2-ethyl-3 Search Results


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  • 93
    Millipore 2 ethyl 3 methylpyrazine
    2 Ethyl 3 Methylpyrazine, supplied by Millipore, used in various techniques. Bioz Stars score: 93/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    99
    Millipore 2 ethyl 3
    2 Ethyl 3, supplied by Millipore, used in various techniques. Bioz Stars score: 99/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    85
    iThemba Pharmaceuticals (Pty) Ltd 2 ethyl 3 o
    Structure of 2-ME and ESE-16. (a)  shows the parent compound, (17 beta)-2-methoxyestra-1,3,5(10)-triene-3,17-diol (2-methoxyestradiol).  (b)  indicates the substitutions at position 2, 3 and 17 of 2-ethyl-3- O -sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16), a sulphamoylated 2-ME analogue [  33 ].
    2 Ethyl 3 O, supplied by iThemba Pharmaceuticals (Pty) Ltd, used in various techniques. Bioz Stars score: 85/100, based on 3 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    99
    Millipore 2 ethyl 3 5 dimethyl pyrazine
    Structure of 2-ME and ESE-16. (a)  shows the parent compound, (17 beta)-2-methoxyestra-1,3,5(10)-triene-3,17-diol (2-methoxyestradiol).  (b)  indicates the substitutions at position 2, 3 and 17 of 2-ethyl-3- O -sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16), a sulphamoylated 2-ME analogue [  33 ].
    2 Ethyl 3 5 Dimethyl Pyrazine, supplied by Millipore, used in various techniques. Bioz Stars score: 99/100, based on 2 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    94
    Millipore 2 ethyl 3 methyl pyrazine
    Structure of 2-ME and ESE-16. (a)  shows the parent compound, (17 beta)-2-methoxyestra-1,3,5(10)-triene-3,17-diol (2-methoxyestradiol).  (b)  indicates the substitutions at position 2, 3 and 17 of 2-ethyl-3- O -sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16), a sulphamoylated 2-ME analogue [  33 ].
    2 Ethyl 3 Methyl Pyrazine, supplied by Millipore, 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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    93
    Millipore 2 ethyl 3 5 and 6 dimethylpyrazine
    Structure of 2-ME and ESE-16. (a)  shows the parent compound, (17 beta)-2-methoxyestra-1,3,5(10)-triene-3,17-diol (2-methoxyestradiol).  (b)  indicates the substitutions at position 2, 3 and 17 of 2-ethyl-3- O -sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16), a sulphamoylated 2-ME analogue [  33 ].
    2 Ethyl 3 5 And 6 Dimethylpyrazine, supplied by Millipore, used in various techniques. Bioz Stars score: 93/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    85
    Roche b s 2 ethyl 3 isobutyl 9
    Structure of 2-ME and ESE-16. (a)  shows the parent compound, (17 beta)-2-methoxyestra-1,3,5(10)-triene-3,17-diol (2-methoxyestradiol).  (b)  indicates the substitutions at position 2, 3 and 17 of 2-ethyl-3- O -sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16), a sulphamoylated 2-ME analogue [  33 ].
    B S 2 Ethyl 3 Isobutyl 9, supplied by Roche, used in various techniques. Bioz Stars score: 85/100, based on 7 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    85
    Merck KGaA n 1 cyanomethyl amino carbonyl 2 ethyl 3 5 dimethylbenzyl
    Structure of 2-ME and ESE-16. (a)  shows the parent compound, (17 beta)-2-methoxyestra-1,3,5(10)-triene-3,17-diol (2-methoxyestradiol).  (b)  indicates the substitutions at position 2, 3 and 17 of 2-ethyl-3- O -sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16), a sulphamoylated 2-ME analogue [  33 ].
    N 1 Cyanomethyl Amino Carbonyl 2 Ethyl 3 5 Dimethylbenzyl, supplied by Merck KGaA, used in various techniques. Bioz Stars score: 85/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    93
    Millipore 2 ethyl 3 hydroxy 4 h pyran 4 one
    Structure of 2-ME and ESE-16. (a)  shows the parent compound, (17 beta)-2-methoxyestra-1,3,5(10)-triene-3,17-diol (2-methoxyestradiol).  (b)  indicates the substitutions at position 2, 3 and 17 of 2-ethyl-3- O -sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16), a sulphamoylated 2-ME analogue [  33 ].
    2 Ethyl 3 Hydroxy 4 H Pyran 4 One, supplied by Millipore, used in various techniques. Bioz Stars score: 93/100, based on 2 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    85
    Dalton Pharma 2 ethyl 3 lcb 4 e 3 4 isopropyl piperazin 1 yl propenyl benzyl
    Structure of 2-ME and ESE-16. (a)  shows the parent compound, (17 beta)-2-methoxyestra-1,3,5(10)-triene-3,17-diol (2-methoxyestradiol).  (b)  indicates the substitutions at position 2, 3 and 17 of 2-ethyl-3- O -sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16), a sulphamoylated 2-ME analogue [  33 ].
    2 Ethyl 3 Lcb 4 E 3 4 Isopropyl Piperazin 1 Yl Propenyl Benzyl, supplied by Dalton Pharma, used in various techniques. Bioz Stars score: 85/100, based on 3 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    91
    Takeda sarm 2f 4 2s 3 s 2 ethyl 3 hydroxy 5 oxopyrrolidin 1 yl 2 trifluoromethyl benzonitrile
    Structure of 2-ME and ESE-16. (a)  shows the parent compound, (17 beta)-2-methoxyestra-1,3,5(10)-triene-3,17-diol (2-methoxyestradiol).  (b)  indicates the substitutions at position 2, 3 and 17 of 2-ethyl-3- O -sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16), a sulphamoylated 2-ME analogue [  33 ].
    Sarm 2f 4 2s 3 S 2 Ethyl 3 Hydroxy 5 Oxopyrrolidin 1 Yl 2 Trifluoromethyl Benzonitrile, supplied by Takeda, used in various techniques. Bioz Stars score: 91/100, based on 2 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    91
    Dalton Pharma 2 ethyl 3 4 e 3 4 isopropyl piperazin 1 yl propenyl benzyl 5 7 dimethyl 3h imidazo 4 5 b pyridine
    Structure of 2-ME and ESE-16. (a)  shows the parent compound, (17 beta)-2-methoxyestra-1,3,5(10)-triene-3,17-diol (2-methoxyestradiol).  (b)  indicates the substitutions at position 2, 3 and 17 of 2-ethyl-3- O -sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16), a sulphamoylated 2-ME analogue [  33 ].
    2 Ethyl 3 4 E 3 4 Isopropyl Piperazin 1 Yl Propenyl Benzyl 5 7 Dimethyl 3h Imidazo 4 5 B Pyridine, supplied by Dalton Pharma, used in various techniques. Bioz Stars score: 91/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    2 ethyl 3 4 e 3 4 isopropyl piperazin 1 yl propenyl benzyl 5 7 dimethyl 3h imidazo 4 5 b pyridine - by Bioz Stars, 2020-08
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    91
    TCI Tokyo Chemical Industry mehp
    Structure of 2-ME and ESE-16. (a)  shows the parent compound, (17 beta)-2-methoxyestra-1,3,5(10)-triene-3,17-diol (2-methoxyestradiol).  (b)  indicates the substitutions at position 2, 3 and 17 of 2-ethyl-3- O -sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16), a sulphamoylated 2-ME analogue [  33 ].
    Mehp, supplied by TCI Tokyo Chemical Industry, used in various techniques. Bioz Stars score: 91/100, based on 19 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    91
    Millipore valnoctamide
    <t>Valnoctamide</t> reverses deficient brain growth induced by mCMV infection. A , Photograph shows decreased brain size in an infected, untreated mouse (i.e., mCMV; middle) compared with an uninfected control (left). VCD treatment restores normal brain growth (mCMV+VCD, right). Quantification of VCD-mediated benefits on postnatal brain growth by calculation of brain-to-body weight ratio. Values are reported as the mean ± SEM; n = 10 mice/group (3 litters). ns, Not significant. ** p
    Valnoctamide, supplied by Millipore, used in various techniques. Bioz Stars score: 91/100, based on 6 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    Enzo Biochem ebelactone b
