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    MedChemExpress mac13243
    <t>MAC13243</t> makes E . coli more susceptible to some large-scaffold antibiotics. ( a ) E . coli MC4100 cells were exposed to 10 μM MAC13234, or large-scaffold antibiotics (½ MIC), or both. Cells were grown in LB for 18 h at 37 °C and cell growth was determined by measuring the optical density (OD 600 ). MICs were determined to be 512 μg mL −1 for vancomycin, 16 μg mL −1 for rifampicin, 256 μg mL −1 for erythromycin and 64 μg mL −1 for novobiocin. ( b ) MAC13243 functions synergistically with some large-scaffold antibiotics. Heat plots showing growth inhibition of E . coli MC4100 in the presence of MAC13243 and vancomycin, rifampicin, erythromycin or novobiocin (in M9 media). Percentage of growth is illustrated with different colours where black represents 100% growth and red 0% growth. These data were used to calculate FICIs (see text for details). MICs were determined to be 256 μg mL −1 for MAC13243, 128 μg mL −1 for vancomycin, 8 μg mL −1 for rifampicin, 256 μg mL −1 for erythromycin and 1024 μg mL −1 for novobiocin.
    Mac13243, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 88/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    MAC13243 makes E . coli more susceptible to some large-scaffold antibiotics. ( a ) E . coli MC4100 cells were exposed to 10 μM MAC13234, or large-scaffold antibiotics (½ MIC), or both. Cells were grown in LB for 18 h at 37 °C and cell growth was determined by measuring the optical density (OD 600 ). MICs were determined to be 512 μg mL −1 for vancomycin, 16 μg mL −1 for rifampicin, 256 μg mL −1 for erythromycin and 64 μg mL −1 for novobiocin. ( b ) MAC13243 functions synergistically with some large-scaffold antibiotics. Heat plots showing growth inhibition of E . coli MC4100 in the presence of MAC13243 and vancomycin, rifampicin, erythromycin or novobiocin (in M9 media). Percentage of growth is illustrated with different colours where black represents 100% growth and red 0% growth. These data were used to calculate FICIs (see text for details). MICs were determined to be 256 μg mL −1 for MAC13243, 128 μg mL −1 for vancomycin, 8 μg mL −1 for rifampicin, 256 μg mL −1 for erythromycin and 1024 μg mL −1 for novobiocin.

    Journal: Scientific Reports

    Article Title: Increasing the permeability of Escherichia coli using MAC13243

    doi: 10.1038/s41598-017-17772-6

    Figure Lengend Snippet: MAC13243 makes E . coli more susceptible to some large-scaffold antibiotics. ( a ) E . coli MC4100 cells were exposed to 10 μM MAC13234, or large-scaffold antibiotics (½ MIC), or both. Cells were grown in LB for 18 h at 37 °C and cell growth was determined by measuring the optical density (OD 600 ). MICs were determined to be 512 μg mL −1 for vancomycin, 16 μg mL −1 for rifampicin, 256 μg mL −1 for erythromycin and 64 μg mL −1 for novobiocin. ( b ) MAC13243 functions synergistically with some large-scaffold antibiotics. Heat plots showing growth inhibition of E . coli MC4100 in the presence of MAC13243 and vancomycin, rifampicin, erythromycin or novobiocin (in M9 media). Percentage of growth is illustrated with different colours where black represents 100% growth and red 0% growth. These data were used to calculate FICIs (see text for details). MICs were determined to be 256 μg mL −1 for MAC13243, 128 μg mL −1 for vancomycin, 8 μg mL −1 for rifampicin, 256 μg mL −1 for erythromycin and 1024 μg mL −1 for novobiocin.

    Article Snippet: Antibiotics and other chemical compounds were purchased from the following manufacturers: Vancomycin, rifampicin, erythromycin, novobiocin and 1-(N-phenylamino)naphthalene (NPN) from Sigma Aldrich (Stockholm, Sweden); MAC13243 from MedChem Express (Stockholm, Sweden); 5-Floxuridine and Streptozotocin from Cayman Chemical (Michigan, USA); Carbadox from Alfa Aesar (Karlsruhe, Germany) and anhydrotetracycline (aTc) from VWR (Stockholm, Sweden).

    Techniques: Inhibition

    MAC13243 is degraded in solution. ( a ) MAC13243 is hydrolysed into one molecule of 3,4-dimethoxyphenethylamine, two molecules of formaldehyde and one molecule of S- (4-chlorobenzyl)isothiourea. At neutral pH the t 1/ 2 is 13 h. Both MAC13243 and the degradation product S- (4-chlorobenzyl)isothiourea bind to LolA 21 , 51 . ( b ) An analogue of the degradation product, called A22 or S- (4-dichlorobenzyl)isothiourea, also binds LolA. Curiously this compound is a known inhibitor of the cytoskeletal protein MreB 51 . Figure adapted from 51 , with permission from the publisher.

