Mt KARI-IN-4 (compound 5c) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 5.48 μM. Mt KARI-IN-4 has inhibitory activity against Mtb H37Rv (MIC = 0.78 μM) and low cytotoxicity (HEK IC50 > 72 μg/mL)[1].
Polybia-MP1 is an antimicrobial mastoparan peptide[1].
Antiviral agent 43 (compound 16) is a potent and orally active influenza A viruses entry inhibitor. Antiviral agent 43 inhibits replications of influenza A strains VH04-H5N1 and PR8-H1N1 with EC50s of 240 nM and 72 nM, respectively[1].
Angustifoline hydrochloride, an alkaloid, can be isolated from Lupinus angustifolius L. alkaloid extract. Angustifoline hydrochloride exhibits antimicrobial activity. Angustifoline hydrochloride could have bacteriostatic effects against S. aureus, B. subtilis, E. coli, P. aeruginosa and B. thuringiensis[1].
RSV L-protein-IN-3 is a wild-type RSV polymerase inhibitor with an IC50 value of 10.4 μM and an EC50 value of 2.1 μM (against RSV). RSV L-protein-IN-3 has lesser cytotoxicity than the clinical agent, Ribavirin (HY-B0434)[1].
Myricetin 3-O-α-L-arabinopyranoside is a quercetin derivative and plant flavonoid with antioxidant, antibacterial and antiurease effects. Myricetin 3-O-α-L-arabinopyranoside inhibits A2E photooxidation-induced RPE cell death. Myricetin 3-O-α-L-arabinopyranoside is protective against retinal degeneration and protects against blue light (BL)-induced damage in RPE cells and mouse models[1].
Ledipasvir D-tartrate is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
Triadimefon is a triazole fungicide used to control powdery mildew, rusts, and other fungal pests on grains, fruit and vegetable crops, turf, shrubs, and trees. Triadimefon inhibits lanosterol 14α-demethylase, interfering with oxidative demethylation reactions in the ergosterol biosynthesis pathway of fungi, and also blocks gibberellin biosynthesis.
Nitroxoline is an antibiotic that has proven to be very effective at combating biofilm infections. Nitroxoline functions by chelating Fe2+ and Zn2+ ions from the biofilm matrix.
Arbemnifosbuvir is a nidovirus DdRp-associated nucleotidyltransferase (NiRAN) domain of non-structural protein 12 (nsp12)-interfering drugs. Arbemnifosbuvir can be used for SARS-CoVs infection research[1].
Olsalazine is an anti-inflammatory drug used in the treatment of Inflammatory Bowel Disease and Ulcerative Colitis.Target: AntibacterialOlsalazine is a derivative of salicylic acid. Inactive by itself (it is a prodrug), it is converted by the bacteria in the colon to mesalamine. Olsalazine is potent inhibitors of human intestinal macrophages chemotaxis to LTB4 with IC50 of 0.39 mM. Olsalazine (0.4 mM) inhibits the superoxide radical production generated by phorbol myristate acetate (PMA)-activated neutrophils or by xanthine-xanthine oxidase reaction by reduction of 31% and 73%, respectively. Olsalazine inhibits tumor growth in a rodent model of colorectal cancer. In 1,2-dimethylhydrazine-treated rats, Olsalazine (25 mg/kg/day) decreases number and volume of tumors by 58.17% and 62.67%, respectively. Administration of Olsalazine induces a 1.7-fold times increase in the number of apoptotic cells, companied with a reduction of 42.4% in cell proliferation rate.
RPW-24 protects C. elegans from bacterial infection by stimulating the host immune response of the nematode. RPW-24 has antibacterial activity[1].
Coronatine is a plant growth regulator produced by Pseudomonas syringae. Coronatine simulates bioactive jasmonic acid (HY-122464A) conjugates or octadecanoid signal molecules of higher plants to make plants appear pathogenic symptoms. Coronatine promotes the virulence of Pseudomonas syringae in plants by activating the signal cascade that inhibits the accumulation of Salicylic acid (HY-B0167)[1][2][3][4].
