Transtorine is a quinoline alkaloid, found from Ephedra transitoria, with antibacterial activity[1].
Allicin (diallyl thiosulfinate), a highly potent natural antimicrobial activity substance, inhibits growth of a variety of microorganisms, among them antibiotic-resistant strains[1].
D77 is anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75. D77 inhibits HIV-1(IIIB) replication by EC50 value of 23.8 μg/ml in MT-4 cell (5.03 μg/ml for C8166 cells).IC50 value: 23.8 μg/ml (EC50, in MT-4 cell ), 5.03 μg/ml (EC50, in C8166 cell)Target: HIV-1in vitro: D77 exhibits a highly specific binding affinity to HIV-1 integrase catalytic core domain.D77 induces a dramatic concentration-dependent decrease of α-galactosidase activity compared to the D77-untreated cells. D77 reveals a significant inhibition activity against the interaction of IN with IBD.
Diamthazole (Dimazole) hydrochloride is an antifungal agent. Diamthazole hydrochloride can be used for the research of infection[1].
Pikromycin is a macrolide antibiotic that has been found in S. venezuelae and active against E. coli, S. aureus and B. subtilis[1].
Macrocarpal D is a potent antibacterial agent. Macrocarpal D is a phloroglucinol dialdehyde diterpene derivatives that can be found in the leaves of Eucalyptus macrocarpa[1].
Nevadensin is a naturally occurring selective inhibitor of human carboxylesterase 1 (hCE1) with an IC50 of 2.64 μM. Nevadensin has a variety of pharmacological effects such as anti-mycobacterium tuberculosis activities, antitussive, anti-inflammatory and anti-hypertensive[1][2].
HLI373 is an efficacious Hdm2 inhibitor. HLI373 inhibits the ubiquitin ligase activity of Hdm2. HLI373 is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents[1]. Antimalarial activity[2].
Sutezolid (PNU-100480) is an oxazolidinone antimicrobial being developed for the treatment of tuberculosis.Target: AntibacterialSutezolid is a much-awaited drug candidate for treatment of Mycobacterium tuberculosis. [1] Sutezolid is an oxazolidinone antibiotic currently in development as a treatment forextensively drug-resistant tuberculosis. Sutezolid is a linezolid analog with superior bactericidal activity against Mycobacterium tuberculosis in the hollow fiber, whole blood and mouse models. Like linezolid, it is unaffected by mutations conferring resistance to standard TB drugs. This study of sutezolid is its first in tuberculosis patients.[2]
STC314 is a small polyanion that interact electrostatically with histones. STC314 blocks disruption of lipid-bilayers by histones that inhibits the cytotoxic, platelet-activating and erythrocyte-damaging effects of histones. STC314 has anti-infective effects and can be uesd for sepsis research[1].
HCV-IN-41 (compound 4) is a highly potent hepatitis C virus (HCV) inhibitor with an EC50 value of 0.006762 nM, 5.183 nM, 1.365 nM and 142.2 nM for HCV genotype 1b, 2a, 3a and 4a, respectively. HCV-IN-41 reduces HCV RNA replication[1].
Vidofludimus (4sc-101; SC12267) hemicalcium is an orally active inhibitor for dihydroorotate dehydrogenase (DHODH) and also is a novel modulator for farnesoid X receptor (FXR). Vidofludimus hemicalcium, as an immunomodulatory agent, can be used for the research of autoimmune disorders such as inflammatory bowel disease (IBD). Vidofludimus hemicalcium also can be used for the research of fatty liver by targeting FXR[1][2][3].
Gliovirin is an antibiotic active against Pythium ultimum. Gliovirin is isolated from Gliocla-dium virens. Gliovirin may be derived from L,L-phenylalanine anhydride, which is also isolated from G. virens[1].
VT-1598 tosylate is an orally active and selective fungal inhibitor targeting CYP51. VT-1598 tosylate shows anti-fungal activity against C. auris[1][2].
BM635 is a MmpL3 inhibitor with outstanding anti-mycobacterial activity. BM635 has an MIC50 of 0.12 μM against M. tuberculosis H37Rv.
