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mek5 inhibitors gw284543  (MedChemExpress)


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    MedChemExpress mek5 inhibitors gw284543
    <t>MEK5/ERK5</t> positively regulates the transcriptional activity of endogenous HH/GLI in melanoma cells. ( A ) Cells transduced with lentiviral vectors carrying control non-targeting shRNA (shNT) or human ERK5-specific shRNA (shERK5-1/shERK5-2) were transfected with pCS2 + MT (-) or pCS2 + MT-GLI1 and GLI-BS for 12 hours. Relative luciferase activity (RLU) was firefly/Renilla ratios normalized for control ± SD (n = 3). ( B ) Cells transfected as above were treated with vehicle (0) or XMD8-92 for 24 hours. RLU was firefly/Renilla ratios normalized for control ± SD (n = 3). ( C ) Cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA, lysed after 48 hours, and Western Blot was performed on total (Whole), cytoplasmic (Cyt) or nuclear (Nuc) extracts with the indicated antibodies. Graph shows quantification of nuclear GLI1. ( D ) HeLa cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA for 24 hours. Immunofluorescence analysis was performed by staining for HA (HA-MEK5DD, green) and GLI1 (red). Confocal images were analysed to quantify GLI1 nuclear staining, represented in the graph as nuclear Pearson’ Coefficient ± SD ( n = 3). ( E ) Cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA and with a GLI-BS for 12 h. RLU was firefly/Renilla ratios normalized for control ± SD ( n = 3). ( F ) Cells transfected as above were lysed after 48 h and GLI1, MEF2C and MEF2D mRNA levels were determined by Q-PCR. Data are presented as means ± SD ( n = 3)
    Mek5 Inhibitors Gw284543, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 94/100, based on 3 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    mek5 inhibitors gw284543 - by Bioz Stars, 2026-02
    94/100 stars

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    1) Product Images from "The MEK5/ERK5 pathway promotes the activation of the Hedgehog/GLI signaling in melanoma cells"

    Article Title: The MEK5/ERK5 pathway promotes the activation of the Hedgehog/GLI signaling in melanoma cells

    Journal: Cellular Oncology (Dordrecht, Netherlands)

    doi: 10.1007/s13402-025-01050-z

    MEK5/ERK5 positively regulates the transcriptional activity of endogenous HH/GLI in melanoma cells. ( A ) Cells transduced with lentiviral vectors carrying control non-targeting shRNA (shNT) or human ERK5-specific shRNA (shERK5-1/shERK5-2) were transfected with pCS2 + MT (-) or pCS2 + MT-GLI1 and GLI-BS for 12 hours. Relative luciferase activity (RLU) was firefly/Renilla ratios normalized for control ± SD (n = 3). ( B ) Cells transfected as above were treated with vehicle (0) or XMD8-92 for 24 hours. RLU was firefly/Renilla ratios normalized for control ± SD (n = 3). ( C ) Cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA, lysed after 48 hours, and Western Blot was performed on total (Whole), cytoplasmic (Cyt) or nuclear (Nuc) extracts with the indicated antibodies. Graph shows quantification of nuclear GLI1. ( D ) HeLa cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA for 24 hours. Immunofluorescence analysis was performed by staining for HA (HA-MEK5DD, green) and GLI1 (red). Confocal images were analysed to quantify GLI1 nuclear staining, represented in the graph as nuclear Pearson’ Coefficient ± SD ( n = 3). ( E ) Cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA and with a GLI-BS for 12 h. RLU was firefly/Renilla ratios normalized for control ± SD ( n = 3). ( F ) Cells transfected as above were lysed after 48 h and GLI1, MEF2C and MEF2D mRNA levels were determined by Q-PCR. Data are presented as means ± SD ( n = 3)
    Figure Legend Snippet: MEK5/ERK5 positively regulates the transcriptional activity of endogenous HH/GLI in melanoma cells. ( A ) Cells transduced with lentiviral vectors carrying control non-targeting shRNA (shNT) or human ERK5-specific shRNA (shERK5-1/shERK5-2) were transfected with pCS2 + MT (-) or pCS2 + MT-GLI1 and GLI-BS for 12 hours. Relative luciferase activity (RLU) was firefly/Renilla ratios normalized for control ± SD (n = 3). ( B ) Cells transfected as above were treated with vehicle (0) or XMD8-92 for 24 hours. RLU was firefly/Renilla ratios normalized for control ± SD (n = 3). ( C ) Cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA, lysed after 48 hours, and Western Blot was performed on total (Whole), cytoplasmic (Cyt) or nuclear (Nuc) extracts with the indicated antibodies. Graph shows quantification of nuclear GLI1. ( D ) HeLa cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA for 24 hours. Immunofluorescence analysis was performed by staining for HA (HA-MEK5DD, green) and GLI1 (red). Confocal images were analysed to quantify GLI1 nuclear staining, represented in the graph as nuclear Pearson’ Coefficient ± SD ( n = 3). ( E ) Cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA and with a GLI-BS for 12 h. RLU was firefly/Renilla ratios normalized for control ± SD ( n = 3). ( F ) Cells transfected as above were lysed after 48 h and GLI1, MEF2C and MEF2D mRNA levels were determined by Q-PCR. Data are presented as means ± SD ( n = 3)

