Fluxapyroxad is a synthetic broad-spectrum fungicide for the control of fungal diseases. It works by inhibiting succinate dehydrogenase in complex II of the mitochondrial respiratory chain, resulting in inhibition of spore germination, germ tubes and mycelia growth within the fungus target species[1].
Ribostamycin (Vistamycin) is a broad-spectrum aminoglycoside antibiotic. Ribostamycin is effective against Gram-Negative and Gram-Positive bacterial infection. Ribostamycin also inhibits the chaperone activity of PDI[1][2].
Magnoflorine chloride (Magnoflorine chloride), an aporphine alkaloid found in Acoruscalamus, reduces the formation of C. albicans biofilm[1]. Magnoflorine chloride has anti-fungal, anti-antidiabetic and anti-oxidative activity[2].
Sulfamerazine D4 is a deuterium labeled Sulfamerazine. Sulfamerazine, a sulfonamide antibacterial, inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA) for binding to dihydropteroate synthesizes[1].
CpG ODN 10101, a synthetic oligodeoxynucleotide (ODN), is a toll-like receptor 9 (TLR9) agonist. CpG ODN 10101 is a potent inducer of cytokine/chemokine expression ex vivo when used in combination with HH2(VQLRIRVAVIRA-NH2). CpG ODN 10101 induces IFN- secretion from dendritic cells (DCs) and stimulates B-cells.CpG ODN 10101 has antiviral and immunomodulatory properties that can influence chronic infection with HCV[1][2].
NSC-60339, an efflux pump inhibitor and a substrate of AcrAB-TolC, is a polybasic terephthalic acid derivative studied as a potential cancer chemotherapeutic agent[1][2].
ZINC475239213 is an inhibitor of the SARS-CoV-2 Nsp14 N7-Methyltransferase (IC50: 20 μM)[1].
Cap-dependent endonuclease-IN-8 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-8 inhibits replication of orthomyxoviruses (including influenza A, influenza B and influenza C) (extracted from patent CN111410661A, compound I-196)[1].
Coreoside B (14-Hydroxycoreoside A) can be isolated from Coreopsis tinctoria Nutt. and has weak antibacterial activity[1].
Avermectin B1 (Abamectin) is a widely used insecticide and anthelmintic. IC50 Value: N/ATarget: AntiparasiticAvermectin B1 is a mixture of avermectins containing more than 80% avermectin B1a and less than 20% avermectin B1b. These two components, B1a and B1b have very similar biological and toxicological properties. The avermectins are insecticidal and antihelmintic compounds derived from various laboratory broths fermented by the soil bacterium Streptomyces avermitilis. Avermectin B1 is a natural fermentation product of this bacterium.
Licoricone is an flavonoid extracted from licorice, exhibits anti-helicobacter pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains[1].
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities[1][2][3][4][5].
APX001 (APX 001A;E1210) is a novel broad-spectrum antifungal agent that inhibits the fungal protein Gwt1, demonstrates significantly acitive MIC50 and MIC90 values of 0.004 and 0.031 ug/ml (16 strains of C. auris); inhibits the inositol acylation activity of C. albicans Gwt1p and A. fumigatus Gwt1p with IC50 of 0.3 to 0.6 uM but has no inhibitory activity against human Pig-Wp; shows significant efficacy in murine model of disseminated C. auris infection, and log reduction in CFU counts in kidney, lung, and brain tissue. Fungal Infection Phase 1 Clinical
Albomycin is an inhibitor of aminoacyl-tRNA synthetases with Trojan-horse effect. Albomycin is delivered by iron-chelator portion into bacterial through ferrichrome-specific transporter system. Albomycin combats against a wide range of Gram-positive and Gram-negative bacteria. Albomycin also serves as an efficient iron-scavenger of producer[1].
Thiostrepton is a natural cyclic oligopeptide antibiotic, is a natural product of the ribosomally synthesized and post-translationally modified peptide (RiPP) class.
Oxytetracycline dihydrate is a broad-spectrum antibiotic that acts by inhibiting protein synthesis in bacteria[1].
Chitin synthase inhibitor 2 (compound 2b) is a potent inhibitor of chitin synthase with the IC50 value of 0.09 mM and the Ki value of 0.12 mM. Chitin synthase inhibitor 2 has antimicrobial activities in vitro and shows synergistic or additive effects with fluconazole or polyoxin B[1].
Ascr#18, an ascaroside, is a hormone of nematodes. Ascr#18 is expressed during nematode development. Ascr#18 increases resistance in Arabidopsis, tomato, potato and barley to viral, bacterial, oomycete, fungal and nematode infections[1].
Valacyclovir hydrochloride is an antiviral drug used in the management of herpes simplex, herpes zoster, and herpes B. Target: HSVValacyclovir is an antiviral drug used in the management of herpes simplex, herpes zoster, and herpes B. VACV uptake was concentration dependent and saturable with a Michaelis-Menten constant and maximum velocity of 1.64 +/- 0.06 mM and 23.34 +/- 0.36 nmol/mg protein/5 min, respectively. A very similar Km value was obtained in hPEPT1/CHO cells and in rat and rabbit tissues and Caco-2 cells, suggesting that hPEPT1 dominates the intestinal transport properties of VACV in vitro . For treatment of a first episode of genital herpes, a large comparative trial has shown that valacyclovir (1 g twice a day) is as effective as acyclovir (200 mg five times a day) when given for 10 days. For treating recurrences, two trials show that valacyclovir is as effective as acyclovir (200 mg five times a day) with a treatment period of 5 days. A daily dose of 1 g of valacyclovir is as effective as 2 g daily. Valacyclovir can be administered once a day. The concentrations of acyclovir in serum and CSF were measured at steady state after 6 days of oral treatment with 1,000 mg of valacyclovir three times a day. EC50 values of PE and AC in 3T3 cells were 0.02 and 0.01 ug/ml, while values in BHK cells were 0.2 and 0.03 ug/ml. Treatment of infected immunosuppressed mice and FA and VA (b.i.d., 5.5 days) reduced the proportion with erythema from 100% to 24% and 38%, and eliminated ear paralysis, ear lesions (vesicles, etc) and death. Virus was absent from ear and brainstem by day 6, but reappeared after discontinuation in mice treated with VA.
Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 lck autophosphorylation and phosphorylation of exogenous substrates with IC50s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans[1][2][3][4].
Cefazolin is an antibiotic used for the research of a number of anti-bacterial infections. Cefazolin can be used for the prophylaxis of surgical antimicrobial. Cefazolin has anti-inflammatory effect and can attenuate post-operative cognitive dysfunction (POCD)[1].
MtUng-IN-1 (Compound 18a) is a Uracil DNA glycosylase of Mycobacterium (MtUng) inhibitor (IC50: 300 μM). MtUng-IN-1 can be used for research of cancers and infectious diseases[1].
Faltan is a dicarboximide fungicide, widely used on vines and several vegetable crops, and is also cytotoxic effect on human bronchial epithelial cells[1].
Bromodiphenhydramine (Ambodryl) is a potent antihistamine with antimicrobial property. Bromodiphenhydramine inhibits a large number of Gram negative and Gram positive bacteria. Bromodiphenhydramine can be used for cutaneous allergies research[1][2][3].
Nyasol ((-)-Nyasol) is an active compound that has antifungal, antibacterial, antileishmanial, hyaluronidase inhibition activities. Nyasol inhibits LTB4 binding to human neutrophils. Nyasol suppresses neuroinflammatory response through the inhibition of I-κB degradation in LPS (HY-D1056)-stimulated BV-2 microglial cells[1][2].
Moiramide B is a potent acetyl-CoA carboxylase (ACC) inhibitor with an IC50 value of 6 nM. Moiramide B has antibacterial activity[1].
Artemisone (Artemifone) is a potent and semi-synthetic antimalarial, inhibits P. falciparum strains, with a mean IC50 of 0.83 nM[1].
Levofloxacin-13C,d3 is the 13C- and deuterium labeled.
FPI-1523 sodium, a derivative of Avibactam, is a potent β-lactamase inhibitor, with Kds of 4 nM and 34 nM for CTX-M-15 and OXA-48, respectively. FPI-1523 sodium also inhibits PBP2, with an IC50 of 3.2 μM. FPI-1523 sodium exhibits considerable antimicrobial activity[1].
4,4'-Dicyanostilbene (compound 43) is a potent antimalarial agent against the Dd2 strain, with an EC50 of 27 nM. 4,4'-Dicyanostilbene exhibits in vivo efficacy against methicillin-resistant Staphylococcus aureus (MRSA)[1].