Neomycin sulfate is an aminoglycoside antibiotic used for preventing or treating bacterial infections.
Narasin sodium is a cationic ionophore and coccidiostat agent. Narasin inhibits NF-κB signaling and induces tumor cells apoptosis. Narasin sodium has antimicrobial and anticancer activity[1].
Brevinin-2 is an antimicrobial peptide derived from the skin secretions of Rana esculenta[1].
Desoxo-narchinol A is an orally active and potent anti-inflammatory agent. Desoxo-narchinol A can be isolated from the roots and rhizomes of Nardostachys jatamansi. Desoxo-narchinol A can be used for septic shock and inflammatory diseases research[1][2][3].
Octenidine is a potent antibacterial agent, possessing activity against multidrug-resistant Gram-negative pathogens. Octenidine can inhibit the expression of biofilm genes and destroy the formation of biofilms[1][3].
ALX 40-4C is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
Methylisothiazolinone hydrochloride is the constituent of the biocide Kathon CG. Methylisothiazolinone hydrochloride is an isothiazolone derivative widely used as a preservative. Methylisothiazolinone hydrochloride is also a moderate sensitizer and reacts with GSH[1][2].
R 59-022 (DKGI-I) is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 is a 5-HTR antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils[1][2][3][4].
Dinitolmide is a fodder additive for poultry, used to prevent coccidiosis infections.
Dehydroglaucine is a potent antimicrobial alkaloid[1].
Peptide 5f is an antimicrobial peptide derived from wasp venom. Peptide 5f has antimicrobial activity against bacteria and fungi. Peptide 5f has little hemolytic activity on human red blood cells [1].
Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to the R site (PKAR), with an EC50 of 6.5 nM and Kd of 8 nM in Trypanosoma brucei. Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα. Anti-parasite activity[1].
Flupyradifurone is a systemic nAChR agonist that interferes with signal transduction in the central nervous system of sucking pests. Flupyradifurone can be used as a butenolide insecticide[1].
Tetrazolast is a HCV inhibitor with the inhibitory activity ranging from 5% to 20%, extracted from patent WO2005030774.
ddUTP (2′,3′-Dideoxyuridine-5′-triphosphate) is a selective HIV and AMV reverse transcriptase inhibitor with Ki values of 0.05 µM and 1 µM, respectively. ddUTP is incorporated into the growing DNA strand primarily at dTTP sites and inhibits further elongation[1].
Verruculogen is a toxin produced mainly by Penicillium and Aspergillus spp. and causes severe tremors in affected animals. Verruculogen inhibits Ca2+-activated K+ channels. Verruculogen is an M phase inhibitor of the mammalian cell cycle[1][2][3].
Antimicrobial Compound 1 is an alkylpyridinium compound, with antimicrobial activity.
NSC309401 is an inhibitor of E. coli DHFR (IC50: 189 nM, KD: 14.57 nM)[1].
Fiacitabine(NSC 382097; FIAC; FOAC) is a selective inhibitior of DNA replication of herpes simplex virus(HSV) with IC50 values of 2.5 nM and 12.6 nM for HSV1 and HSV2, respectively. IC50 value: 2.5/12.6 nM (HSV1/2) [2]Target: HSVFIAC suppressed by 90% the replication of various strains of herpes simplex virus types 1 and 2 at concentrations of 0.0025 to 0.0126 microM. Cytotoxicity was minimal, as determined by trypan blue dye exclusion with norman Vero, WI-38, and NC-37 cell proliferation; the 50% inhibitory dose was 4 to 10 microM in a 4-day assay. FIAC was active at much lower concentrations than arabinosylcytosine, iododeoxyuridine, and arabinosyladenine. It was slightly more active against herpes simplex virus type 1 than acycloquanosine and slightly more toxic to normal cells. FIAC was about 8,000 times more active against the replication of wild-type herpes simplex virus type 1 than against a mutant strain lacking the expression of virus-specified thymidine kinase [2].
c[Arg-Arg-Arg-Arg-Dip-Dip-Dip] (Compound 8C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 12.5 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively[1].
MRV03-037 is a selective colibactin-activated peptidase (ClbP) inhibitor that blocks the genotoxic effect of Colibactin (HY-145930) on eukaryotic cells. MRV03-037 prevents gut bacterial genotoxin production[1].
UK-2A (Antibiotic UK 2A) is a potent antifungal antibiotic. UK-2A shows antifungal activity[1][2].
Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity.
ML267 a potent Sfp phosphopantetheinyl transferase (PPTases) inhibitor with an IC50 of 0.29 μM. ML267 also inhibits AcpS-PPTase with an IC50 of 8.1 μM. ML267 possesses specific Gram-positive-targeted bactericidal activities[1].
TBA-354 is a potent anti-tuberculosis compound; maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates.IC50 value:Target: Anti-tuberculosis agentin vitro: TBA-354 is narrow spectrum and bactericidal in vitro against replicating and nonreplicating Mycobacterium tuberculosis, with potency similar to that of delamanid and greater than that of PA-824. TBA-354 maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates [1]. TBA-354 is 5 to 10 times more potent than PA-824, but selected mutants are cross-resistant to PA-824 and delamanid. TBA-354 is 2 to 4 times more potent than PA-824 when combined with bedaquiline, and when administered at a dose equivalent to that of PA-824, TBA-354 demonstrated superior sterilizing efficacy [2].in vivo: TBA-354 has high bioavailability and a long elimination half-life. In vitro studies suggest a low risk of drug-drug interactions. Low-dose aerosol infection models of acute and chronic murine tuberculosis reveal time- and dose-dependent in vivo bactericidal activity that is at least as potent as that of delamanid and more potent than that of PA-824.
Hygromycin B is an aminoglycoside antibiotic active against prokaryotic and eukaryotic cells.
4aα,7α,7aα-Nepetalactone exhibits antibacterial activity, and inhibits Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Salmonella typhi and Enterococcus faecalis.
Rhuscholide A is a benzofuran lactone that shows significant anti-HIV-1 activity, with an EC50 of 1.62 μM[1].
(E/Z)-4,4'-Dicyanostilbene is the inactive isomer of 4,4'-Dicyanostilbene (HY-W112166A), and can be used as an experimental control. 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].
Ajoene, a garlic-derived compound, is an antithrombotic and antifungal agent. Ajoene inhibits proliferation and induces apoptosis of human leukaemia CD34-negative cells including HL-60, U937, HEL and OCIM-I. Anticancer activities[1][2].