    <t>Valnoctamide</t> reverses deficient brain growth induced by mCMV infection. A , Photograph shows decreased brain size in an infected, untreated mouse (i.e., mCMV; middle) compared with an uninfected control (left). VCD treatment restores normal brain growth (mCMV+VCD, right). Quantification of VCD-mediated benefits on postnatal brain growth by calculation of brain-to-body weight ratio. Values are reported as the mean ± SEM; n = 10 mice/group (3 litters). ns, Not significant. ** p
    Ebelactone B, supplied by Enzo Biochem, used in various techniques. Bioz Stars score: 91/100, based on 3 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    91
    FUJIFILM mehp
    <t>Valnoctamide</t> reverses deficient brain growth induced by mCMV infection. A , Photograph shows decreased brain size in an infected, untreated mouse (i.e., mCMV; middle) compared with an uninfected control (left). VCD treatment restores normal brain growth (mCMV+VCD, right). Quantification of VCD-mediated benefits on postnatal brain growth by calculation of brain-to-body weight ratio. Values are reported as the mean ± SEM; n = 10 mice/group (3 litters). ns, Not significant. ** p
    Mehp, supplied by FUJIFILM, used in various techniques. Bioz Stars score: 91/100, based on 41 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    Takeda sarm 2f 4 2s
    <t>Valnoctamide</t> reverses deficient brain growth induced by mCMV infection. A , Photograph shows decreased brain size in an infected, untreated mouse (i.e., mCMV; middle) compared with an uninfected control (left). VCD treatment restores normal brain growth (mCMV+VCD, right). Quantification of VCD-mediated benefits on postnatal brain growth by calculation of brain-to-body weight ratio. Values are reported as the mean ± SEM; n = 10 mice/group (3 litters). ns, Not significant. ** p
    Sarm 2f 4 2s, supplied by Takeda, used in various techniques. Bioz Stars score: 91/100, based on 2 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    86
    Millipore ro4 1284
    <t>Ro4-1284</t> pretreatment affords protection against long-lasting MDMA-induced tissue 5-HT depletions. 5-HT and 5-HIAA levels were measured from cortex (A, C) and striatum (B, D) 7 days after MDMA exposure by HPLC-CEAS. Ro4-1284 (10 mg/kg, ip) was
    Ro4 1284, supplied by Millipore, used in various techniques. Bioz Stars score: 86/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    99
    Millipore 16 doxylstearic acids
    <t>Ro4-1284</t> pretreatment affords protection against long-lasting MDMA-induced tissue 5-HT depletions. 5-HT and 5-HIAA levels were measured from cortex (A, C) and striatum (B, D) 7 days after MDMA exposure by HPLC-CEAS. Ro4-1284 (10 mg/kg, ip) was
    16 Doxylstearic Acids, supplied by Millipore, used in various techniques. Bioz Stars score: 99/100, based on 3 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    93
    iThemba Pharmaceuticals (Pty) Ltd silico designed 2me2 analog
    <t>Ro4-1284</t> pretreatment affords protection against long-lasting MDMA-induced tissue 5-HT depletions. 5-HT and 5-HIAA levels were measured from cortex (A, C) and striatum (B, D) 7 days after MDMA exposure by HPLC-CEAS. Ro4-1284 (10 mg/kg, ip) was
    Silico Designed 2me2 Analog, supplied by iThemba Pharmaceuticals (Pty) Ltd, used in various techniques. Bioz Stars score: 93/100, based on 21 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    88
    iThemba Pharmaceuticals (Pty) Ltd ese 16 compound
    Confocal microscopy images of the microtubule architecture of SNO cells with the use of anti-α tubulin antibodies and nuclear stain 4 ′, 6 - diamidino - 2 - phenylindole. (A) Cells propogated in medium only, (B) cells exposed to DMSO – vehicle control, (C) cells exposed to actinomycin D – positive control and (D) cells exposed to <t>ESE-16</t> at a concentration of 0.2 μM. The α-tubulin of the cells were stained green by a FITC-conjugate diluent while the nuclei were stained blue by DAPI to provide contrast to the green fluorescence. Cells propogated in medium and vehicle control cells showed normal microtubule architecture. The positive control showed a decrease in cell density and revealed shrunken cells. ESE-16-treated cells showed a decrease in cell density and abnormal spindle formation when compared to the appropriate controls. The abnormal spindle formation is indicative of metaphase block. Scale bar: 10 μm.
    Ese 16 Compound, supplied by iThemba Pharmaceuticals (Pty) Ltd, used in various techniques. Bioz Stars score: 88/100, based on 22 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    99
    Millipore 16 doxylstearic acid
    Confocal microscopy images of the microtubule architecture of SNO cells with the use of anti-α tubulin antibodies and nuclear stain 4 ′, 6 - diamidino - 2 - phenylindole. (A) Cells propogated in medium only, (B) cells exposed to DMSO – vehicle control, (C) cells exposed to actinomycin D – positive control and (D) cells exposed to <t>ESE-16</t> at a concentration of 0.2 μM. The α-tubulin of the cells were stained green by a FITC-conjugate diluent while the nuclei were stained blue by DAPI to provide contrast to the green fluorescence. Cells propogated in medium and vehicle control cells showed normal microtubule architecture. The positive control showed a decrease in cell density and revealed shrunken cells. ESE-16-treated cells showed a decrease in cell density and abnormal spindle formation when compared to the appropriate controls. The abnormal spindle formation is indicative of metaphase block. Scale bar: 10 μm.
    16 Doxylstearic Acid, supplied by Millipore, used in various techniques. Bioz Stars score: 99/100, based on 8 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    Millipore 16 doxylstearic acid spin probes
    Confocal microscopy images of the microtubule architecture of SNO cells with the use of anti-α tubulin antibodies and nuclear stain 4 ′, 6 - diamidino - 2 - phenylindole. (A) Cells propogated in medium only, (B) cells exposed to DMSO – vehicle control, (C) cells exposed to actinomycin D – positive control and (D) cells exposed to <t>ESE-16</t> at a concentration of 0.2 μM. The α-tubulin of the cells were stained green by a FITC-conjugate diluent while the nuclei were stained blue by DAPI to provide contrast to the green fluorescence. Cells propogated in medium and vehicle control cells showed normal microtubule architecture. The positive control showed a decrease in cell density and revealed shrunken cells. ESE-16-treated cells showed a decrease in cell density and abnormal spindle formation when compared to the appropriate controls. The abnormal spindle formation is indicative of metaphase block. Scale bar: 10 μm.
    16 Doxylstearic Acid Spin Probes, supplied by Millipore, used in various techniques. Bioz Stars score: 99/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    85
    Kyowa Hakko Kirin resorcinol analog kw 2478
    Confocal microscopy images of the microtubule architecture of SNO cells with the use of anti-α tubulin antibodies and nuclear stain 4 ′, 6 - diamidino - 2 - phenylindole. (A) Cells propogated in medium only, (B) cells exposed to DMSO – vehicle control, (C) cells exposed to actinomycin D – positive control and (D) cells exposed to <t>ESE-16</t> at a concentration of 0.2 μM. The α-tubulin of the cells were stained green by a FITC-conjugate diluent while the nuclei were stained blue by DAPI to provide contrast to the green fluorescence. Cells propogated in medium and vehicle control cells showed normal microtubule architecture. The positive control showed a decrease in cell density and revealed shrunken cells. ESE-16-treated cells showed a decrease in cell density and abnormal spindle formation when compared to the appropriate controls. The abnormal spindle formation is indicative of metaphase block. Scale bar: 10 μm.
    Resorcinol Analog Kw 2478, supplied by Kyowa Hakko Kirin, used in various techniques. Bioz Stars score: 85/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    Image Search Results