Triclabendazole(CGA89317) is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis.Target: Microtubule/TubulinTriclabendazole treatment produces percentage decreases of the fluke egg output by 15.3%, 4.3% and 36.6%, respectively, in sheep, dairy cows and heifers, these results indicate the presence of TCBZ-resistant Fasciola hepatica in sheep and cattle on this farm [1]. Triclabendazole sulphoxide (50 mg/mL) results in extensive damage to the tegument of triclabendazole-susceptible F. hepatica, whereas triclabendazole-resistant flukes shows only localized and relatively minor disruption of the tegument covering the spines [2].Triclabendazole is metabolized into a number of compounds, depending on the route of administration, plasma levels peak at 18-24 hours (Triclabendazole sulphoxide) and 36-48 hours (Triclabendazole sulphone), neither Triclabendazole nor any toher metabolites can be detected in plasma. Triclabendazole sulphoxide blocks the transport of secretory bodies from the cell body to the tegumental surface, the block occurs at the site of their formation by the Golgi complex in the cell body, in their movement through the cytoplasmic connections to the syncytium, and in their movement from the base to the apex of the syncytium. Triclabendazole binds to the colchicine binding site on the β-tubulin molecule and this has been used at the basis for evaluating the relative acitvity of Triclabendazole [3].
Transketolase-IN-4 is a potent transketolase inhibitor (IC50=3.9 μM). Transketolase-IN-4 inhibits tumor cell proliferation of SW620, LS174T, and MIA PaCa-2. Transketolase-IN-4 is a possible Mycobacterium tuberculosis DXS inhibitor, with an IC50 value of 114.1 μM[1][2].
Beludavimab (BMS 4182137; VIR 7832) is a monoclonal antibody targeting the spike glycoprotein of SARS-CoV-2. Beludavimab binds to recombinant spike protein receptor-binding domain (S-RBD) with an EC50 value of 14.9 ng/mL and a Kd of 0.21 nM[1].
Pseudane IX, a compound isolated from the leaves of Ruta angustifolia, has strong anti-HCV activity with an IC50 value of 1.4 μg/mL. Pseudane IX reduces HCV RNA replication and viral protein synthesis levels[1].
LJ 001 ((LJ-001, LJ001) is a broad-spectrum antiviral agent targeting entry of enveloped viruses, including influenza A, filoviruses, poxviruses, arenaviruses, bunyaviruses, paramyxoviruses, flaviviruses, and HIV-1; specifically intercalates into viral membranes, irreversibly inactivates virions while leaving functionally intact envelope proteins, and inhibits viral entry at a step after virus binding but before virus-cell fusion; specifically inhibits virus-cell but not cell-cell fusion
Pepstatin is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
Elipovimab is a potent broadly neutralizing HIV-1 antibody for the targeted elimination of HIV-infected cells[1]
Azadirachtin B is an limonoid isolated from seed kernels of Azadirachta indica. Azadirachtin B increases alkaline phosphatase (ALP) activity and stimulates osteoblast differentiation. Azadirachtin B is active against the Epstein-Barr virus early antigen (EBV-EA). Azadirachtin B has insecticidal, nematocidal, anticancer, anti-inflammatory, antiviral and osteogenic properties[1][2][3].
Pepticinnamin E is a Farnesyltransferase (FTase) inhibitor (IC50=42 µM). Pepticinnamin E can be used in cancer and malaria research[1][2].
Salicyl-AMS is a mycobactin biosynthesis inhibitor which can also inhibit M. tuberculosis growth in vitro under iron-limited conditions.
HCV NS4A Protein (18-40) (JT strain) is an HCV NS4A peptide, which comprised residues 18 to 40 of the NS4A protein and is known to increase the catalytic efficiency of NS3 protease[1].
Umifoxolaner is an anti-parasitic agent (veterinary).
Besifovir Dipivoxil maleate (LB80380 maleate) is an oral prodrug of LB80317. Besifovir Dipivoxil maleate (LB80380 maleate) is effective in hepatitis B virus (HBV) DNA suppression for both treatment-naive and lamivudine-resistant chronic hepatitis B (CHB) patients in preliminary studies[1][2]
ML318 is a biaryl nitrile inhibitor of PvdQ acylase with an IC50 of 20 nM by binding in the acyl-binding site. ML318 inhibits P. aeruginosa (PAO1) with an IC50 of 19 μM. ML318 prevents pyoverdine production and limits the growth of P. aeruginosa under iron-limiting conditions[1].