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
- Formule: C51H69N7O15
- Masse moléculaire:1020.13
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero E6 | MIC |
> 50 μg/mL
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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.
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24843001 |
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.
Chemical Information
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CAS No. 152340-22-2
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Masse moléculaire 1020.13
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Formule 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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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Salinamide A Related Classifications
HY-125442 Related Classifications
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