilutions of compound and subsequently stimulated with 6.25 nM CXCL12. Fluorescence changes were measured over time in all wells simultaneously. (A): The inhibitory effect of different concentrations of AMD11070 on CXCL12-induced calcium release is shown. The red and blue line represent the negative (untreated, without CXCL12 stimulation) and positive (untreated, CXCL12 stimulation) control, respectively. Calcium fluxes are represented as % of baseline ( i . e . mean relative light units in each well during a fixed time interval before CXCL12 addition). One representative experiment out of three is shown with each data point corresponding to the mean fluorescence of three to six replicates. (B), (C) and (D): Inhibitory effect of (B) T22, T140, TC14012, CTCE-9908, (C) AMD3100, AMD3465, AMD11070, IT1t, (D) WZ811, Me6TREN and gambogic acid on CXCL12-induced calcium flux. Data are represented as % inhibition of CXCL12-induced calcium mobilization relative to the positive and negative control. Mean ± SEM of three independent experiments is shown.

    Journal: PLoS ONE

    Article Title: Comparison of cell-based assays for the identification and evaluation of competitive CXCR4 inhibitors

    doi: 10.1371/journal.pone.0176057

    Figure Lengend Snippet: Fluo-2 AM loaded cells were treated with serial dilutions of compound and subsequently stimulated with 6.25 nM CXCL12. Fluorescence changes were measured over time in all wells simultaneously. (A): The inhibitory effect of different concentrations of AMD11070 on CXCL12-induced calcium release is shown. The red and blue line represent the negative (untreated, without CXCL12 stimulation) and positive (untreated, CXCL12 stimulation) control, respectively. Calcium fluxes are represented as % of baseline ( i . e . mean relative light units in each well during a fixed time interval before CXCL12 addition). One representative experiment out of three is shown with each data point corresponding to the mean fluorescence of three to six replicates. (B), (C) and (D): Inhibitory effect of (B) T22, T140, TC14012, CTCE-9908, (C) AMD3100, AMD3465, AMD11070, IT1t, (D) WZ811, Me6TREN and gambogic acid on CXCL12-induced calcium flux. Data are represented as % inhibition of CXCL12-induced calcium mobilization relative to the positive and negative control. Mean ± SEM of three independent experiments is shown.

    Article Snippet: The compounds TC14012 (MW: 2,066.4 g/mol) [ ], CTCE-9908 (MW: 1,927.3 g/mol) [ ], IT1t (MW: 479.6 g/mol) [ ] and AMD3465 Hexahydrobromide (MW: 896.1 g/mol) [ ] were obtained from Tocris (Bristol, UK).

    Techniques: Fluorescence, Control, Inhibition, Negative Control

    SUP-T1 cells were stained with a mAb targeting the N-terminus of CXCR4 (clone 1D9) and then treated with different concentrations of compound. CXCR4 internalization was induced by stimulating samples with CXCL12 at 37°C and quantified by flow cytometry. (A): Flow cytometric analysis of the negative (untreated, no CXCL12 stimulation; red histogram) and positive (untreated, CXCL12 stimulation; dark blue histogram) control and TC14012-treated samples (50 nM to 0.5 nM; light blue, green and orange histogram, respectively). (B), (C) and (D): Inhibitory effect of (B) T22, T140, TC14012, CTCE-9908, (C) AMD3100, AMD3465, AMD11070, IT1t, (D) WZ811, Me6TREN and gambogic acid on CXCR4 endocytosis. Data are represented as % of CXCR4 internalization relative to the positive and negative control. Mean ± SEM of at least two independent experiments is shown.