    Journal: Scientific Reports

    Article Title: Increasing the permeability of Escherichia coli using MAC13243

    doi: 10.1038/s41598-017-17772-6

    Figure Lengend Snippet: MAC13243 is degraded in solution. ( a ) MAC13243 is hydrolysed into one molecule of 3,4-dimethoxyphenethylamine, two molecules of formaldehyde and one molecule of S- (4-chlorobenzyl)isothiourea. At neutral pH the t 1/ 2 is 13 h. Both MAC13243 and the degradation product S- (4-chlorobenzyl)isothiourea bind to LolA 21 , 51 . ( b ) An analogue of the degradation product, called A22 or S- (4-dichlorobenzyl)isothiourea, also binds LolA. Curiously this compound is a known inhibitor of the cytoskeletal protein MreB 51 . Figure adapted from 51 , with permission from the publisher.

    Article Snippet: Antibiotics and other chemical compounds were purchased from the following manufacturers: Vancomycin, rifampicin, erythromycin, novobiocin and 1-(N-phenylamino)naphthalene (NPN) from Sigma Aldrich (Stockholm, Sweden); MAC13243 from MedChem Express (Stockholm, Sweden); 5-Floxuridine and Streptozotocin from Cayman Chemical (Michigan, USA); Carbadox from Alfa Aesar (Karlsruhe, Germany) and anhydrotetracycline (aTc) from VWR (Stockholm, Sweden).

    Techniques:

    A sub-lethal concentration of MAC13243 makes the outer membrane of E . coli more permeable. ( a ) The NPN dye can be used to monitor the integrity of the outer membrane. NPN is excluded from WT cells but penetrates into cells with a compromised outer membrane where it binds to the phospholipid layer, resulting in prominent fluorescence. ( b ) E . coli MC4100 grown in M9 media were exposed to different small molecules (½ MIC), and the permeability of the outer membrane was assessed by measuring the fluorescence of NPN. MICs were determined to be 1 μg mL −1 for carbadox, 256 μg mL −1 for streptozotocin, 0.002 μg mL −1 for floxuridine and 256 μg mL −1 for MAC13243. Fluorescence values were compared to cells treated with a solvent control. Note that we did not test all small molecules in the NPN uptake assay, but focussed on those that were readily available and that were representative of a class. For example, floxuridine ( 9 ) was deemed to be representative of the nucleoside analogues ( 7 , 8 ). ( c ) E . coli MC4100 were grown in M9 media then exposed to different concentrations of MAC13234 (MIC = 256 μg mL −1 ) and NPN uptake was monitored (left panel). The increase in fluorescence was deemed to be due to increased permeability of the outer membrane, not cell lysis, since the amount of MAC13243 used did not affect cell viability (right panel). In these experiments cell aliquots were harvested after the NPN uptake assays, 10-fold serially diluted and spotted on LB agar. All data (mean ± SD) are from four experiments. ****p

    Journal: Scientific Reports

    Article Title: Increasing the permeability of Escherichia coli using MAC13243

    doi: 10.1038/s41598-017-17772-6

    Figure Lengend Snippet: A sub-lethal concentration of MAC13243 makes the outer membrane of E . coli more permeable. ( a ) The NPN dye can be used to monitor the integrity of the outer membrane. NPN is excluded from WT cells but penetrates into cells with a compromised outer membrane where it binds to the phospholipid layer, resulting in prominent fluorescence. ( b ) E . coli MC4100 grown in M9 media were exposed to different small molecules (½ MIC), and the permeability of the outer membrane was assessed by measuring the fluorescence of NPN. MICs were determined to be 1 μg mL −1 for carbadox, 256 μg mL −1 for streptozotocin, 0.002 μg mL −1 for floxuridine and 256 μg mL −1 for MAC13243. Fluorescence values were compared to cells treated with a solvent control. Note that we did not test all small molecules in the NPN uptake assay, but focussed on those that were readily available and that were representative of a class. For example, floxuridine ( 9 ) was deemed to be representative of the nucleoside analogues ( 7 , 8 ). ( c ) E . coli MC4100 were grown in M9 media then exposed to different concentrations of MAC13234 (MIC = 256 μg mL −1 ) and NPN uptake was monitored (left panel). The increase in fluorescence was deemed to be due to increased permeability of the outer membrane, not cell lysis, since the amount of MAC13243 used did not affect cell viability (right panel). In these experiments cell aliquots were harvested after the NPN uptake assays, 10-fold serially diluted and spotted on LB agar. All data (mean ± SD) are from four experiments. ****p

