Bruceantinol (compound 4) is a quassinoid compound isolated from the CH3OH extract of Brucea javanica. Bruceantinol exhibits inactivation effects in systemic host plants. Bruceantinol is potent, with a minimum inhibitory concentration of 10 μM[1].
Cilastatin sodium (MK0791 sodium) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin sodium inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin sodium is an antibacterial adjunct[1][2][3].
Nafcillin sodium monohydrate is a semi-synthetic antibiotic related to penicillin.Target: AntibacterialNafcillin sodium is a narrow-spectrum, beta-lactam antibiotic of the penicillin class. As a beta-lactamase-resistant penicillin, it is used to treat infections caused by Gram-positive bacteria, in particular, species of staphylococci that are resistant to other penicillins. Nafcillin is considered therapeutically equivalent to oxacillin, although its safety profile is somewhat different. Nafcillin was shown to reversibly inhibit beta-lactamase from Staphylococcus aureus PC1 with characteristics indicative of a type A inhibitor [Citri, Samuni & Zyk (1976) Proc. Natl. Acad. Sci. U.S.A. 73, 1048-1052]. At nafcillin concentrations above 80 mM, complete inactivation occurred within 200 s. Upon removal of the excess nafcillin the inhibited enzyme was re-activated completely, with a rate constant of 2.0 x 10(-3) s-1 (25 degrees C) [1, 2].
Enniatin A is a Fusarium mycotoxin. Enniatin A inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 22 μM in an enzyme assay using rat liver microsomes[1].
Brevicompanine B, a diketopiperazine alkaloid, is an antiplasmodial agent. Brevicompanine B is active against the malaria parasite Plasmodium falciparum 3D7 IC50 of 35 mg/mL[1].
4-Hydroxybenzoic acid-13C is the 13C labeled 4-Hydroxybenzoic acid[1]. 4-Hydroxybenzoic acid, a phenolic derivative of benzoic acid, could inhibit most gram-positive and some gram-negative bacteria, with an IC50 of 160 μg/mL[2].
Grazoprevir sodium salt (MK-5172 sodium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
Closantel-13C6 is the 13C6 labeled Closantel. Closantel is a halogenated salicylanilide with a potent anti-parasitic activity. Closantel is a potent and highly specific Onchocerca volvulus chitinase (OvCHT1) inhibitor with an IC50 of 1.6 μM and a Ki of 468 nM. Closantel inhibits the O. volvulus L3 to L4 molt of developing.
FAAL-IN-1 (compound 32) is a selective inhibitor of fatty acyl-AMP ligase (FAAL), with a Ki of 0.7 μM for FAAL28. FAAL-IN-1 shows antimycobacterial activity[1].
Antibacterial agent 53 (example 19) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
Lyoniside is a lignan glycoside with antioxidant, allelopathic and antifungal activities, which can be isolated from the rhizomes and stems of bilberry (Vaccinium myrtillus L.). Lyoniside exhibits radical scavenging properties with an IC50 value of 23 μg/mL in DPPH assay. Lyoniside inhibits the mycelial growth of Fusarium oxysporum and Mucor hiemalis at 50 μg/mL with inhibitory rates of 78% and 80%, respectively[1].
Cephalothin sodium is a first generation cephem antibiotic with a wide range antibacterial activity, is active against gram-positive and gram-negative bacteria.
HBV-IN-34 (compound 17i) is a potent HBsAg production inhibitor. HBV-IN-34 exhibits excellent in vitro anti-HBV potency, with an EC50 of 0.018 μM and 0.044 μM for HBV DNA and HBsAg, respectively[1].
L18-MDP is a derivative of muramyl dipeptide, an antibacterial agent. L18-MDP has antibacterial activity and has potential applications in bacterial and fungal infections[1].
Diallyl Trisulfide is isolated from Garlic. Diallyl Trisulfide suppresses the growth of Penicillium expansum (MFC99 value: ≤ 90 μg/mL) and promotes apoptosis via production of reactive oxygen species (ROS) and disintegration of cellular ultrastructure. Anticancer effect[1].
Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
Xanthoquinodin A1 is an anticoccidial antibiotic having a new xanthone-anthraquinone conjugate system[1].
ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1).
Netilmicin Sulfate is an active aminoglycoside antibiotic against most Gram-negative and some Gram-positive bacteria, including certain strains resistant to gentamicin.
Ralzapastotug (AB-308) is a monoclonal antibody targeting amino acids 106-126 of the cellular prion protein PrPC[1].
Canocapavir (ZM-H1505R) has orally antiviral activity. Canocapavir is a HBV capsid inhibitor that can be used in the research of Chronic hepatitis B. [1].
NCI-B16 is a small molecule RNA binder and inhibits HCV viral replication[1].
Hexa-D-arginine TFA (Furin Inhibitor II TFA) is a stable furin inhibitor with Ki values 106 nM, 580 nM and 13.2 μM for furin, PACE4 and prohormone convertase-1 (PC1), respectively. Hexa-D-arginine TFA blocks Pseudomonas exotoxin A and anthrax toxins toxicity in vitro and in vivo[1][2][3].
AVG-233 (AVG233) is a potent, allosteric inhibitor of respiratory syncytial virus (RSV) RNA-dependent RNA polymerase (RdRp) complex, demonstrates nanomolar activity against both laboratory-adapted RSV strains and clinical RSV isolates (EC50=34-79 nM); exhibits 34% oral bioavailability and sustained high drug levels in the circulation after a single oral dose of 20 mg/kg.
Fosmanogepix (APX001) is a first-in-class and orally available broad-spectrum antifungal agent, which targets the highly conserved Gwt1 fungal enzyme. Fosmanogepix (APX001) is an N-phosphonooxymethyl prodrug which is rapidly and completely metabolized by systemic alkaline phosphatases to the active moiety, APX001A. Fosmanogepix (APX001) can be used in development for the treatment of invasive fungal infections[1][2].
Phleomycin is a wide-spectrum glycopeptide antibiotic found in Streptomyces verticillus. Phleomycin, an effective DNA-cleaving agent, binds and intercalates DNA to damage the integrity of the double helix, which is similar to Bleomycin (HY-17565A)[1].
Detiviciclovir (AM365) is an antiviral nucleoside analogue[1].
Antitrypanosomal agent 14 (Compound 1) is a T. brucei inhibitor (EC50: 0.47 μM). Antitrypanosomal agent 14 inhibits TbGSK3 with an IC50 of 12 μM. Antitrypanosomal agent 14 can be used for the research of Human African trypanosomiasis[1].
Secnidazole is a nitroimidazole anti-infective drug.
Antibacterial agent 55 (example 21) is a antibacterial agent (extracted from patent WO2013030735A1)[1].