Activators & Inhibitors

Feglymycin (Legacy Tebubio ref. 282T37874). Feglymycin is a 13-amino acid peptide originally isolated from Streptomyces that has antibacterial and antiviral activities. It is active against Gram-positive bacteria (MICs = 32-64 μg/ml) and inhibits HIV viral replication in H9 cells (IC50 = ~5 μM). Feglymycin is also active against clinical isolates of HIV-1 from clades A-D, A/E, and G (EC50s = 0.5-6.7 μM). It interacts with gp120 and inhibits HIV-1 NL4.3 binding to human soluble CD4 (EC50 = 4.4 μM) and to CD4+ SupT1 T cells by 74.5% when used at a concentration of 10.5 μM. Feglymycin inhibits the E. coli peptidoglycan biosynthesis enzymes MurA and MurC (Kis = 3.4 and 0.3 μM, respectively) in a noncompetitive manner.

Fenbendazole sulfone (Legacy Tebubio ref. 282T37875). Fenbendazole sulfone is a minor metabolite of the anthelmintic fenbendazole . Fenbendazole undergoes oxidation to form oxfendazole, which is further oxidized to form fenbendazole sulfone.

Ribavirin 5'-monophosphate (lithium salt) (Legacy Tebubio ref. 282T37877). Ribavirin 5'-monophosphate (lithium salt) directly inhibits IMP dehydrogenase (converts IMP to XMP).

N-tridecanoyl-L-Homoserine lactone (Legacy Tebubio ref. 282T37878). Quorum sensing is a regulatory system used by bacteria for controlling gene expression in response to increasing cell density. This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production. Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of which generally consists of a fatty acid coupled with homoserine lactone (HSL). Regulation of bacterial quorum sensing signaling systems to inhibit pathogenesis represents a new approach to antimicrobial therapy in the treatment of infectious diseases. AHLs vary in acyl group length (C4-C18), in the substitution of C3 (hydrogen, hydroxyl, or oxo group), and in the presence or absence of one or more carbon-carbon double bonds in the fatty a

N-undecanoyl-L-Homoserine lactone (Legacy Tebubio ref. 282T37879). N-acylated homoserine lactones (AHLs) are a class of autoinducers used in bacterial quorum sensing to control gene expression in response to cell density. These molecules, comprising a fatty acid coupled with homoserine lactone (HSL), vary in acyl group length (C4-C18), C3 substitution (hydrogen, hydroxyl, or oxo group), and the presence of carbon-carbon double bonds, determining signal specificity through LuxR family transcriptional regulators. C11-HSL, with its rare odd-numbered acyl carbon chain, may act as a minor quorum-sensing signaling molecule in P. aeruginosa strains. Regulating bacterial quorum sensing can inhibit pathogenesis and represents a novel antimicrobial therapy approach for infectious diseases.

Rehmannioside A (Legacy Tebubio ref. 282T3788). Rehmannioside A, a cyclic enol ether terpene glycoside extracted from the traditional Chinese medicine Dihuang, possesses neuroprotective activity and acts by inhibiting NF-κB and MAPK signaling pathways.

OPC-167832 (Legacy Tebubio ref. 282T37880). OPC-167832 is a potent and orally active dprE1 Inhibitor with an IC50 of 0.258 μM. OPC-167832 has antituberculosis activity and can be used for the research of tuberculosis caused by Mycobacterium tuberculosis[1].

Oritavancin(LY-333328) (Legacy Tebubio ref. 282T37881). Oritavancin is a novel semisynthetic glycopeptide antibiotics. On August 6, 2014, the FDA approved oritavancin for treatment of skin infections. Oritavancin possesses potent and rapid bactericidal activity in vitro against a broad spectrum of both resistant and susceptible Gram-positive bacteria, including Staphylococcus aureus, MRSA, enterococci, and streptococci.

(S)-Enzaplatovir (Legacy Tebubio ref. 282T37883). (S)-Enzaplatovir ((S)-BTA-C585) is the S-enantiomer of Enzaplatovir, exhibiting antiviral activity with an EC50 of 56 nM against respiratory syncytial virus (RSV)[1].