Propamidine is a covalent inhibitor of TMPRSS2 and has some antibacterial activity.[1].
MUT056399 is a highly potent inhibitor of the FabI enzyme of both S. aureus and E. coli with 50% inhibitory concentration IC50s of 12 nM and 58 nM, respectively. IC50 value: 12 nM (for S. aureus), 58 nM (for E. coli) [1]Target: FabI enzymein vitro: MUT056399 is a highly potent new inhibitor of the FabI enzyme of both Staphylococcus aureus and Escherichia coli. MUT056399 is very active against S. aureus strains, including methicillin-susceptible S. aureus (MSSA), methicillin-resistant S. aureus (MRSA), linezolid-resistant, and multidrug-resistant strains, with MIC90s between 0.03 and 0.12 μg/ml. MUT056399 is also active against coagulase-negative staphylococci, with MIC90s between 0.12 and 4 μg/ml. MUT056399 is very active against the 118 S. aureus strains tested, including MSSA and MRSA isolates and linezolid-resistant and multidrug-resistant strains, with MIC90s between ≤0.03 and 0.12 μg/ml.In vivo: MUT056399, administered subcutaneously, protected mice from a lethal systemic infection induced by MSSA, MRSA, and vancomycin-intermediate S. aureus strains (50% effective doses ranging from 19.3 mg/kg/day to 49.6 mg/kg/day). In the nonneutropenic murine thigh infection model, the same treatment with MUT056399 reduced the bacterial multiplication of MSSA and MRSA in the thighs of immunocompetent mice.
Puromycin dihydrochloride is the dihydrochloride salt of puromycin. Puromycin is an aminoglycoside antibiotic that inhibits protein synthesis.
UDP-3-O-acyl-GlcNAc (UDP-3-O-(3-hydroxytetradecanoyl)-N-acetylglucosamine) is an E. coli metabolite that is involved in 3-deoxy-D-manno-octulosonate (KDO) biosynthesis pathway[1].
QStatin is a novel, potent, and selective Vibrio quorum sensing (QS) inhibitor, shows pan-QS inhibitor activity in diverse Vibrio species. QStatin attenuates representative QS-regulated phenotypes in various Vibrio speciesbinds tightly to a putative ligand-binding pocket in SmcR and changes the flexibility of the protein, thereby altering its transcription regulatory activity. QStatin may be a sustainable antivibriosis agent useful in aquacultures[1].
Isochamaejasmin is a biflavonoid with anti-cancer, antiplasmodial and insecticidal activities. Isochamaejasmin displays a potent NF-κB (NF-κB) activation activity. Isochamaejasmin could cause DNA damage and induce Apoptosis via the mitochondrial pathway in AW1 cells[1][2]. Isochamaejasmin also has a moderate antiplasmodial activity (IC50 of 7.3 μM for P. falciparum) and relatively low cytotoxicity (CC50 of 29.0 μM)[3].
Aloperine is an alkaloid in sophora plants such as Sophora alopecuroides L, which has shown anti-cancer, anti-inflammatory and anti-virus properties[1]. Aloperine is widely used to treat patients with allergic contact dermatitis eczema and other skin inflammation in China[2]. Aloperine induces apoptosis and autophagy in HL-60 cells[1].
MMV688845 is a nontuberculous mycobacteria (NTM) RNA polymerase inhibitor with bactericidal activity against Mycobacterium abscessus and anti-tuberculosis efficacy[1].
Oxiconazole (Ro 13-8996) is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest[1][2][3].
PDE12-IN-1 is a potent and selective PDE12 inhibitor with a pIC50 value for enzyme inhibition of 9.1. PDE12-IN-1 increases 2′,5′-linked adenylate polymers (2-5A) levels, and the pEC50 value is 7.7. PDE12-IN-1 shows antiviral activity[1].
Psoracorylifol C is a natural product. Psoracorylifol C has important activity against Helicobacter pylori. Psoracorylifol C can be isolated from the seeds of Psoralea corylifolia[1].
L-(+)-threo-Chloramphenicol ((+)-Chloramphenicol) is the S,S-stereoisomer of Chloramphenicol (HY-B0239). L-(+)-Threo-chloramphenicol inhibits protein synthesis in reticulocytes. L-(+)-threo-Chloramphenicol also inhibits the oxidative activity of isolated mitochondria[1][2].