    Techniques Used: Activity Assay, Transduction, Control, shRNA, Transfection, Luciferase, Western Blot, Immunofluorescence, Staining

    Combined targeting of MEK5 and GLI synergistically reduces the volume of melanoma spheroids. ( A - B ) A375 ( A ) and SSM2c ( B ) spheroids were treated with DMSO (-), GANT-61, GW284543 or BIX02189 or with the combinations at the indicated concentrations. Graphs show the quantification of spheroid volume after 5 days normalized for the time point 0. Data represent mean ± SD from three independent experiments. Representative images of spheroids taken at day 5 are shown. § Bliss independence score (> 0) indicates synergistic effects over single treatments. Bliss score = 0.027 (GANT + GW284543 ) or 0.008 (GANT + BIX02189) in A375 cells; Bliss score = 0.291 (GANT + GW284543 ) or 0.327 (GANT + BIX02189) in SSM2c cells
    Figure Legend Snippet: Combined targeting of MEK5 and GLI synergistically reduces the volume of melanoma spheroids. ( A - B ) A375 ( A ) and SSM2c ( B ) spheroids were treated with DMSO (-), GANT-61, GW284543 or BIX02189 or with the combinations at the indicated concentrations. Graphs show the quantification of spheroid volume after 5 days normalized for the time point 0. Data represent mean ± SD from three independent experiments. Representative images of spheroids taken at day 5 are shown. § Bliss independence score (> 0) indicates synergistic effects over single treatments. Bliss score = 0.027 (GANT + GW284543 ) or 0.008 (GANT + BIX02189) in A375 cells; Bliss score = 0.291 (GANT + GW284543 ) or 0.327 (GANT + BIX02189) in SSM2c cells

    Techniques Used:



