ACSS2-IN-1 is a potent ACSS2 inhibitor for the treatment of cancer.ACSS2-IN-1 (Cpmpound 1) is a potent ACSS2 inhibitor. ACSS2-IN-1 inhibits ACSS2 with the IC50 of 0.01 nM to <1 nM. ACSS2-IN-1 can be used for the research of cancer[1].
Tenofovir-C3-O-C12-trimethylsilylacetylene (ammonium) exhibits substantially longer t1/2 values than tenofovir in human liver microsomes, potent anti-HIV activity in vitro, and enhances pharmacokinetic properties in vivo.
Sulfamethazine sodium (Sulfadimidine sodium) is an antimicrobial that is widely used to treat and prevent various animal diseases (such as gastrointestinal and respiratory tract infections). In China and the European Commission, the maximum residue level for Sulfamethazine sodium in animal product is set at 100 µg/kg[1][2].
Antistaphylococcal agent 1 is an antistaphylococcal therapeutic agent.
Quinoxyfen (DE-795) is a powdery mildew fungicide[1].
Antibacterial agent 54 (example 20) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
HIV-1 integrase inhibitor 4 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC50 of 3.7 nM.
4(3H)-Quinazolinone is a building block in chemical synthesis. Biologically active nitrogen heterocyclic compounds. Possesses a wide spectrum of biological properties like antibacterial, antifungal, anticonvulsant, anti-inflammatory, anti-HIV, anticancerous and analgesic activities[1][2].
Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum Crantz with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with Kis of 3.4 µM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca2+ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities[1][2][3].
N-3-Oxo-tetradecanoyl-L-homoserine lactone (oxo-C14-HSL) is a rhizobacterial inducer and can improve basic defense against nematodes[1].
NITD-349 is an MmpL3 inhibitor that shows highly potent anti-mycobacterial activity with MIC50 of 23 nM against virulent Mycobacterium tuberculosis H37Rv.
Cadrofloxacin (Caderofloxacin; CS-940), a orally active fluoroquinolone, is effective against aerobic/anaerobic Gram-positive and Gram-negative bacteria. Cadrofloxacin can be used for the research of infectious diseases[1][2][3].
AT-9010 triethylamine, a triphosphate active metabolite of AT-527, is a potent inhibitor of NiRAN (a function essential for viral replication). AT-9010 triethylamine can inhibit SARS-CoV-2 replication[1].
16,17-Dihydroheronamide C has antifungal activity and is designed as probe for the mode-of-action analysis of heronamide C[1].
Lomtegovimab (BI 767551) is a humanized anti-SARS-COV-2 spike glycoprotein monoclonal antibody. Lomtegovimab binds and neutralizes SARS-CoV-2. Lomtegovimab shows antiviral efficacy. Lomtegovimab has the potential for the research of COVID-19[1][2].
Buparvaquone is a hydroxynaphthoquinone antiprotozoal drug related to parvaquone and atovaquone.
Phosphoglycolohydroxamic acid is a potent aldolase and triose-phosphate isomerase inhibitor. Phosphoglycolohydroxamic acid can be used in the research of antibacterial and antifungal area[1][2].
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].
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.
Hexachlorophene(Hexachlorofen) is a potent KCNQ1/KCNE1 potassium channel activator with EC50 of 4.61 ± 1.29 μM; also is an inhibitor of Wnt/beta-catenin signaling.IC50 value: 4.61 ± 1.29 μM(EC50) [1]Target: KCNQ1 activatorin vitro: HCP potently increases the current amplitude of KCNQ1/KCNE1 expressed by stabilizing the channel in an open state with an EC(50) of 4.61 ± 1.29 μM. Further studies in cardiomyocytes showed that HCP significantly shortens the action potential duration at 1 μM. In addition, HCP is capable of rescuing the loss of function of the LQTs mutants caused by either impaired activation gating or phosphatidylinositol-4,5-bisphosphate (PIP2) binding affinity [1]. Hexachlorophene antagonized CRT that was stimulated by Wnt3a-conditioned medium by promoting the degradation of beta-catenin. hexachlorophene represses the expression of cyclin D1 [2]. Triclosan and hexachlorophene inhibited both ecFabI and saFabI. hexachlorophene prevented the formation of a stable FabI-NAD(P)(+)-drug ternary complex [3].
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.