Cyclosporin A-Derivative 3 is a derivative of Cyclosporin A (HY-B0579) with calcineurin inhibition[1].
Diiodohydroxyquinoline is a topical therapeutic agent, with satisfactory antibacterial properties.
Porgaviximab is a monoclonal antibody that can be used Ebola infection research[1].
Acibenzolar-S-methyl (ASM) is a plant resistance inducer that mimics pathogen-host interactions and leads to systemic acquired resistance in plants. Acibenzolar-S-methyl helps reduce the use of pesticides and can be used in research to prevent plant diseases[1][2].
L-Canaline is a nonprotein amino acid stored in many leguminous plants. L-Canaline is a cytotoxic metabolite catalyzed by L-canavanine and its arginase. L-Canaline is a potent and irreversible inhibitor of ornithine aminotransferase. L-Canaline inhibits the growth of the malaria parasite Plasmodium falciparum with an IC50 of 297 nM. L-Canaline has anticancer and antiproliferative effects[1][2][3].
Globomycin is a lipopeptide antibiotic and a signal peptidase II (LspA) inhibitor. Globomycin inhibits processing of the prolipoprotein by binding irreversibly to the peptidase. Globomycin has toxic for the mollicute Spiroplasma melliferum with a MIC in the range 6.25-12.5 μM[1][2].
D-Cycloserine is an analog of the amino acid D-alanine.Target: AntibacterialD-Cycloserine selectively potentiated the duration of motor cortical excitability enhancements induced by anodal tDCS. D-Cycloserine alone did not modulate excitability [1]. Participants receiving d-cycloserine in addition to exposure therapy reported significantly less social anxiety compared with patients receiving exposure therapy plus placebo. Controlled effect sizes were in the medium to large range [2]. Chronic D-cycloserine significantly reduced nicotine self-administration selectively in rats with low baseline nicotine use, but was ineffective with the rats with higher levels of baseline nicotine self-administration [3].
CCR5 antagonist 3 (Compound 26) is a CCR5 antagonist with an IC50 of 15.90 nM. CCR5 antagonist 3 shows broad-spectrum anti-HIV-1 activities[1].
BRD4-IN-3 (compound 141) is a potent BRD4 inhibitor with an IC50 of <0.5 µM. BRD4-IN-3 shows cytoxicity for MYC-Raji with an IC50 value of >1 µM[1].
Bismuth subcitrate potassium is an antibiotic against 12 C. pyloridis strains with MIC50 of 8 ug/ml[1]. Bismuth subcitrate potassium is used to treat diseases of the upper gastrointestinal tract infected with Helicobacter pylori[2].
Cefaclor monohydrate is an effective antibiotic agent, and specifically binds to penicillin-binding protein 3 (PBP 3)[1].
HBV-IN-8 is a potent HBV inhibitor with an EC50 of 287.9 nM (WO2021213445A1, compound 13)[1].
Pibrentasvir is a novel and pan-genotypic hepatitis C virus (HCV) NS5A inhibitor with EC50s ranging from 1.4 to 5.0 pM against HCV replicons containing NS5A from genotypes 1 to 6.
UCK2 Inhibitor-3 is a non-competitive inhibitor of uridine-cytidine kinase 2 (UCK2, a pyrimidine salvage enzyme) with an IC50 value of 16.6 μM. UCK2 can replace dihydroorotate dehydrogenase (DHODH), in a certain extent, in infected or rapidly dividing cells to continue efficient uridine salvage. UCK2 Inhibitor-3 also inhibits DNA polymerase eta and kappa with IC50s of 56 μM and 16 μM[1].
Epimedokoreanin B is a natural flavonoid with anticancer, anti-inflammatory and antibacterial effects. Epimedokoreanin B inhibits the growth of lung cancer cells through endoplasmic reticulum stress-mediated Apoptosis accompanied by autophagosome accumulation. Epimedokoreanin B is an anti-periodontitis agent that inhibits gingipains and Porphyromonas gingivalis growth and biofilm formation[1][2][3].