    Article Snippet: Antibiotics and other chemical compounds were purchased from the following manufacturers: Vancomycin, rifampicin, erythromycin, novobiocin and 1-(N-phenylamino)naphthalene (NPN) from Sigma Aldrich (Stockholm, Sweden); MAC13243 from MedChem Express (Stockholm, Sweden); 5-Floxuridine and Streptozotocin from Cayman Chemical (Michigan, USA); Carbadox from Alfa Aesar (Karlsruhe, Germany) and anhydrotetracycline (aTc) from VWR (Stockholm, Sweden).

    Techniques: Concentration Assay, Fluorescence, Permeability, Lysis

    A model depicting how MAC13243 could affect the permeability of the outer membrane in E . coli . Lipoprotein precursors are synthesised on cytosolic ribosomes, then trafficked to the periplasm through either the Sec or Tat translocons. In the periplasm the N-terminal cysteine residue is acylated and then cleaved in successive reactions by Lgt, LspA and Lnt (not shown). Left panel, the mature lipoprotein is bound by the ABC transporter complex LolCDE then released to the periplasmic chaperone LolA. The LolA-lipoprotein complex is trafficked to the outer membrane where it binds to the LolB receptor and transfers the lipoprotein cargo. LolB then inserts the lipoprotein into the outer membrane. Note that some lipoproteins have a Lol avoidance signal and they are retained in the inner membrane. See 13 for more details. Right panel, a sub-lethal concentration of MAC13243 (step 1) results in partial inhibition of LolA (step 2). This results in the partial retention of outer membrane lipoproteins at the inner membrane (step 3). Some of these mis-targeted lipoproteins are directly involved in outer membrane biogenesis, such as LolB (insertion of lipoproteins 13 ), BamB (insertion of ß-barrel proteins 1 ) and LptE (insertion of LPS molecules 52 ). Thus partial depletion of LolA can directly affect the biogenesis of the key components of the outer membrane, which weakens the membrane and results in increased permeability (step 4). The increased permeability in cells treated with MAC13243 can be exploited to increase the uptake of NPN and large-scaffold antibiotics (step 5).

    Journal: Scientific Reports

    Article Title: Increasing the permeability of Escherichia coli using MAC13243

    doi: 10.1038/s41598-017-17772-6

    Figure Lengend Snippet: A model depicting how MAC13243 could affect the permeability of the outer membrane in E . coli . Lipoprotein precursors are synthesised on cytosolic ribosomes, then trafficked to the periplasm through either the Sec or Tat translocons. In the periplasm the N-terminal cysteine residue is acylated and then cleaved in successive reactions by Lgt, LspA and Lnt (not shown). Left panel, the mature lipoprotein is bound by the ABC transporter complex LolCDE then released to the periplasmic chaperone LolA. The LolA-lipoprotein complex is trafficked to the outer membrane where it binds to the LolB receptor and transfers the lipoprotein cargo. LolB then inserts the lipoprotein into the outer membrane. Note that some lipoproteins have a Lol avoidance signal and they are retained in the inner membrane. See 13 for more details. Right panel, a sub-lethal concentration of MAC13243 (step 1) results in partial inhibition of LolA (step 2). This results in the partial retention of outer membrane lipoproteins at the inner membrane (step 3). Some of these mis-targeted lipoproteins are directly involved in outer membrane biogenesis, such as LolB (insertion of lipoproteins 13 ), BamB (insertion of ß-barrel proteins 1 ) and LptE (insertion of LPS molecules 52 ). Thus partial depletion of LolA can directly affect the biogenesis of the key components of the outer membrane, which weakens the membrane and results in increased permeability (step 4). The increased permeability in cells treated with MAC13243 can be exploited to increase the uptake of NPN and large-scaffold antibiotics (step 5).

    Article Snippet: Antibiotics and other chemical compounds were purchased from the following manufacturers: Vancomycin, rifampicin, erythromycin, novobiocin and 1-(N-phenylamino)naphthalene (NPN) from Sigma Aldrich (Stockholm, Sweden); MAC13243 from MedChem Express (Stockholm, Sweden); 5-Floxuridine and Streptozotocin from Cayman Chemical (Michigan, USA); Carbadox from Alfa Aesar (Karlsruhe, Germany) and anhydrotetracycline (aTc) from VWR (Stockholm, Sweden).

    Techniques: Permeability, Concentration Assay, Inhibition