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GC-072 (GC072) is a potent, 4-oxoquinolizine antibiotic with selective inhibitory activity against bacterial topoisomerases (E. coli Topo II/DNA gyrase, IC50=0.18-1.5 uM).GC-072 demonstrated no detectable inhibition of human Topo I and II, is selective for bacterial topoisomerases (IC50>100 uM).GC-072 inhibits E. coli Quinolone-resistant gyrase (IC50=1.3-1.5 uM), S. aureus Gyrase and Topo IV (IC50=2-30 uM).GC-072 demonstrated good activity against B. pseudomallei, with an MIC90 of 0.25 ug/mL.GC-072 exhibited strong in vitro antimicrobial potency against biothreat agents Bacillus anthracis, Yersinia pestis, and Francisella tularensis and category B biothreat agent Burkholderia mallei.GC-072 is efficacious against B. pseudomallei aerosol infection in a mouse model following exposure to a 24-LD50 bacterial challenge.
Savirin (S. aureus virulence inhibitor) is a small molecule that targets the agr (accessory gene regulator) quorum sensing system in Staphylococcus aureus (S. aureus). The agr system is a key regulatory pathway that controls the expression of virulence factors in S. aureus, which are critical for its pathogenicity. The system involves a two-component signal transduction pathway consisting of AgrC (a histidine kinase) and AgrA (a response regulator).
JSF-2414 (JSF2414) is a potent, small molecule GyrB/ParE dual binding inhibitor, simultaneously binds to ATP binding regions of DNA gyrase (GyrB) and topoisomerase (ParE) and displays potent in vitro activity against strains of MRSA, VRSA and VISA.
COE2-2hexyl represents an innovative class of antimicrobial agents, demonstrating broad-spectrum antibacterial activity through its unique conjugated oligoelectrolyte (COE) structure.
Cymal-6 (Cyclohexyl-hexyl-β-D-maltoside) is a potent TEM-1 beta-lactamase inhibitor with an Ki value of 40.05 µM. Cymal-6 (Cyclohexyl-hexyl-β-D-maltoside) can be used as glycosidic surfactant.
UNC10201652 is a potent Loop 1 (L1)-specific gut bacterial β-glucuronidase (GUSs) inhibitor with an IC50 value of 0.117 μM for E. coli GUS. UNC10201652 can block SN-38 glucuronide processing only in individuals whose fecal gut microbiota is highly abundant in L1 GUS enzymes.
VP-4604 is a potent anti-methicillin-resistant Staphylococcus aureus (MRSA) agent. VP-4604 exhibits significant microbial growth inhibition toward Staphylococcus aureus (ATCC 43300) with MIC of 4-8 µg/mL. VP-4604 inhibits the growth of methicillin‐resistant Staphylococcus aureus with growth inhibition >95%.
EDA-DA is an unnatural dipeptide building block (an ethynyl-D-alanine and a D-alanine). It incorporates a biorthogonal alkyne group into peptidoglycan (PG) through MurF in the cytoplasmic pathway, which enables selective labeling via a click-chemistry reaction. EDA-DA allows labeling of PG in Gram-positive (B. subtilis), Gram-negative (E. coli and C. trachomatis), Mycobacterium (M. smegmatis) and moss plastids (P. patens) with azide modified fluorescent dyes such as Alexa Fluor 488.
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