    Structure of 2-ME and ESE-16. (a)  shows the parent compound, (17 beta)-2-methoxyestra-1,3,5(10)-triene-3,17-diol (2-methoxyestradiol).  (b)  indicates the substitutions at position 2, 3 and 17 of 2-ethyl-3- O -sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16), a sulphamoylated 2-ME analogue [  33 ].

    Journal: Cancer Cell International

    Article Title: Molecular crosstalk between apoptosis and autophagy induced by a novel 2-methoxyestradiol analogue in cervical adenocarcinoma cells

    doi: 10.1186/1475-2867-13-87

    Figure Lengend Snippet: Structure of 2-ME and ESE-16. (a) shows the parent compound, (17 beta)-2-methoxyestra-1,3,5(10)-triene-3,17-diol (2-methoxyestradiol). (b) indicates the substitutions at position 2, 3 and 17 of 2-ethyl-3- O -sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16), a sulphamoylated 2-ME analogue [ 33 ].

    Article Snippet: Chemical compound and appropriate controls The non-commercially available 2-ethyl-3-O -sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16) was synthesized by iThemba (PTY) Ltd. Pharmaceuticals (Modderfontein, Gauteng, South Africa).

    Techniques:

    Valnoctamide reverses deficient brain growth induced by mCMV infection. A , Photograph shows decreased brain size in an infected, untreated mouse (i.e., mCMV; middle) compared with an uninfected control (left). VCD treatment restores normal brain growth (mCMV+VCD, right). Quantification of VCD-mediated benefits on postnatal brain growth by calculation of brain-to-body weight ratio. Values are reported as the mean ± SEM; n = 10 mice/group (3 litters). ns, Not significant. ** p

    Journal: The Journal of Neuroscience

    Article Title: Valnoctamide Inhibits Cytomegalovirus Infection in Developing Brain and Attenuates Neurobehavioral Dysfunctions and Brain Abnormalities

    doi: 10.1523/JNEUROSCI.0970-17.2017

    Figure Lengend Snippet: Valnoctamide reverses deficient brain growth induced by mCMV infection. A , Photograph shows decreased brain size in an infected, untreated mouse (i.e., mCMV; middle) compared with an uninfected control (left). VCD treatment restores normal brain growth (mCMV+VCD, right). Quantification of VCD-mediated benefits on postnatal brain growth by calculation of brain-to-body weight ratio. Values are reported as the mean ± SEM; n = 10 mice/group (3 litters). ns, Not significant. ** p

    Article Snippet: Valnoctamide (catalog #V4765) was purchased from Sigma-Aldrich as powder and was dissolved in dimethylsulfoxide (DMSO) to yield a 1 m stock solution.

