GKL003
GKL003 is a bacterial transcription inhibitor that targets the RNAP-σ interaction interface, with a Ki of 5.79 nM. GKL003 specifically binds to the RNAP β' clamp helix region at the σA factor binding site, blocks the formation of RNAP holoenzyme, and inhibits the formation of bacterial transcription initiation complexes. GKL003 inhibits the growth of both Gram-positive and Gram-negative bacterial cells, and also exhibits activity against drug-resistant strains.
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- CAS No.: 1445801-61-5
- Formule: C34H28Cl2N4O6
- Masse moléculaire:659.52
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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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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
GKL003 (0.5-25 μM) inhibits in vitro transcription by the E. coli RNAP core enzyme combined with B. subtilis σᴬ, with stronger inhibitory activity observed at the subsaturating σᴬ:RNAP core enzyme ratio of 0.5:1[1].
GKL003 (0-500 nM) inhibits the in vitro transcription activity of E. coli RNAP core enzyme with B. subtilis σᴬ, with an inhibition constant Ki of 5.79 nM[1].
GKL003 (10-500 nM) inhibits the in vitro transcription activity of the E. coli RNAP core enzyme with E. coli σ70[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GKL003 (0.5-2 mM) significantly inhibits the growth of Methicillin (HY-121544)-resistant Gram-positive Staphylococcus aureus strain USA300 at concentrations ≥ 1 mM, and dose-dependently suppresses transcription in viable S. aureus USA300 cells[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. 1445801-61-5
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Masse moléculaire 659.52
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Formule C34H28Cl2N4O6
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SMILES
O=C(C1=C(C=C(C2=C1NC=C2C3=CC=C(Cl)C=C3)OC)OC)NNC(C4=C(C=C(C5=C4NC=C5C6=CC=C(Cl)C=C6)OC)OC)=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)
GKL003 Related Classifications
HY-102072 Related Classifications
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- GKL003
- 1445801-61-5
- GKL 003
- GKL-003
- Bacterial
- DNA/RNA Synthesis
- Gram-positive bacterial cells
- Escherichia coli
- RNAP holoenzyme
- community-acquired methicillin-resistant Staphylococcus aureus strain USA300
- bacterial transcription initiation complex
- bacterial infections
- σ^A factor
- Gram-negative bacterial cells
- Bacillus subtilis
- RNAP β' clamp-helix region
- Inhibitor
- inhibitor
- inhibit