DNA Gyrase-IN-6 

Antibacterial agent 138 is a benzothiazole inhibitor of bacterial DNA gyrase and topoisomerase IV. Antibacterial agent 138 exhibits favorable solubility and plasma protein binding. Antibacterial agent 138 has antibacterial activity against Gram-positive and Gram-negative strains. Antibacterial agent 138 is a dual GyrB and ParE inhibitor^[1].

DNA gyrase, Topoisomerase IV^[1]

Antibacterial agent 138 (compound 7a) inhibits DNA gyrase and topoisomerase IV from S. aureus (IC₅₀=1.22 nM and 8.0 nM, repsectivley), E. coli (IC₅₀=<10 nM and 44 nM, repsectivley), A. baumannii (IC₅₀=2.42 nM and 119.7 nM, repsectivley), and P. aeruginosa (IC₅₀=<10 nM and 27.5 nM, repsectivley) with low nanomolar ranges^[1].
Antibacterial agent 138 (up to 100 μM) shows no cytotoxicity on a breast cancer MCF-7 cell line and a liver cancer HepG2 cell^[1].

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

Antibacterial agent 138 (compound 7a) (25 and 50 mg/kg; iv; single dose) shows bactericidal activity in neutropenic mouse thigh infection model^[1].

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

455.32

C₁₈H₁₆Cl₂N₄O₄S

CC1=C(C(Cl)=C(N1)C(NC2=NC3=C(S2)C=C(C=C3N4CCOCC4)C(O)=O)=O)Cl

Room temperature in continental US; may vary elsewhere.

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

• [1]. Durcik M, et al. New Dual Inhibitors of Bacterial Topoisomerases with Broad-Spectrum Antibacterial Activity and In Vivo Efficacy against Vancomycin-Intermediate Staphylococcus aureus. J Med Chem. 2023 Mar 23;66(6):3968-3994.  [Content Brief]