    Journal: PLoS ONE

    Article Title: Comparison of cell-based assays for the identification and evaluation of competitive CXCR4 inhibitors

    doi: 10.1371/journal.pone.0176057

    Figure Lengend Snippet: SUP-T1 cells were stained with a mAb targeting the N-terminus of CXCR4 (clone 1D9) and then treated with different concentrations of compound. CXCR4 internalization was induced by stimulating samples with CXCL12 at 37°C and quantified by flow cytometry. (A): Flow cytometric analysis of the negative (untreated, no CXCL12 stimulation; red histogram) and positive (untreated, CXCL12 stimulation; dark blue histogram) control and TC14012-treated samples (50 nM to 0.5 nM; light blue, green and orange histogram, respectively). (B), (C) and (D): Inhibitory effect of (B) T22, T140, TC14012, CTCE-9908, (C) AMD3100, AMD3465, AMD11070, IT1t, (D) WZ811, Me6TREN and gambogic acid on CXCR4 endocytosis. Data are represented as % of CXCR4 internalization relative to the positive and negative control. Mean ± SEM of at least two independent experiments is shown.

    Article Snippet: The compounds TC14012 (MW: 2,066.4 g/mol) [ ], CTCE-9908 (MW: 1,927.3 g/mol) [ ], IT1t (MW: 479.6 g/mol) [ ] and AMD3465 Hexahydrobromide (MW: 896.1 g/mol) [ ] were obtained from Tocris (Bristol, UK).

    Techniques: Staining, Flow Cytometry, Control, Negative Control

    (A), (B) and (C): Effect of (A) T22, T140, TC14012, CTCE-9908, (B) AMD3100, AMD3465, AMD11070, IT1t, (C) WZ811, Me6TREN and gambogic acid on chemotaxis of CXCR4-positive Jurkat cells. After compound treatment, cells were allowed to migrate towards 6.25 nM CXCL12, present in the lower compartment of the insert, for two hours. The migrated cells were counted by flow cytometry. Data are represented as % inhibition of migration relative to the negative and positive control (spontaneously migrated cells and cells migrated towards CXCL12, respectively). ± SEM of two to three independent experiments, each performed in triplicate.

    Journal: PLoS ONE

    Article Title: Comparison of cell-based assays for the identification and evaluation of competitive CXCR4 inhibitors

    doi: 10.1371/journal.pone.0176057

    Figure Lengend Snippet: (A), (B) and (C): Effect of (A) T22, T140, TC14012, CTCE-9908, (B) AMD3100, AMD3465, AMD11070, IT1t, (C) WZ811, Me6TREN and gambogic acid on chemotaxis of CXCR4-positive Jurkat cells. After compound treatment, cells were allowed to migrate towards 6.25 nM CXCL12, present in the lower compartment of the insert, for two hours. The migrated cells were counted by flow cytometry. Data are represented as % inhibition of migration relative to the negative and positive control (spontaneously migrated cells and cells migrated towards CXCL12, respectively). ± SEM of two to three independent experiments, each performed in triplicate.

    Article Snippet: The compounds TC14012 (MW: 2,066.4 g/mol) [ ], CTCE-9908 (MW: 1,927.3 g/mol) [ ], IT1t (MW: 479.6 g/mol) [ ] and AMD3465 Hexahydrobromide (MW: 896.1 g/mol) [ ] were obtained from Tocris (Bristol, UK).

    Techniques: Chemotaxis Assay, Flow Cytometry, Inhibition, Migration, Positive Control

    Anti-HIV-1 (X4) activity of CXCR4 compounds evaluated in CD4-positive MT-4 cells and PHA-stimulated PBMCs.

    Journal: PLoS ONE

    Article Title: Comparison of cell-based assays for the identification and evaluation of competitive CXCR4 inhibitors

    doi: 10.1371/journal.pone.0176057

    Figure Lengend Snippet: Anti-HIV-1 (X4) activity of CXCR4 compounds evaluated in CD4-positive MT-4 cells and PHA-stimulated PBMCs.

    Article Snippet: The compounds TC14012 (MW: 2,066.4 g/mol) [ ], CTCE-9908 (MW: 1,927.3 g/mol) [ ], IT1t (MW: 479.6 g/mol) [ ] and AMD3465 Hexahydrobromide (MW: 896.1 g/mol) [ ] were obtained from Tocris (Bristol, UK).

    Techniques: Activity Assay