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. Nr.: 1445801-61-5
- Formel: C34H28Cl2N4O6
- Molecular Weight:659.52
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
In Vitro
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. Further protocols information, click here.
In Vivo
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. Nr. 1445801-61-5
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Molecular Weight 659.52
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Gram Staining of Tissue Sections
Gram staining of tissue sections is a histochemical technique used to differentiate Gram-positive and Gram-negative bacteria within histological specimens based on differences in bacterial cell wall structure and dye retention, adapted from classical bacteriological Gram staining into tissue-compatible “histological Gram stain” variants. In tissue applications, modifications of the Brown-Hopps and Brown-Brenn methods are commonly used to improve differentiation of microorganisms embedded within host connective tissue and to reduce overstaining or loss of Gram-negative signal, which are known limitations of earlier approaches. The principle relies on crystal violet-iodine complex retention in Gram-positive organisms and subsequent decolorization and counterstaining steps that allow contrast visualization of Gram-negative organisms against tissue background.
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Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
GKL003 Related Classifications
HY-102072 Related Classifications
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Keywords
- 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