GKL003 

GKL003 is a bacterial transcription inhibitor that targets the RNAP-σ interaction interface, with a K_i of 5.79 nM. GKL003 specifically binds to the RNAP β' clamp helix region at the σ^A 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^[1].

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 K_i 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 σ^70[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GKL003 (1-2 mM) significantly inhibits the growth of Gram-negative E. coli DH5α cultures at concentrations ≥ 1 mM^[1].
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.

659.52

C₃₄H₂₈Cl₂N₄O₆

1445801-61-5

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Ma C, et al. Inhibitors of bacterial transcription initiation complex formation. ACS Chem Biol. 2013 Sep 20;8(9):1972-80.
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