ml 128

VU0361737 (ML-128) is a specific positive allosteric modulator (PAM) of the mGlu4 receptor with an EC50 of 240 nM for human receptors and 110 nM for rat receptors. It exhibits weak activity at mGlu5 and mGlu8 receptors and is inactive at mGlu1, mGlu2, mGlu3, mGlu6, and mGlu7 receptors. The compound can penetrate the CNS.

ATP Synthase Inhibitor 2 (Compound 22) TFA is a potent inhibitor of Pseudomonas aeruginosa ATP synthase with an IC50 value of 10 μg/mL. It effectively halts ATP synthesis in Pseudomonas aeruginosa at a concentration of 128 μg/mL [1].

Antibacterial Agent 128, a siderophore analog-Ciprofloxacin (Ciprofloxacin) conjugate connected via a cleavable linker, demonstrates effective antibiotic properties. Specifically, it exhibits activity against P. aeruginosa and B. pseudomallei, with Minimum Inhibitory Concentration (MIC) values ranging from 0.25 to 64 μg/mL and 1 to 32 μg/mL, respectively [1].

ATP Synthase Inhibitor 2, a compound targeting Pseudomonas aeruginosa (PA) ATP synthase with an IC50 of 10 μg/mL, fully inhibits the ATP synthesis activity of PA at a concentration of 128 μg/mL [1].

(-)-Mycousnine is a microbial metabolite and derivative of usnic acid originally isolated fromM. nawaethat has antibacterial and antifungal activities.1,2It is active against the Gram-positive bacteriaB. subtilis,K. rhizophila, andS. aureus(MICs = 4, 8, and 4 g/ml, respectively) but not the Gram-negative bacteriaE. coli,S. typhimurium, andK. pneumoniae(MICs = >128 g/ml for all).2(-)-Mycousnine is also active against the fungiT. mentagrophytes,T. rubrum, andC. albicans(MICs = 25, 25, and 100 μg/ml, respectively).1 1.Sassa, T., and Igarashi, M.Structures of (-)-mycousnine, (+)-isomycousnine and (+)-oxymycousnine, new usnic acid derivatives from phytopathogenic Mycosphaerella nawaeAgric. BioI. Chem.54(9)2231-2237(1990) 2.Lee, J., Lee, J., Kim, G.J., et al.Mycousfurans A and B, antibacterial usnic acid congeners from the fungus Mycosphaerella sp., isolated from a marine sedimentMar. Drugs17(7)422(2019)

Antitubercular agent-17 (Compound 8a) is an efficacious antitubercular agent, demonstrating Minimum Inhibitory Concentration (MIC) values of 2 μg ml against M. tuberculosis H37Rv, Spec. 192, and Spec. 210, and 128 μg ml against Spec. 800. It exhibits highly selective antimycobacterial effects [1].

Leoidin is a depsidone originally isolated from L. gangaleoides that has antibacterial and enzyme inhibitory activities.1,2,3 It is active against the bacteria E. faecalis, H. influenzae, M. catarrhalis, S. aureus, and S. pneumoniae (MICs = 8, 32, 1, 128, and 64 μg/ml, respectively).2 Leoidin inhibits phenylalanyl-tRNA synthetase (PheRS) isolated from P. aeruginosa (IC50 = 42 μM). It also inhibits organic anion-transporting polypeptide 1B1 (OATP1B1) and OATP1B3 with Ki values of 0.08 and 1.84 μM, respectively, in CHO cells expressing the human transporters.3

Antibacterial agent 50 (example 47) is a compound exhibiting antibacterial activity with minimum inhibitory concentration (MIC) values of 32, 64, and 128 mcg mL against E. coli strains NCTC 13351, M 50, and 7 MP, respectively [WO2013030733A1].

Antimicrobial Agent-1 (compound 6C) shows strong activity (MIC = 2 μg/mL) against TolC mutant E. coli. Additionally, it synergistically interacts with Colistin to exhibit enhanced activity against Gram-negative bacteria. Importantly, Antimicrobial Agent-1 exhibits no cytotoxic effects on mammalian cell lines. Its MIC values on Caco-2 and Vero cell lines are greater than 128 μg/mL [1].

Antitubercular agent-18 (Compound 9a) is an antitubercular agent that exhibits highly selective antimycobacterial effects, with minimum inhibitory concentration (MIC) values of 2 μg ml against M. tuberculosis H37Rv, Spec. 192, and Spec. 210, and 128 μg ml against Spec. 800, demonstrating its efficacy in inhibiting the growth of these mycobacterial strains [1].

A-39183A is an active component of the A-39183 antibiotic complex produced by aerobic fermentation of Streptomyces NRRL 12049. It has activity against penicillin-resistant S. aureus 3055 and S. faecalis X66 (MICs = 32 and 32 μg/ml, respectively) and a variety of Gram-positive and Gram-negative anaerobic bacteria (MICs = 16-128 μg/ml) in an agar dilution assay.

Sinapaldehyde (trans-3,5-Dimethoxy-4-hydroxy cinnamaldehyde) is a natural product. Sinapaldehyde exhibits moderate antibacterial against Methicillin resistant S. aureus (MRSA) and E. coli with MIC values of 128 and 128 μg/mL.

YKAs3003, a potent inhibitor of pathogenic KAS III, displays minimal inhibitory concentration (MIC) values in the range 128-256 microg/mL against various bacteria.

Ranalexin, an antimicrobial peptide, demonstrates inhibition of S. aureus, E. coli, and P. aeruginosa, with respective minimum inhibitory concentrations (MICs) of 4, 32, and 128 μg/mL [1].

IMCTA-C14, a detergent and derivative of the microbial metabolite 4-trehalosamine, exhibits a critical micelle concentration (CMC) of 0.11 mM and a hydrophilic-lipophilic balance (HLB) value of 9.72. It effectively extracts proteins, including membrane proteins, from OVK18 ovarian cancer cells at concentrations of 0.05 and 0.5%. Furthermore, IMCTA-C14 demonstrates antibacterial activity against various bacterial strains (MICs = 8-128 µg/ml) and shows cytotoxicity against a spectrum of 52 cancer cell lines (IC50s = 2.9-29.2 µg/ml). At a concentration of 50 µM, it induces autophagy in OVK18 cells.

β-Defensin-1 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth ofB. adolescentis,L. acidophilus,B. breve,B. vulgatus,L. fermentum,B. longum, andS. thermophilusin an antimicrobial radial diffusion assay.2β-Defensin-1 also inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius, and of susceptibleM. tuberculosisH37Rv but not of resistantM. tuberculosisRM22 when used at a concentration of 128 μg/ml.3,4It blocks human and mouse Kv1.3 voltage-gated potassium channels (IC50s = 11.8 and 13.2 μM, respectively).5Overexpression of β-defensin-1 in the human oral squamous cell carcinoma (OSCC) cell lines HSC-3, UM-1, and SCC-9 increases migration and invasion but not proliferation.6 1.Lehrer, R.I.Primate defensinsNat. Rev. Microbiol.2(9)727-738(2004) 2.Schroeder, B.O., Ehmann, D., Precht, J.C., et al.Paneth cell α-defensin 6 (HD-6) is an antimicrobial peptideMucosal Immunol.8(3)661-671(2015) 3.Ouhara, K., Komatsuzawa, H., Yamada, S., et al.Susceptibilities of periodontopathogenic and cariogenic bacteria to antibacterial peptides, β-defensins and LL37, produced by human epithelial cellsJ. Antimicrob. Chemother.55(6)888-896(2005) 4.Fattorini, L., Gennaro, R., Zanetti, M., et al.In vitro activity of protegrin-1 and beta-defensin-1, alone and in combination with isoniazid, against Mycobacterium tuberculosisPeptides25(7)1075-1077(2004) 5.Feng, J., Xie, Z., Yang, W., et al.Human beta-defensin 1, a new animal toxin-like blocker of potassium channelToxicon113(2016) 6.Han, Q., Wang, R., Sun, C., et al.Human beta-defensin-1 suppresses tumor migration and invasion and is an independent predictor for survival of oral squamous cell carcinoma patientsPLoS One9(3)e91867(2014)

1-(3,4-Dimethoxyphenyl)-2-(4-allly-2,6-dimethoxyphenoxy)propan-1-ol shows anti-staphylococcal activity against a total of five multidrug-resistant (MDR) and methicillin-resistant Staphylococcus aureus strains and the minimum inhibitory concentrations (MIC

GP-2B, an antimicrobial peptide, exhibits antibacterial activity against Gram-positive strains, with a minimum inhibitory concentration (MIC) ranging from 8 to 128 μg/mL for S. aureus and Enterococcus faecalis [1].

Lynronne-3, an antimicrobial peptide, demonstrates activity against Gram-positive bacteria, including multi-drug resistant (MDR) strains, with a minimum inhibitory concentration (MIC) ranging from 32-128 μg/mL for methicillin-resistant Staphylococcus aureus (MRSA) strains. Additionally, Lynronne-3 is efficacious in combating Pseudomonas aeruginosa infections [1].

Chalepensin, a furanocoumarin isolated from the rutaceae plant Ruta chalepensis L., is a selective CYP2A6 inhibitor, inhibiting CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4.Chalepensin exhibits Chalepensin j has antiprotozoal activity and inhibits methicillin-resistant Staphylococcus aureus (MRSA) with MIC values in the range of 32-128 μg/mL.