    Techniques: Infection, Mouse Assay

    Valnoctamide suppresses mCMV load in the brain of mice infected intraperitoneally on the day of birth. Newborn mice were infected at P0 with 750 pfu of mCMV intraperitoneally and were randomized to receive either vehicle (mCMV+VEH) or VCD (mCMV+VCD) subcutaneously from P1 until P21. A–E , Viral load was quantified in the cerebrum ( A ), cerebellum ( B ), whole blood ( C ), liver ( D ), and spleen ( E ) by qRT-PCR at the specified time points and were expressed as log 10 genome copies per gram/ml harvested tissue/blood. Data are presented as the mean ± SEM; n = 7–10 mice/time point. Viral titers below the limit of detection (LoD, dotted line) were plotted as 2 log 10 genome copies. ns, Not significant. * p

    Journal: The Journal of Neuroscience

    Article Title: Valnoctamide Inhibits Cytomegalovirus Infection in Developing Brain and Attenuates Neurobehavioral Dysfunctions and Brain Abnormalities

    doi: 10.1523/JNEUROSCI.0970-17.2017

    Figure Lengend Snippet: Valnoctamide suppresses mCMV load in the brain of mice infected intraperitoneally on the day of birth. Newborn mice were infected at P0 with 750 pfu of mCMV intraperitoneally and were randomized to receive either vehicle (mCMV+VEH) or VCD (mCMV+VCD) subcutaneously from P1 until P21. A–E , Viral load was quantified in the cerebrum ( A ), cerebellum ( B ), whole blood ( C ), liver ( D ), and spleen ( E ) by qRT-PCR at the specified time points and were expressed as log 10 genome copies per gram/ml harvested tissue/blood. Data are presented as the mean ± SEM; n = 7–10 mice/time point. Viral titers below the limit of detection (LoD, dotted line) were plotted as 2 log 10 genome copies. ns, Not significant. * p

    Article Snippet: Valnoctamide (catalog #V4765) was purchased from Sigma-Aldrich as powder and was dissolved in dimethylsulfoxide (DMSO) to yield a 1 m stock solution.

    Techniques: Mouse Assay, Infection, Quantitative RT-PCR

    Subcutaneously injected valnoctamide enters the brain and suppresses mCMV replication within the brain. Quantification of mCMV load in the brain of mice intracranially infected with 2 × 10 4 pfu of mCMV on day 3 after birth. The amount of virus in the cerebrum (left) and the cerebellum (right) was calculated by qRT-PCR in P9 mice receiving either vehicle (VEH) or VCD subcutaneously from P3 through P8 and expressed as genome copies per gram of harvested tissue. Values are reported as the mean ± SEM; n = 8 mice/time-point. ** p

    Journal: The Journal of Neuroscience

    Article Title: Valnoctamide Inhibits Cytomegalovirus Infection in Developing Brain and Attenuates Neurobehavioral Dysfunctions and Brain Abnormalities

    doi: 10.1523/JNEUROSCI.0970-17.2017

    Figure Lengend Snippet: Subcutaneously injected valnoctamide enters the brain and suppresses mCMV replication within the brain. Quantification of mCMV load in the brain of mice intracranially infected with 2 × 10 4 pfu of mCMV on day 3 after birth. The amount of virus in the cerebrum (left) and the cerebellum (right) was calculated by qRT-PCR in P9 mice receiving either vehicle (VEH) or VCD subcutaneously from P3 through P8 and expressed as genome copies per gram of harvested tissue. Values are reported as the mean ± SEM; n = 8 mice/time-point. ** p

    Article Snippet: Valnoctamide (catalog #V4765) was purchased from Sigma-Aldrich as powder and was dissolved in dimethylsulfoxide (DMSO) to yield a 1 m stock solution.

    Techniques: Injection, Mouse Assay, Infection, Quantitative RT-PCR

    Impaired cerebellar-mediated motor functions in mCMV-infected mice are ameliorated by valnoctamide treatment. A , Photographs display stereotypical clasping response with hindlimbs retracted to the abdomen in an mCMV-infected mouse (middle), and a normal response with splayed out hindlimbs in an uninfected control (left) and in an mCMV-infected, VCD-treated animal (right). B , Scoring of clasping response according to hindlimb position. C , Increased T LA in infected, untreated mice in the vertical pole test, compared with VCD-treated infected animals and uninfected controls. D , E , Investigation of fine motor coordination and balance by challenging beam traversal test. Infected mice need more time to traverse the beam ( D ) and slip more ( E ) than the control mice. Both aspects are improved by VCD administration. Values are reported as the mean ± SEM; n = 10–13 mice/group. * p

    Journal: The Journal of Neuroscience

    Article Title: Valnoctamide Inhibits Cytomegalovirus Infection in Developing Brain and Attenuates Neurobehavioral Dysfunctions and Brain Abnormalities

    doi: 10.1523/JNEUROSCI.0970-17.2017

    Figure Lengend Snippet: Impaired cerebellar-mediated motor functions in mCMV-infected mice are ameliorated by valnoctamide treatment. A , Photographs display stereotypical clasping response with hindlimbs retracted to the abdomen in an mCMV-infected mouse (middle), and a normal response with splayed out hindlimbs in an uninfected control (left) and in an mCMV-infected, VCD-treated animal (right). B , Scoring of clasping response according to hindlimb position. C , Increased T LA in infected, untreated mice in the vertical pole test, compared with VCD-treated infected animals and uninfected controls. D , E , Investigation of fine motor coordination and balance by challenging beam traversal test. Infected mice need more time to traverse the beam ( D ) and slip more ( E ) than the control mice. Both aspects are improved by VCD administration. Values are reported as the mean ± SEM; n = 10–13 mice/group. * p

    Article Snippet: Valnoctamide (catalog #V4765) was purchased from Sigma-Aldrich as powder and was dissolved in dimethylsulfoxide (DMSO) to yield a 1 m stock solution.

    Techniques: Infection, Mouse Assay

    Delayed acquisition of neurological milestones induced by mCMV infection is completely rescued by valnoctamide therapy. A–H , Graphs show neurodevelopmental delays in mCMV-infected pups (solid gray triangles) as assessed by the righting reflex ( A ), the cliff aversion ( B ), the forelimb grasping and placing reflex ( C , D ), the negative geotaxis ( E ), the level screen test ( F ), the screen climbing test ( G ), and the vibrissa placing reflex ( H ; for a detailed description, see Materials and Methods). VCD-treated animals (solid green triangles) showed neurological responses similar to uninfected controls receiving either vehicle (VEH; empty gray circles) or VCD (empty green circles). Values are reported as the mean ± SEM, n = 20–24 mice (9–12 males)/experimental group. ns, Not significant. * p

    Journal: The Journal of Neuroscience

    Article Title: Valnoctamide Inhibits Cytomegalovirus Infection in Developing Brain and Attenuates Neurobehavioral Dysfunctions and Brain Abnormalities

    doi: 10.1523/JNEUROSCI.0970-17.2017

    Figure Lengend Snippet: Delayed acquisition of neurological milestones induced by mCMV infection is completely rescued by valnoctamide therapy. A–H , Graphs show neurodevelopmental delays in mCMV-infected pups (solid gray triangles) as assessed by the righting reflex ( A ), the cliff aversion ( B ), the forelimb grasping and placing reflex ( C , D ), the negative geotaxis ( E ), the level screen test ( F ), the screen climbing test ( G ), and the vibrissa placing reflex ( H ; for a detailed description, see Materials and Methods). VCD-treated animals (solid green triangles) showed neurological responses similar to uninfected controls receiving either vehicle (VEH; empty gray circles) or VCD (empty green circles). Values are reported as the mean ± SEM, n = 20–24 mice (9–12 males)/experimental group. ns, Not significant. * p

    Article Snippet: Valnoctamide (catalog #V4765) was purchased from Sigma-Aldrich as powder and was dissolved in dimethylsulfoxide (DMSO) to yield a 1 m stock solution.

    Techniques: Infection, Mouse Assay

    Valnoctamide substantially ameliorates cerebellar development in mCMV-infected mice. A , Photomicrograph of representative fluorescent Nissl-stained cerebellar areas in control (left) and infected mice with (right, mCMV+VCD) or without (middle, mCMV) VCD. Note the delayed foliation in infected, untreated cerebellum, rescued by VCD. Scale bar, 200 μm. B , Graph depicts cerebellar area, expressed as a percentage of total brain area (three sagittal sections/animal, five animals/group). C , Photomicrograph showing cerebellar PCs and ML by means of calbindin D-28K staining. Infected, untreated cerebellum (middle) displays loss of PCs and thinner ML compared with uninfected control (left); VCD improves both parameters (right). Scale bar, 200 μm. D–F , Quantification of PC number ( D ), and ML ( E ) and IGL thickness ( F ) along 500 μm of the primary fissure (prf; both sides; three sagittal sections/mouse, five mice/group). G , Fluorescent micrograph of heterotopic PCs (arrowheads) identified in an infected untreated cerebellum. Scale bar, 100 μm. H , Photomicrograph displays pathological persistence of EGL in mCMV-infected, untreated cerebellum at P30 (middle); no EGL could be identified at the same time point in uninfected control (left) and infected, VCD-treated cerebellum (right). Scale bar, 200 μm. Values are reported as the mean ± SEM. ns, Not significant. * p

    Journal: The Journal of Neuroscience

    Article Title: Valnoctamide Inhibits Cytomegalovirus Infection in Developing Brain and Attenuates Neurobehavioral Dysfunctions and Brain Abnormalities

    doi: 10.1523/JNEUROSCI.0970-17.2017

    Figure Lengend Snippet: Valnoctamide substantially ameliorates cerebellar development in mCMV-infected mice. A , Photomicrograph of representative fluorescent Nissl-stained cerebellar areas in control (left) and infected mice with (right, mCMV+VCD) or without (middle, mCMV) VCD. Note the delayed foliation in infected, untreated cerebellum, rescued by VCD. Scale bar, 200 μm. B , Graph depicts cerebellar area, expressed as a percentage of total brain area (three sagittal sections/animal, five animals/group). C , Photomicrograph showing cerebellar PCs and ML by means of calbindin D-28K staining. Infected, untreated cerebellum (middle) displays loss of PCs and thinner ML compared with uninfected control (left); VCD improves both parameters (right). Scale bar, 200 μm. D–F , Quantification of PC number ( D ), and ML ( E ) and IGL thickness ( F ) along 500 μm of the primary fissure (prf; both sides; three sagittal sections/mouse, five mice/group). G , Fluorescent micrograph of heterotopic PCs (arrowheads) identified in an infected untreated cerebellum. Scale bar, 100 μm. H , Photomicrograph displays pathological persistence of EGL in mCMV-infected, untreated cerebellum at P30 (middle); no EGL could be identified at the same time point in uninfected control (left) and infected, VCD-treated cerebellum (right). Scale bar, 200 μm. Values are reported as the mean ± SEM. ns, Not significant. * p

    Article Snippet: Valnoctamide (catalog #V4765) was purchased from Sigma-Aldrich as powder and was dissolved in dimethylsulfoxide (DMSO) to yield a 1 m stock solution.

    Techniques: Infection, Mouse Assay, Staining

    Ro4-1284 pretreatment affords protection against long-lasting MDMA-induced tissue 5-HT depletions. 5-HT and 5-HIAA levels were measured from cortex (A, C) and striatum (B, D) 7 days after MDMA exposure by HPLC-CEAS. Ro4-1284 (10 mg/kg, ip) was

    Journal: Toxicological Sciences

    Article Title: Vesicular Monoamine Transporter 2 and the Acute and Long-Term Response to 3,4-(±)-Methylenedioxymethamphetamine

    doi: 10.1093/toxsci/kfu222

    Figure Lengend Snippet: Ro4-1284 pretreatment affords protection against long-lasting MDMA-induced tissue 5-HT depletions. 5-HT and 5-HIAA levels were measured from cortex (A, C) and striatum (B, D) 7 days after MDMA exposure by HPLC-CEAS. Ro4-1284 (10 mg/kg, ip) was

    Article Snippet: The VMAT2 inhibitor, Ro4-1284 (2-hydroxy-2-ethyl-3-isobutyl-9,10-dimethoxy-1,2,3,4,5,6,7-hexahydrobenzo[a]chinolizine), was also purchased from Sigma-Aldrich.

    Techniques: High Performance Liquid Chromatography

    Acute effects of Ro4-1284 on striatal indoleamine and catecholamine content. Concentrations of 5-HT, DA, and corresponding metabolites, 5HIAA and DOPAC were assessed in rat striatum 1 and 12 h following Ro4-1284 (10 mg/kg, ip) treatment

    Journal: Toxicological Sciences

    Article Title: Vesicular Monoamine Transporter 2 and the Acute and Long-Term Response to 3,4-(±)-Methylenedioxymethamphetamine

    doi: 10.1093/toxsci/kfu222

    Figure Lengend Snippet: Acute effects of Ro4-1284 on striatal indoleamine and catecholamine content. Concentrations of 5-HT, DA, and corresponding metabolites, 5HIAA and DOPAC were assessed in rat striatum 1 and 12 h following Ro4-1284 (10 mg/kg, ip) treatment

    Article Snippet: The VMAT2 inhibitor, Ro4-1284 (2-hydroxy-2-ethyl-3-isobutyl-9,10-dimethoxy-1,2,3,4,5,6,7-hexahydrobenzo[a]chinolizine), was also purchased from Sigma-Aldrich.

    Techniques:

    Ro4-1284 pretreatment attenuates horizontal velocity and vertical activity in MDMA-treated rats. Locomotor activity was monitored by placing animals into open-field activity chambers. Baseline levels of locomotor activity were measured for 30 min,

    Journal: Toxicological Sciences

    Article Title: Vesicular Monoamine Transporter 2 and the Acute and Long-Term Response to 3,4-(±)-Methylenedioxymethamphetamine

    doi: 10.1093/toxsci/kfu222

    Figure Lengend Snippet: Ro4-1284 pretreatment attenuates horizontal velocity and vertical activity in MDMA-treated rats. Locomotor activity was monitored by placing animals into open-field activity chambers. Baseline levels of locomotor activity were measured for 30 min,

    Article Snippet: The VMAT2 inhibitor, Ro4-1284 (2-hydroxy-2-ethyl-3-isobutyl-9,10-dimethoxy-1,2,3,4,5,6,7-hexahydrobenzo[a]chinolizine), was also purchased from Sigma-Aldrich.

    Techniques: Activity Assay

    MDMA-mediated hyperthermia is absent in Ro4-1284-treated rats. Temperature probes implanted into the peritoneal cavity of Sprague-Dawley rats recorded core body temperature. Animals were given Ro4-1284 (10 mg/kg, ip) 1 h prior to MDMA

    Journal: Toxicological Sciences

    Article Title: Vesicular Monoamine Transporter 2 and the Acute and Long-Term Response to 3,4-(±)-Methylenedioxymethamphetamine

    doi: 10.1093/toxsci/kfu222

    Figure Lengend Snippet: MDMA-mediated hyperthermia is absent in Ro4-1284-treated rats. Temperature probes implanted into the peritoneal cavity of Sprague-Dawley rats recorded core body temperature. Animals were given Ro4-1284 (10 mg/kg, ip) 1 h prior to MDMA

    Article Snippet: The VMAT2 inhibitor, Ro4-1284 (2-hydroxy-2-ethyl-3-isobutyl-9,10-dimethoxy-1,2,3,4,5,6,7-hexahydrobenzo[a]chinolizine), was also purchased from Sigma-Aldrich.

    Techniques:

    Long-term effects of Ro4-1284 and MDMA on striatal catecholamine content. DA and DOPAC concentrations were measured from striatum 7 days after MDMA exposure by HPLC-CEAS. Ro4-1284 (10 mg/kg, ip) was administered 1 h prior to MDMA treatment

    Journal: Toxicological Sciences

    Article Title: Vesicular Monoamine Transporter 2 and the Acute and Long-Term Response to 3,4-(±)-Methylenedioxymethamphetamine

    doi: 10.1093/toxsci/kfu222

    Figure Lengend Snippet: Long-term effects of Ro4-1284 and MDMA on striatal catecholamine content. DA and DOPAC concentrations were measured from striatum 7 days after MDMA exposure by HPLC-CEAS. Ro4-1284 (10 mg/kg, ip) was administered 1 h prior to MDMA treatment

    Article Snippet: The VMAT2 inhibitor, Ro4-1284 (2-hydroxy-2-ethyl-3-isobutyl-9,10-dimethoxy-1,2,3,4,5,6,7-hexahydrobenzo[a]chinolizine), was also purchased from Sigma-Aldrich.

    Techniques: High Performance Liquid Chromatography

    Loss of striatal serotonergic nerve-terminal density following MDMA dosing is prevented with Ro4-1284 treatment. Representative images of rat striatum were captured by light microscopy. Coronal sections were stained for SERT in animals treated with saline,

    Journal: Toxicological Sciences

    Article Title: Vesicular Monoamine Transporter 2 and the Acute and Long-Term Response to 3,4-(±)-Methylenedioxymethamphetamine

    doi: 10.1093/toxsci/kfu222

    Figure Lengend Snippet: Loss of striatal serotonergic nerve-terminal density following MDMA dosing is prevented with Ro4-1284 treatment. Representative images of rat striatum were captured by light microscopy. Coronal sections were stained for SERT in animals treated with saline,

    Article Snippet: The VMAT2 inhibitor, Ro4-1284 (2-hydroxy-2-ethyl-3-isobutyl-9,10-dimethoxy-1,2,3,4,5,6,7-hexahydrobenzo[a]chinolizine), was also purchased from Sigma-Aldrich.

    Techniques: Light Microscopy, Staining

    Confocal microscopy images of the microtubule architecture of SNO cells with the use of anti-α tubulin antibodies and nuclear stain 4 ′, 6 - diamidino - 2 - phenylindole. (A) Cells propogated in medium only, (B) cells exposed to DMSO – vehicle control, (C) cells exposed to actinomycin D – positive control and (D) cells exposed to ESE-16 at a concentration of 0.2 μM. The α-tubulin of the cells were stained green by a FITC-conjugate diluent while the nuclei were stained blue by DAPI to provide contrast to the green fluorescence. Cells propogated in medium and vehicle control cells showed normal microtubule architecture. The positive control showed a decrease in cell density and revealed shrunken cells. ESE-16-treated cells showed a decrease in cell density and abnormal spindle formation when compared to the appropriate controls. The abnormal spindle formation is indicative of metaphase block. Scale bar: 10 μm.

    Journal: Cell & Bioscience

    Article Title: Induction of the intrinsic apoptotic pathway via a new antimitotic agent in an esophageal carcinoma cell line

    doi: 10.1186/2045-3701-4-68

    Figure Lengend Snippet: Confocal microscopy images of the microtubule architecture of SNO cells with the use of anti-α tubulin antibodies and nuclear stain 4 ′, 6 - diamidino - 2 - phenylindole. (A) Cells propogated in medium only, (B) cells exposed to DMSO – vehicle control, (C) cells exposed to actinomycin D – positive control and (D) cells exposed to ESE-16 at a concentration of 0.2 μM. The α-tubulin of the cells were stained green by a FITC-conjugate diluent while the nuclei were stained blue by DAPI to provide contrast to the green fluorescence. Cells propogated in medium and vehicle control cells showed normal microtubule architecture. The positive control showed a decrease in cell density and revealed shrunken cells. ESE-16-treated cells showed a decrease in cell density and abnormal spindle formation when compared to the appropriate controls. The abnormal spindle formation is indicative of metaphase block. Scale bar: 10 μm.

    Article Snippet: The ESE-16 compound was synthesized by iThemba Pharmaceuticals (Pty) Ltd (Modderfontein, Gauteng, SA).

    Techniques: Confocal Microscopy, Staining, Positive Control, Concentration Assay, Fluorescence, Blocking Assay

    Haematoxylin and eosin staining images revealing morphological changes in the nuclear and cytoplasmic components in SNO cells. (A) Cells propogated in medium only, (B) cells exposed to dimethyl sulphoxide (DMSO) – vehicle control, (C) cells exposed to actinomycin D – positive control and (D) cells exposed to ESE-16 at a concentration of 0.2 μM. Cells propogated in medium and the vehicle-treated cells showed normal cell morphology, with the majority of the cells being in interphase. The positive control for apoptosis and the ESE-16 treated cells showed a decrease in cell density and morphological characteristics of apoptosis such as membrane blebbing and apoptotic bodies. The ESE-16 treated cells also showed an increase in the number of round cells with hypercondensed chromatin indicative of a metaphase block (Magnification: ×20).

    Journal: Cell & Bioscience

    Article Title: Induction of the intrinsic apoptotic pathway via a new antimitotic agent in an esophageal carcinoma cell line

    doi: 10.1186/2045-3701-4-68

    Figure Lengend Snippet: Haematoxylin and eosin staining images revealing morphological changes in the nuclear and cytoplasmic components in SNO cells. (A) Cells propogated in medium only, (B) cells exposed to dimethyl sulphoxide (DMSO) – vehicle control, (C) cells exposed to actinomycin D – positive control and (D) cells exposed to ESE-16 at a concentration of 0.2 μM. Cells propogated in medium and the vehicle-treated cells showed normal cell morphology, with the majority of the cells being in interphase. The positive control for apoptosis and the ESE-16 treated cells showed a decrease in cell density and morphological characteristics of apoptosis such as membrane blebbing and apoptotic bodies. The ESE-16 treated cells also showed an increase in the number of round cells with hypercondensed chromatin indicative of a metaphase block (Magnification: ×20).

    Article Snippet: The ESE-16 compound was synthesized by iThemba Pharmaceuticals (Pty) Ltd (Modderfontein, Gauteng, SA).

    Techniques: Staining, Positive Control, Concentration Assay, Blocking Assay

    Bar graph illustrating the ratio to medium of the effector caspase 3 levels in SNO cells exposed to ESE - 16 and various controls. Results revealed a statistically significant increase ( P -value of 0.004) * in caspase 3 activity in the ESE-16-treated cells when compared to the vehicle control. The ESE-16-treated cells had a ratio to medium value of 2.9772, while the vehicle control had a ratio to medium value of 1.0681.

    Journal: Cell & Bioscience

    Article Title: Induction of the intrinsic apoptotic pathway via a new antimitotic agent in an esophageal carcinoma cell line

    doi: 10.1186/2045-3701-4-68

    Figure Lengend Snippet: Bar graph illustrating the ratio to medium of the effector caspase 3 levels in SNO cells exposed to ESE - 16 and various controls. Results revealed a statistically significant increase ( P -value of 0.004) * in caspase 3 activity in the ESE-16-treated cells when compared to the vehicle control. The ESE-16-treated cells had a ratio to medium value of 2.9772, while the vehicle control had a ratio to medium value of 1.0681.

    Article Snippet: The ESE-16 compound was synthesized by iThemba Pharmaceuticals (Pty) Ltd (Modderfontein, Gauteng, SA).

    Techniques: Activity Assay

    Histograms illustrating superoxide levels in SNO cells after exposure to ESE - 16 and the appropriate controls of a representative repeat. (A) Cells propogated in medium only, (B) cells exposed to DMSO – vehicle control, (C) cells exposed to actinomycin D – positive control and (D) cells exposed to ESE-16 at a concentration of 0.2 μM. Viable cells represent the population of cells which showed little or no increase in fluorescence, thus no increase. The non-viable cells represent the population of cells with an increase in fluorescence thus indicating an increase in O 2 − production. The ESE-16-treated cells showed 38.17% of its population to be non-viable compared to the 21.45% non-viable population of the vehicle control.

    Journal: Cell & Bioscience

    Article Title: Induction of the intrinsic apoptotic pathway via a new antimitotic agent in an esophageal carcinoma cell line

    doi: 10.1186/2045-3701-4-68

    Figure Lengend Snippet: Histograms illustrating superoxide levels in SNO cells after exposure to ESE - 16 and the appropriate controls of a representative repeat. (A) Cells propogated in medium only, (B) cells exposed to DMSO – vehicle control, (C) cells exposed to actinomycin D – positive control and (D) cells exposed to ESE-16 at a concentration of 0.2 μM. Viable cells represent the population of cells which showed little or no increase in fluorescence, thus no increase. The non-viable cells represent the population of cells with an increase in fluorescence thus indicating an increase in O 2 − production. The ESE-16-treated cells showed 38.17% of its population to be non-viable compared to the 21.45% non-viable population of the vehicle control.

    Article Snippet: The ESE-16 compound was synthesized by iThemba Pharmaceuticals (Pty) Ltd (Modderfontein, Gauteng, SA).

    Techniques: Positive Control, Concentration Assay, Fluorescence

    Bar graph illustrating the ratio to medium of the initiator caspase 9 levels in SNO cells exposed to ESE - 16 and various controls. Results revealed a statistically insignificant increase ( P -value of 0.238) in caspase 9 activity in the ESE-16-treated cells when compared to the vehicle control. The ESE-16-treated cells had a ratio to medium value of 1.2188, while the vehicle control had a ratio to medium value of 1.0625.

    Journal: Cell & Bioscience

    Article Title: Induction of the intrinsic apoptotic pathway via a new antimitotic agent in an esophageal carcinoma cell line

    doi: 10.1186/2045-3701-4-68

    Figure Lengend Snippet: Bar graph illustrating the ratio to medium of the initiator caspase 9 levels in SNO cells exposed to ESE - 16 and various controls. Results revealed a statistically insignificant increase ( P -value of 0.238) in caspase 9 activity in the ESE-16-treated cells when compared to the vehicle control. The ESE-16-treated cells had a ratio to medium value of 1.2188, while the vehicle control had a ratio to medium value of 1.0625.

    Article Snippet: The ESE-16 compound was synthesized by iThemba Pharmaceuticals (Pty) Ltd (Modderfontein, Gauteng, SA).

    Techniques: Activity Assay

    Transmission electron microscopy images providing information on the internal ultrastructure of SNO cells propogated in medium only and SNO cells treated with DMSO. (A) Cells propogated in medium only, (B) cells exposed to DMSO – vehicle control, (C) cells exposed to actinomycin D – positive control and (D) cells exposed to ESE-16 at a concentration of 0.2 μM. Both the cells propogated in medium and the vehicle control cells showed microvilli protruding from their cell membrane surface. The nuclear membrane is smoothly outlined and well-preserved cytoplasmic organelles are visible. The positive control for apoptosis showed loss of microvilli, membrane blebbing and the presence of apoptotic bodies. ESE-16-treated cells revealed a decrease in nuclear membrane definition, membrane blebbling and apoptotic body formation. Scale bar: 5 μm.

    Journal: Cell & Bioscience

    Article Title: Induction of the intrinsic apoptotic pathway via a new antimitotic agent in an esophageal carcinoma cell line

    doi: 10.1186/2045-3701-4-68

    Figure Lengend Snippet: Transmission electron microscopy images providing information on the internal ultrastructure of SNO cells propogated in medium only and SNO cells treated with DMSO. (A) Cells propogated in medium only, (B) cells exposed to DMSO – vehicle control, (C) cells exposed to actinomycin D – positive control and (D) cells exposed to ESE-16 at a concentration of 0.2 μM. Both the cells propogated in medium and the vehicle control cells showed microvilli protruding from their cell membrane surface. The nuclear membrane is smoothly outlined and well-preserved cytoplasmic organelles are visible. The positive control for apoptosis showed loss of microvilli, membrane blebbing and the presence of apoptotic bodies. ESE-16-treated cells revealed a decrease in nuclear membrane definition, membrane blebbling and apoptotic body formation. Scale bar: 5 μm.

    Article Snippet: The ESE-16 compound was synthesized by iThemba Pharmaceuticals (Pty) Ltd (Modderfontein, Gauteng, SA).

    Techniques: Transmission Assay, Electron Microscopy, Positive Control, Concentration Assay

    Bar graph showing the average mean fluorescent intensity increase in the ESE - 16 - treated cells compared to the appropriate controls illustrating an increase in phosphatidylserine externalization. This bar graph represents the average MFI of all three repeats done. Cells propogated in medium had an average MFI of 11.31, the vehicle control had an average MFI of 15.74, the positive control had an average MFI of 18.82 while the ESE-16-treated cells an average MFI of 25.50. The increased MFI indicates an increase in PS externalization which is an early apoptotic indicator [ 35 ].

    Journal: Cell & Bioscience

    Article Title: Induction of the intrinsic apoptotic pathway via a new antimitotic agent in an esophageal carcinoma cell line

    doi: 10.1186/2045-3701-4-68

    Figure Lengend Snippet: Bar graph showing the average mean fluorescent intensity increase in the ESE - 16 - treated cells compared to the appropriate controls illustrating an increase in phosphatidylserine externalization. This bar graph represents the average MFI of all three repeats done. Cells propogated in medium had an average MFI of 11.31, the vehicle control had an average MFI of 15.74, the positive control had an average MFI of 18.82 while the ESE-16-treated cells an average MFI of 25.50. The increased MFI indicates an increase in PS externalization which is an early apoptotic indicator [ 35 ].

    Article Snippet: The ESE-16 compound was synthesized by iThemba Pharmaceuticals (Pty) Ltd (Modderfontein, Gauteng, SA).

    Techniques: Positive Control

    Structural comparison between (A) 2ME and (B) ESE-16. When the two chemical structures are compared, an exchange of a sulphamoylated group for a hydroxyl group at position 3 and the removal of a hydroxyl group at position 17 on the ESE-16 compound are noticed. The sulphamoylated group increases the bioavailability of the compound [ 8 , 13 , 20 , 28 , 29 ], while the modifications at position 3 and −17 increases the anticancer potency and provides a prolonged half-life [ 6 , 11 , 13 , 22 , 27 , 28 ].

    Journal: Cell & Bioscience

    Article Title: Induction of the intrinsic apoptotic pathway via a new antimitotic agent in an esophageal carcinoma cell line

    doi: 10.1186/2045-3701-4-68

    Figure Lengend Snippet: Structural comparison between (A) 2ME and (B) ESE-16. When the two chemical structures are compared, an exchange of a sulphamoylated group for a hydroxyl group at position 3 and the removal of a hydroxyl group at position 17 on the ESE-16 compound are noticed. The sulphamoylated group increases the bioavailability of the compound [ 8 , 13 , 20 , 28 , 29 ], while the modifications at position 3 and −17 increases the anticancer potency and provides a prolonged half-life [ 6 , 11 , 13 , 22 , 27 , 28 ].

    Article Snippet: The ESE-16 compound was synthesized by iThemba Pharmaceuticals (Pty) Ltd (Modderfontein, Gauteng, SA).

    Techniques:

    Bar graph showing the average mean fluorescent intensity increase in the ESE - 16 - treated cells compared to the appropriate controls , illustrating a decrease in mitochondrial membrane potential. This bar graph represents the average MFI of all three repeats done. The vehicle control had an average MFI of 28.79 while the postive control had an average MFI of 45.58 and the ESE-16-treated cells an average MFI of 37.995. The increase in the MFI seen in the ESE-16-treated cells is statistically significantly ( P -value of 0.019) * higher than that of the vehicle control indicating a decrease in ∆Ψm and possible mitochondrial membrane degradation.

    Journal: Cell & Bioscience

    Article Title: Induction of the intrinsic apoptotic pathway via a new antimitotic agent in an esophageal carcinoma cell line

    doi: 10.1186/2045-3701-4-68

    Figure Lengend Snippet: Bar graph showing the average mean fluorescent intensity increase in the ESE - 16 - treated cells compared to the appropriate controls , illustrating a decrease in mitochondrial membrane potential. This bar graph represents the average MFI of all three repeats done. The vehicle control had an average MFI of 28.79 while the postive control had an average MFI of 45.58 and the ESE-16-treated cells an average MFI of 37.995. The increase in the MFI seen in the ESE-16-treated cells is statistically significantly ( P -value of 0.019) * higher than that of the vehicle control indicating a decrease in ∆Ψm and possible mitochondrial membrane degradation.

    Article Snippet: The ESE-16 compound was synthesized by iThemba Pharmaceuticals (Pty) Ltd (Modderfontein, Gauteng, SA).

    Techniques: