DNA Gyrase/ribosomes-IN-1 

DNA Gyrase/ribosomes-IN-1 is a bacterial ribosome and DNA gyrase inhibitor, with IC₅₀ values of 1.11 μM and 3.31 μM, respectively. DNA Gyrase/ribosomes-IN-1 also inhibits CYP3A4, with an IC₅₀ of 18.5 μM, and exhibits stability in mouse plasma and liver microsomes. DNA Gyrase/ribosomes-IN-1 inhibits bacterial protein synthesis by interacting with ribosomal RNA and associated sites. DNA Gyrase/ribosomes-IN-1 suppresses bacterial DNA replication by interacting with the gyrase complex. DNA Gyrase/ribosomes-IN-1 restores activity against macrolide-resistant, erm-mediated Gram-positive pathogens and enhances activity against Gram-negative bacteria such as Haemophilus influenzae and Moraxella catarrhalis. DNA Gyrase/ribosomes-IN-1 can be used in research on community-acquired bacterial pneumonia^[1].

DNA Gyrase/ribosomes-IN-1 (compound 26l) (0.01-5 μM) inhibits E. coli protein synthesis with an IC₅₀ of 1.11 μM and E. coli DNA gyrase with an IC₅₀ of 3.31 μM, demonstrating dual inhibition of these two targets^[1].
DNA Gyrase/ribosomes-IN-1 (0.01-30 μM) inhibits CYP3A4 with an IC₅₀ of 18.5 μM^[1].
DNA Gyrase/ribosomes-IN-1 (1 μM) exhibits high stability in mouse plasma (99.30% remaining after 0.5 h) and moderate stability in mouse liver microsomes (75.82% remaining after 1 h)^[1].
DNA Gyrase/ribosomes-IN-1 (10-50 μM; 48 h) exhibits cytotoxicity with CC₅₀ values of 25.77 μM in HepG2 cells and 23.40 μM in 293T cells^[1].
DNA Gyrase/ribosomes-IN-1 (0.008-256 μg/mL; 16-24 h) exhibits antibacterial activity against various strains including S. pneumoniae, S. pyogenes, and H. influenzae with MIC values ranging from 0.03 to 0.5 μg/mL^[1].

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

1046.20

C₅₃H₇₇F₂N₅O₁₄

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Room temperature in continental US; may vary elsewhere.

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

• [1]. Liu RC, et al. Dual-targeting ketolide-quinolone hybrids overcome erm-mediated resistant pathogens via ribosomal and DNA gyrase inhibition. Eur J Med Chem. 2026;305:118562.  [Content Brief]