Aeroplysinin 1 ((+)-Aeroplysinin-1), a secondary metabolite isolated from marine sponges, shows potent antibiotic effects on Gram-positive bacteria and exerts antiviral activity against HIV-1 (IC50=14.6 μM). Aeroplysinin 1 has anti-inflammatory, anti-angiogenic and anti-tumor activities. Aeroplysinin 1 induces apoptosis in endothelial cells[1][2].
(±)-BI-D is a potent ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site.IC50 value: 2.4–2.9 μM(HIV-Luc infection of WT and Hdgfrp2 KO cells) [1]Target: integrase inhibitorin vitro: Approximately 2.4–2.9 μM of BI-D was required to inhibit 50% of HIV-Luc infection of WT and Hdgfrp2 KO cells, while the IC50 decreased dramatically, to 160–200 nM, in Psip1 and double-KO cells [1].
Phytol ((E)-Phytol), a diterpene alcohol from chlorophyll widely used as a food additive and in medicinal fields, possesses promising antischistosomal properties. Phytol has antinociceptive and antioxidant activitiesas well as anti-inflammatory and antiallergic effects. Phytol has antimicrobial activity against Mycobacterium tuberculosis and Staphylococcus aureus[1].
Sennoside A is an anthraquinone glycoside, found in large quantities in leaves and pods of Senna (Cassia angustifolia)[1]. Sennoside A is a HIV-1 inhibitor effective on HIV-1 replication[2].
Aurein 2.6 is an antibiotic antimicrobial peptide. Aurein 2.6 is active against Gram-positive bacterial (MIC: 25, 25, 30, 25, 30 μM for M. luteus, S. aureus, S. epidermis, S. mutans, B. subtilis)[1][2].
Methotrexate (hydrate) is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Bekanamycin is an aminoglycoside antibiotic.
nTZDpa is an antibiotic. nTZDpa is a PPARG partial agonist. nTZDpa has antibacterial activity. nTZDpa is effective against growing and persistent Staphylococcus aureus by lipid bilayer disruption[1].
Z-Gly-Gly-Leu-AMC is the substrate of ClpP1 and ClpP2, to detect the enzymatic activity in the presence of the activating peptide Z-Leu-Leu[1].
(R,R)-BAY-Y 3118 is the R-enantiomer of BAY-Y 3118. (R,R)-BAY-Y 3118 shows weak bactericidal activity[1].
MI 14 is a selective PI4KIIIβ inhibitor with IC50s of 54 nM, >100 μM, >100 μM for PI4KIIIβ, PI4KIIIα, PI4KIIα, respectively. MI 14 has antiviral activity against HCV 1b, CVB3, HRVM, HVC 2a[1].
Neuraminidase-IN-11 (15e) is a potent and selective neuraminidase (NA) inhibitor with the IC50 values of 4.7 nM, 8.46 nM and 1.5 nM against H1N1, H5N1 and H5N8 NAs respectively[1].
Clindamycin hydrochloride monohydrate is an oral protein synthesis inhibitory agent that has the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin hydrochloride monohydrate resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin hydrochloride monohydrate decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla)[1].
APJ receptor agonist 1, a biphenyl acid derivative, is a potent APJ receptor (APJ-R) agonist (EC50s 0.093 and 0.12 nM for human and rat APJ-R, respectively). APJ receptor agonist 1 displays in vitro potency to apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 has the potential for the research of heart failure[1].
HPi1 is a potent, selective and orally active antimicrobial against Helicobacter pylori with an IC50 of 0.24 μM and an MIC of 0.08-0.16 μg/mL. HPi1 is inactive against other bacteria, including the gut commensals Lactobacillus casei, Lactobacillus reuteri, and Bifidobacterium longum[1].
Lysicamine, a natural compound, possesses antibacterial, anticancer and anti-inflammation activity[1].
Thiomandelic acid is a broad spectrum inhibitor of Zinc -lactamases[1].