Acetylgliotoxin
Acetylgliotoxin (Gliotoxin monoacetate) is a farnesyltransferase (FTase) inhibitor with an IC50 of 4.4 μM against human targets. Acetylgliotoxin inhibits the growth of fungal, bacterial, and viral pathogens; it binds to free protein thiols and induces ROS production. Acetylgliotoxin increases the survival rate of Caenorhabditis elegans infected with Candida albicans, but exhibits toxicity at higher concentrations. Acetylgliotoxin is applicable to research related to Candida albicans infections.
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- CAS No.: 146016-64-0
- Formule: C15H16N2O5S2
- Masse moléculaire:368.43
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.89 μM
Compound: 361
|
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
|
[PMID: 38181652] |
| HEK293 | IC50 |
4.49 μM
Compound: 361
|
Cytotoxicity against HEK293 cells assessed as cell growth inhibition
Cytotoxicity against HEK293 cells assessed as cell growth inhibition
|
[PMID: 38181652] |
| HepG2 | IC50 |
0.49 μM
Compound: 361
|
Cytotoxicity against human HepG2 cells assessed as reduction in cell growth incubated for 48 hrs by SRB assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell growth incubated for 48 hrs by SRB assay
|
[PMID: 38181652] |
| HepG2 | IC50 |
0.32 μM
Compound: 361
|
Cytotoxicity against human HepG2 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay
|
[PMID: 38181652] |
| MCF7 | IC50 |
0.22 μM
Compound: 361
|
Cytotoxicity against human MCF7 cells assessed as reduction in cell growth incubated for 48 hrs by SRB assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell growth incubated for 48 hrs by SRB assay
|
[PMID: 38181652] |
| NCI-H460 | IC50 |
0.32 μM
Compound: 361
|
Cytotoxicity against human NCI-H460 cells assessed as reduction in cell growth incubated for 48 hrs by SRB assay
Cytotoxicity against human NCI-H460 cells assessed as reduction in cell growth incubated for 48 hrs by SRB assay
|
[PMID: 38181652] |
| NCI-H460 | IC50 |
0.49 μM
Compound: 361
|
Cytotoxicity against human NCI-H460 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay
Cytotoxicity against human NCI-H460 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay
|
[PMID: 38181652] |
| RKO | IC50 |
1.24 μM
Compound: 361
|
Cytotoxicity against human RKO cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
Cytotoxicity against human RKO cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
|
[PMID: 38181652] |
| SF-268 | IC50 |
0.25 μM
Compound: 361
|
Cytotoxicity against human SF-268 cells assessed as reduction in cell growth incubated for 48 hrs by SRB assay
Cytotoxicity against human SF-268 cells assessed as reduction in cell growth incubated for 48 hrs by SRB assay
|
[PMID: 38181652] |
In Vitro
Acetylgliotoxin (AGT) (30 minutes) inhibits farnesyl-protein transferase from human monocyte THP-1 cells in its reduced dithiol form with an IC50 of 4.4 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 146016-64-0
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Masse moléculaire 368.43
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Formule C15H16N2O5S2
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SMILES
O=C1[C@@]23N(C([C@](N1C)(SS3)CO)=O)[C@@]4([H])C(C2)=CC=C[C@@H]4OC(C)=O
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Synonyms
Gliotoxin monoacetate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- Acetylgliotoxin
- 146016-64-0
- Gliotoxin monoacetate
- Farnesyl Transferase
- Fungal
- Bacterial
- Reactive Oxygen Species (ROS)
- human monocyte THP-1 cells
- reactive oxygen species
- farnesyl-protein transferase
- bacteria
- fungi
- Caenorhabditis elegans
- Candida albicans
- Caenorhabditis elegans glp-4;sek-1 mutants
- viruses
- Inhibitor
- inhibitor
- inhibit