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    <t>MEK5/ERK5</t> positively regulates the transcriptional activity of endogenous HH/GLI in melanoma cells. ( A ) Cells transduced with lentiviral vectors carrying control non-targeting shRNA (shNT) or human ERK5-specific shRNA (shERK5-1/shERK5-2) were transfected with pCS2 + MT (-) or pCS2 + MT-GLI1 and GLI-BS for 12 hours. Relative luciferase activity (RLU) was firefly/Renilla ratios normalized for control ± SD (n = 3). ( B ) Cells transfected as above were treated with vehicle (0) or XMD8-92 for 24 hours. RLU was firefly/Renilla ratios normalized for control ± SD (n = 3). ( C ) Cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA, lysed after 48 hours, and Western Blot was performed on total (Whole), cytoplasmic (Cyt) or nuclear (Nuc) extracts with the indicated antibodies. Graph shows quantification of nuclear GLI1. ( D ) HeLa cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA for 24 hours. Immunofluorescence analysis was performed by staining for HA (HA-MEK5DD, green) and GLI1 (red). Confocal images were analysed to quantify GLI1 nuclear staining, represented in the graph as nuclear Pearson’ Coefficient ± SD ( n = 3). ( E ) Cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA and with a GLI-BS for 12 h. RLU was firefly/Renilla ratios normalized for control ± SD ( n = 3). ( F ) Cells transfected as above were lysed after 48 h and GLI1, MEF2C and MEF2D mRNA levels were determined by Q-PCR. Data are presented as means ± SD ( n = 3)
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    <t>MEK5/ERK5</t> positively regulates the transcriptional activity of endogenous HH/GLI in melanoma cells. ( A ) Cells transduced with lentiviral vectors carrying control non-targeting shRNA (shNT) or human ERK5-specific shRNA (shERK5-1/shERK5-2) were transfected with pCS2 + MT (-) or pCS2 + MT-GLI1 and GLI-BS for 12 hours. Relative luciferase activity (RLU) was firefly/Renilla ratios normalized for control ± SD (n = 3). ( B ) Cells transfected as above were treated with vehicle (0) or XMD8-92 for 24 hours. RLU was firefly/Renilla ratios normalized for control ± SD (n = 3). ( C ) Cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA, lysed after 48 hours, and Western Blot was performed on total (Whole), cytoplasmic (Cyt) or nuclear (Nuc) extracts with the indicated antibodies. Graph shows quantification of nuclear GLI1. ( D ) HeLa cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA for 24 hours. Immunofluorescence analysis was performed by staining for HA (HA-MEK5DD, green) and GLI1 (red). Confocal images were analysed to quantify GLI1 nuclear staining, represented in the graph as nuclear Pearson’ Coefficient ± SD ( n = 3). ( E ) Cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA and with a GLI-BS for 12 h. RLU was firefly/Renilla ratios normalized for control ± SD ( n = 3). ( F ) Cells transfected as above were lysed after 48 h and GLI1, MEF2C and MEF2D mRNA levels were determined by Q-PCR. Data are presented as means ± SD ( n = 3)
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    Image Search Results


    MEK5/ERK5 positively regulates the transcriptional activity of endogenous HH/GLI in melanoma cells. ( A ) Cells transduced with lentiviral vectors carrying control non-targeting shRNA (shNT) or human ERK5-specific shRNA (shERK5-1/shERK5-2) were transfected with pCS2 + MT (-) or pCS2 + MT-GLI1 and GLI-BS for 12 hours. Relative luciferase activity (RLU) was firefly/Renilla ratios normalized for control ± SD (n = 3). ( B ) Cells transfected as above were treated with vehicle (0) or XMD8-92 for 24 hours. RLU was firefly/Renilla ratios normalized for control ± SD (n = 3). ( C ) Cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA, lysed after 48 hours, and Western Blot was performed on total (Whole), cytoplasmic (Cyt) or nuclear (Nuc) extracts with the indicated antibodies. Graph shows quantification of nuclear GLI1. ( D ) HeLa cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA for 24 hours. Immunofluorescence analysis was performed by staining for HA (HA-MEK5DD, green) and GLI1 (red). Confocal images were analysed to quantify GLI1 nuclear staining, represented in the graph as nuclear Pearson’ Coefficient ± SD ( n = 3). ( E ) Cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA and with a GLI-BS for 12 h. RLU was firefly/Renilla ratios normalized for control ± SD ( n = 3). ( F ) Cells transfected as above were lysed after 48 h and GLI1, MEF2C and MEF2D mRNA levels were determined by Q-PCR. Data are presented as means ± SD ( n = 3)

    Journal: Cellular Oncology (Dordrecht, Netherlands)

    Article Title: The MEK5/ERK5 pathway promotes the activation of the Hedgehog/GLI signaling in melanoma cells

    doi: 10.1007/s13402-025-01050-z

    Figure Lengend Snippet: MEK5/ERK5 positively regulates the transcriptional activity of endogenous HH/GLI in melanoma cells. ( A ) Cells transduced with lentiviral vectors carrying control non-targeting shRNA (shNT) or human ERK5-specific shRNA (shERK5-1/shERK5-2) were transfected with pCS2 + MT (-) or pCS2 + MT-GLI1 and GLI-BS for 12 hours. Relative luciferase activity (RLU) was firefly/Renilla ratios normalized for control ± SD (n = 3). ( B ) Cells transfected as above were treated with vehicle (0) or XMD8-92 for 24 hours. RLU was firefly/Renilla ratios normalized for control ± SD (n = 3). ( C ) Cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA, lysed after 48 hours, and Western Blot was performed on total (Whole), cytoplasmic (Cyt) or nuclear (Nuc) extracts with the indicated antibodies. Graph shows quantification of nuclear GLI1. ( D ) HeLa cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA for 24 hours. Immunofluorescence analysis was performed by staining for HA (HA-MEK5DD, green) and GLI1 (red). Confocal images were analysed to quantify GLI1 nuclear staining, represented in the graph as nuclear Pearson’ Coefficient ± SD ( n = 3). ( E ) Cells were transfected with pcDNA3.1 (control) or pCMV5-MEK5DD-HA and with a GLI-BS for 12 h. RLU was firefly/Renilla ratios normalized for control ± SD ( n = 3). ( F ) Cells transfected as above were lysed after 48 h and GLI1, MEF2C and MEF2D mRNA levels were determined by Q-PCR. Data are presented as means ± SD ( n = 3)

    Article Snippet: ERK5 inhibitors JWG-071 [ ], AX15836 [ ] and XMD8-92 [ ], MEK5 inhibitors GW284543 [ ] and BIX02189 [ ] (MedChemExpress LLC, Princeton, NJ, U.S.A.), the GLI1/2 inhibitor GANT61 [ ] and the SMO agonist SAG [ ] (Sigma-Aldrich, St Louis, MO, U.S.A. and MedChemExpress LLC, Princeton, NJ, U.S.A.) were dissolved in DMSO.

    Techniques: Activity Assay, Transduction, Control, shRNA, Transfection, Luciferase, Western Blot, Immunofluorescence, Staining

    Combined targeting of MEK5 and GLI synergistically reduces the volume of melanoma spheroids. ( A - B ) A375 ( A ) and SSM2c ( B ) spheroids were treated with DMSO (-), GANT-61, GW284543 or BIX02189 or with the combinations at the indicated concentrations. Graphs show the quantification of spheroid volume after 5 days normalized for the time point 0. Data represent mean ± SD from three independent experiments. Representative images of spheroids taken at day 5 are shown. § Bliss independence score (> 0) indicates synergistic effects over single treatments. Bliss score = 0.027 (GANT + GW284543 ) or 0.008 (GANT + BIX02189) in A375 cells; Bliss score = 0.291 (GANT + GW284543 ) or 0.327 (GANT + BIX02189) in SSM2c cells

    Journal: Cellular Oncology (Dordrecht, Netherlands)

    Article Title: The MEK5/ERK5 pathway promotes the activation of the Hedgehog/GLI signaling in melanoma cells

    doi: 10.1007/s13402-025-01050-z

    Figure Lengend Snippet: Combined targeting of MEK5 and GLI synergistically reduces the volume of melanoma spheroids. ( A - B ) A375 ( A ) and SSM2c ( B ) spheroids were treated with DMSO (-), GANT-61, GW284543 or BIX02189 or with the combinations at the indicated concentrations. Graphs show the quantification of spheroid volume after 5 days normalized for the time point 0. Data represent mean ± SD from three independent experiments. Representative images of spheroids taken at day 5 are shown. § Bliss independence score (> 0) indicates synergistic effects over single treatments. Bliss score = 0.027 (GANT + GW284543 ) or 0.008 (GANT + BIX02189) in A375 cells; Bliss score = 0.291 (GANT + GW284543 ) or 0.327 (GANT + BIX02189) in SSM2c cells

    Article Snippet: ERK5 inhibitors JWG-071 [ ], AX15836 [ ] and XMD8-92 [ ], MEK5 inhibitors GW284543 [ ] and BIX02189 [ ] (MedChemExpress LLC, Princeton, NJ, U.S.A.), the GLI1/2 inhibitor GANT61 [ ] and the SMO agonist SAG [ ] (Sigma-Aldrich, St Louis, MO, U.S.A. and MedChemExpress LLC, Princeton, NJ, U.S.A.) were dissolved in DMSO.

    Techniques: