Salinamide A
Salinamide A is a bacterial RNA polymerase inhibitor with IC50: 0.2 μM against Staphylococcus aureus; 0.2 μM against Escherichia coli. Salinamide A inhibits transcription initiation and elongation, as well as bacterial RNA and protein synthesis without affecting DNA synthesis. Salinamide A can be used in studies related to the N-terminal hinge conformation and function of the RNAP bridge helix, and bacterial infections.
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- CAS No.: 152340-22-2
- 화학식: C51H69N7O15
- 분자량:1020.13
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero E6 | MIC |
> 50 μg/mL
|
Growth-inhibitory activity against mammalian Vero E6 ATCC CRL1586 cells measured by broth microdilution assay with incubation for 16-48 hr at 37°C with 7% CO2 atmosphere.
Growth-inhibitory activity against mammalian Vero E6 ATCC CRL1586 cells measured by broth microdilution assay with incubation for 16-48 hr at 37°C with 7% CO2 atmosphere.
|
24843001 |
In Vitro
Salinamide A (1.56-50 μg/mL; 16-48 hr) inhibits the growth of Gram-positive and Gram-negative pathogenic bacteria (it exhibits the strongest activity against Enterobacter cloacae ATCC 13047, with an MIC = 1.56 μg/mL)[1].
Salinamide A (>50 μg/mL; 16-48 hr) exhibits no cytotoxicity against mammalian Vero E6 ATCC CRL1586 cells[1].
Salinamide A (0-100 μM; 10 min) potently inhibits RNAP from Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli, with an IC50 of 0.2 μM for both, and does not inhibit RNAP from Thermus thermophilus or human RNAP I/II/III even at concentrations as high as 100 μM[1].
Salinamide A (0.098 μg/mL; 10-30 min) inhibits RNA synthesis in Escherichia coli D21f2tolC cells within 10 min, suppresses protein synthesis at subsequent time points, and exerts no effect on DNA synthesis[1].
Spontaneous resistance mutations induced in Escherichia coli D21f2tolC by salinamide A (0.6-1.2 μg/mL; 24-48 hr) localize exclusively to the RNA polymerase (RNAP) subunit genes rpoC and rpoB, and confer ≥ 16-fold resistance to the strain[1].
Salinamide A (10 μM; 5 min) does not inhibit the formation of heparin-resistant transcription initiation open complexes between Escherichia coli RNAP holoenzyme and lacUV5 (ICAP) promoter DNA[1].
Salinamide A (10 μM; 10 min) inhibits nucleotide addition during primer-dependent transcription initiation[1].
Salinamide A (10 μM; 5 min) inhibits nucleotide addition during transcription elongation by Escherichia coli RNA polymerase holoenzyme and suppresses pyrophosphorolysis[1].
Salinamide A (0-0.4 μM; 30 min) inhibits nucleotide addition by the Escherichia coli RNA polymerase holoenzyme in a non-competitive manner, with a Ki of 0.2 μM[1].
Salinamide A (0-64 μM; 5 min) exerts equivalent inhibitory effects on the nucleotide addition process of wild-type and trigger loop-deleted (ΔTL) Escherichia coli RNAP core enzymes[1].
Salinamide A (20 mM; 30 min) binds to the bridge helix cap structure of Escherichia coli RNA polymerase holoenzyme[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 152340-22-2
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분자량 1020.13
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화학식 C51H69N7O15
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SMILES
C[C@H]([C@@]1(CO1)/C=C\C(NCC(OC[C@@]2(NC([C@]([H])(NC([C@@H](N3C)CC4=CC=CC=C4)=O)[C@@H](C)O)=O)[H])=O)=O)OC(C=C5)=CC=C5[C@@](NC(C([C@H](CC)C)NC([C@H]([C@H](OC2=O)C)NC([C@@H]([C@@H](C(C)C)O)C)=O)=O)=O)([H])C3=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
The EdU incorporation assay measures DNA synthesis by adding the thymidine analog 5-ethynyl-2′-deoxyuridine to cells or tissues, where it is incorporated into newly synthesized DNA during S phase. Incorporated EdU is detected by copper-catalyzed azide-alkyne cycloaddition, in which a fluorescent azide covalently reacts with the ethynyl group on EdU, allowing S-phase cells to be detected by fluorescence microscopy, flow cytometry, or high-content imaging. EdU detection does not require DNA denaturation or anti-BrdU antibody access, which preserves sample structure and improves compatibility with immunostaining and multiparameter cytometry compared with BrdU-based detection. EdU can be cytotoxic in a cell-type- and exposure-dependent manner, so pulse duration, concentration, and continuous-labeling designs should be validated for each cell type.
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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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BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)