MAC13243, an antibacterial agent, is a likely inhibitor of the bacterial lipoprotein targeting chaperone, LolA.IC50 Value: Target: AntibacterialMAC13243, a molecule that belongs to a new chemical class and that has a unique mechanism and promising activity against multidrug-resistant Pseudomonas aeruginosa. MAC13243 inhibits the function of the LolA protein and represents a new chemical probe of lipoprotein targeting in bacteria with promise as an antibacterial lead with Gram-negative selectivity.
ISPA-28 is a specific plasmodial surface anion channel (PSAC) antagonist. ISPA-28 binds directly and reversibly to CLAG3[1][2].
Jh-X-119-01 is a novel potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 irreversibly labels IRAK1 at C302. This compound exhibited cytotoxic activity at single digit micromolar concentrations in a panel of WM, DLBCL, and lymphoma cell lines expressing MYD88. Cotreatment of JH-X-119-01 with the BTK inhibitor ibrutinib resulted in synergistic killing effects in these systems.
Pyrindamycin B is an antibiotic, actives against gram-positive and gram-negative bacterias, and exhibits strong therapeutic effects against both drug-sensitive and resistant cells of P388 leukemia in mice[1].
Dermaseptin-S5 is an antimicrobial peptide derived from frog skin against filamentous fungi[1].
FG944 (FG-944) is a potent selective LpxC inhibitor with MIC50 of 0.5 ug/mL against K.pneumoniae, synergizes with rifampin in carbapenem resistant K. pneumoniae and E. coli.
Josamycin (EN-141) is a macrolide antibiotic exhibiting antimicrobial activity against a wide spectrum of pathogens, such as bacteria. The dissociation constant Kd from ribosome for Josamycin is 5.5 nM.
Diamthazole (Dimazole) is an antifungal agent. Diamthazole can be used for the research of infection[1].
Iodobananin is an effective inhibitor of the ATPase activity of the SARS Coronavirus helicase with an IC50 value of 0.54 μM.
Ofloxacin-d8 (Hoe-280-d8) is the deuterium labeled Ofloxacin. Ofloxacin (Hoe-280) is a fluoroquinolone whose primary mechanism of action is inhibition of bacterial DNA gyrase.
Sinapaldehyde, isolated from the stems of Rhodamnia dumetorum, exhibits moderate antibacterial against Methicillin resistant S. aureus (MRSA) and E. coli with MIC values of 128 and 128 μg/mL[1].
Marbofloxacin is a potent antibiotic of which depends upon its inhibition of DNA-gyrase. Marbofloxacin is a synthetic, broad spectrum bactericidal agent.Target: DNA-gyraseMarbofloxacin is a third-generation fluoroquinolone for veterinary use, the antimicrobial of which depends upon its inhibition of DNA-gyrase and topoisomerase IV. With a broad spectrum bactericidal activity and good efficacy, marbofloxacin is indicated for dermatological, respiratory and urinary tract infections due to both Gram-positive and Gram-negative bacteria and Mycoplasma [1].Administration of Marbofloxacin at 6 mg/kg once daily for 7 days in a Staphylococcus aureus infection in tissue cages in ponies is not effective for the elimination of S. aureus infections from secluded sites [2]. The pharmacokinetic properties of marbofloxacin were investigated in 6 horses after i.v., subcutaneous and oral administration of a single dose of 2 mg/kg bwt and the minimal inhibitory concentrations (MIC) assessed for bacteria isolated from equine infectious pathologies. The clearance of marbofloxacin was mean +/- s.d. 0.25 +/- 0.05 l/kg/h and the terminal half-life 756 +/- 1.99 h. The marbofloxacin absolute bioavailabilities after subcutaneous and oral administration were 98 +/- 11% and 62 +/- 8%, respectively. Considering the breakpoint values of efficacy indices for fluoroquinolones, a marbofloxacin dosage regimen of 2 mg/kg bwt/24 h by i.v., subcutaneous or oral routes was more appropriate for enterobacteriaceae than for S. aureus [3]. Toxicity: cramps; vomiting; anorexia; soft stools; diarrhoea
Majoranaquinone exhibits a high antibacterial effect against 4 Staphylococcus, 1 Moraxella, and 1 Enterococcus strains. Majoranaquinone shows substantial efflux pump inhibitory activity in Escherichia coliATCC 25922 strain. Majoranaquinone is found to be an effective biofilm formation inhibitor on E.coli, ATCC 25922 and E. coli K-12 AG100 bacteria[1].
KAMP-19, a keratin-derived antimicrobial peptide, is an antimicrobial peptide against P. aeruginosa. [1].
Adeninobananin, a negative control tool, does not show any inhibitory activity of the SARS Coronavirus helicase.
3, 5-diprenyl-4-hydroxybenzaldehyde is an isoprene phenyl butyl aldehyde. 3, 5-diprenyl-4-hydroxybenzaldehyde had the ability to inhibit biofilm formation in strains. 3, 5-diprenyl-4-hydroxybenzaldehyde can be used to study the potential synergistic effect of clinically relevant antibiotics [1].
HIV Protease Substrate 1, a fiuorogenic HIV protease substrate, can be used to study enzymatic activity of HIV protease[1].
Ceftezole is an α-Glucosidase inhibitor with an IC50 and a Ki of 2.1 μM and 0.578 μM, respectively.
Taribavirin hydrochloride is an inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus[1]. Taribavirin hydrochloride is a Ribavirin prodrug, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia[2].
7-Deaza-2',3'-dideoxyguanosine (7-Deaza-ddG) is a 2′,3′-dideoxynucleoside 5′-triphosphate, which can inhibit HIV-1 reverse transcriptase with a Ki of 25 nM[1].
Venturicidin A (Aabomycin A1), from actinomycetes, is a membrane-active natural product inhibitor of ATP synthase. Venturicidin A potentiates the aminoglycoside antibiotic gentamicin against multidrug-resistant clinical isolates of Staphylococcus, Enterococcus, and Pseudomonas aeruginosa. Venturicidin A shows noticeable toxicity toward human embryonic-kidney (HEK)cells with an IC50 of 31 μg/mL[1].
Oseltamivir acid D3 (GS 4071 D3) is a deuterium labeled Oseltamivir acid. Oseltamivir acid, the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses[1][2].
PF-5081090 (LpxC-4) is a potent LpxC inhibitor, is a rapidly bactericidal with broad-spectrum activity. PF-5081090 serves as a regulator of lipid A biosynthesis in Gram-negative pathogens[1][2].
Aszonapyrone A is a metabolite produced by Aspergillus zonatus[1].
HBV-IN-38 (Example 193) is an HBV DNA inhibitor (EC50≤100nM). HBV-IN-38 can be used to study viral infections[1].
Dehydroandrographolide succinate, extracted from herbal medicine Andrographis paniculata (Burm f) Nees, is widely used for the treatment of viral pneumonia and viral upper respiratory tract infections because of its immunostimulatory, anti-infective and anti-inflammatory effect[1].
Ulifloxacin is a broad-spectrum quinolone antibiotic. Ulifloxacin is the active metabolite of Prulifloxacin (HY-B0024). Ulifloxacin has anti-bacterial activity[1].
Antibacterial agent 59 (example 24) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
Maleic Acid-d2 is the deuterium labeled Maleic Acid[1]. Maleic Acid is a Glutamate Decarboxylase (GAD) inhibitor of E. coli and L. monocytogenes[2][3].
Methyl cinnamate (Methyl 3-phenylpropenoate), an active component of Zanthoxylum armatum, is a widely used natural flavor compound. Methyl cinnamate (Methyl 3-phenylpropenoate) possesses antimicrobial activity and is a tyrosinase inhibitor that can prevent food browning. Methyl cinnamate (Methyl 3-phenylpropenoate) has antiadipogenic activity through mechanisms mediated, in part, by the CaMKK2-AMPK signaling pathway[1].