Tryglysin A is an antimicrobial peptide inhibits the growth of other streptococci[1].
Quinoprazine is a potent inhibitor of Vaccinia virus DNA synthesis with an IC50 value of 10 μM. Quinoprazine has antimalarial activity against Plasmodium berghei and also displays antiprion potency, significantly decreases PrPSc levels[1]-[5].
BMY-43748 is a promising antibacterial agent, exhibiting great in vitro and in vivo antibacterial activity.
Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively[1].
HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to drugs targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM[1].
BMS-626529 is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells.
Lauric acid-d3 is the deuterium labeled Lauric acid. Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively.
Tetrahydroepiberberine is a isoquinoline alkaloid isolated from Corydalis impatiens (Pall). Tetrahydroepiberberine has antifungal and selective inhibition against the PI-3 virus activities[1].
Metoprolol fumarate (CGP 2175C) is an orally active, selective β1-adrenoceptor antagonist. Metoprolol fumarate shows anti-inflammation, antitumor and anti-angiogenic properties[1][2][3].
Amitivir (LY 217896), a thiadiazole derivative, possesses broad antiviral activity against orthomyxo- and paramyxoviruses. Amitivir is effective against influenza A and B viruses[1][2].
ERDRP-0519 is an orally bioavailable small-molecule polymerase inhibitor.
Albendazole is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.Target: AntiparasiticAlbendazole, marketed as Albenza (United States), Eskazole, Zentel, Andazol and Alworm, is a benzimidazole drug used for the treatment of a variety of parasitic worm infestations. Although this use is widespread in the United States, the U.S. Food and Drug Administration (FDA) has not approved albendazole for this indication. It is marketed by Amedra Pharmaceuticals. Albendazole was first discovered at the SmithKline Animal Health Laboratories in 1972. It is a broad spectrum anthelmintic, effective against roundworms, tapeworms, and flukes of domestic animals and humans.Albendazole has been used as an anthelmintic and for control of flukes in a variety of animal species, including cattle, sheep, goats, swine, camels, dogs, cats, elephants, poultry and others. In many countries, it is very commonly used for ruminant livestock. For use in livestock, albendazole is marketed by Zoetis (formerly Pfizer Animal Health) in numerous countries (including the United States and Canada) as Valbazen in oral suspension and paste formulations; by Interchemie in the Netherlands and elsewhere as Albenol-100; by Channelle Animal Health Ltd. in the United Kingdom as Albex; by Ravensdown in New Zealand as Albendazole; etc. Although most formulations are administered orally, Ricomax (ricobendazole, or albendazole sulfoxide) is administered by subcutaneous injection.
Cefodizime is a third generation cephalosporin antibiotic with a broad spectrum of antibacterial activity. Cefodizime has no renal toxic effect, good tolerance and immune regulation activity, and is widely used in the treatment of severe infections of the respiratory and urinary tracts[1][2].
Antibacterial agent 103 (compound 7) has highly antibacterial activity against kinds of Gram-positive and -negative bacteria. Antibacterial agent 103 can be used for researching inhibition of resistance bacterial strains[1].
Procodazole is a non-specific active immunoprotective agent against viral and bacterial infections, used as a potentiator.
Anticancer agent 119 (compound 15) is an N-acylated ciprofloxacin derivative, which has certain antibacterial activity and induces ROS production to promote cancer cell apoptosis[1].
Antibacterial agent 124 (Compound 3) is a potent bacterial prolyl-tRNA synthetase (ProRS) inhibitor with an IC50 of 0.18 μM against Staphylococcus aureus ProRS (SaProRS)[1].
Amustaline (S-303) dihydrochloride, a nucleic acid-targeted alkylator, is an efficient pathogen inactivation agent for blood components containing red blood cells. Amustaline dihydrochloride has three components: an acridine anchor (an intercalator that targets nucleic acids non-covalently), an effector (a bis-alkylator group that reacts with nucleophiles), and a linker (a small flexible carbon chain containing a labile ester bond that hydrolyzes at neutral pH to yield non-reactive breakdown products)[1][2].
Deaminase inhibitor-1 is a small molecule inhibitor of APOBEC3G DNA Deaminase, with an IC50 value of 18.9 μM[1].
Itraconazole is a triazole antifungal agent.IC50 Value: N/ATarget: antifungalin vitro: Itraconazole is pharmacologically distinct from other azole antifungal agents in that it is the only inhibitor in this class that has been shown to inhibit both the hedgehog signaling pathway and angiogenesis[1, 2]. These distinct activities are unrelated to inhibition of the cytochrome P450 lanosterol 14 alpha-demethylase and the exact molecular targets responsible remain unidentified. Functionally, the antiangiogenic activity of itraconazole has been shown to be linked to inhibition of glycosylation, VEGFR2 phosphorylation and cholesterol biosynthesis pathways [2].Evidence suggests the structural determinants for inhibition of hedgehog signaling by itraconazole are recognizably different from those associated with antiangiogenic activity [3].in vivo: Nine volunteers were given either 200 mg itraconazole, or matched placebo orally once daily for 4 days. On day 4, itraconazole increased the area under the midazolam concentration-time curve from 10 to 15 times (p < 0.001) and mean peak concentrations three to four times (p < 0.001) compared with the placebo phase. In psychomotor tests, the interaction was statistically significant (p < 0.05) until at least 6 hours after drug administration. Inhibition of the cytochrome P450IIIA by itraconazole may explain the observed pharmacokinetic interaction [4].
Rivabazumab pegol is a PcrV protein antibody that can be used to study the phase II pegylated Fab of chronic Pseudomonas aeruginosa infection[1].
Acetylastragaloside I is a glycoside that can be isolated from the roots of Astragalus baibutensis. Acetylastragaloside I is the first cycloartane-type triterpene with remarkable trypanocidal activity with IC50 values of 9.5 and 5.0 μg/mL for T. brucei rhodesiense and T. cruzi, respectively. Acetylastragaloside I can be used for the research of trypanosome infection[1].
Quinoxaline-d4 is the deuterium labeled Quinoxaline[1]. Quinoxaline is a chemical compound that acts as an intermediate for anti-tuberculosis agent Pyrazinamide. Quinoxaline presents a structure that is similar to quinolone antibiotics[2].
Pam3CSK4 TFA is a toll-like receptor 1/2 (TLR1/2) agonist with an EC50 of 0.47 ng/mL for human TLR1/2[1].
Bisdionin C is a potent GH18 chitinases inhibitor, with an IC50 of 0.2 μM for A. fumigatus ChiB1 (AfChiB1). Bisdionin C inhibits HCHT (human macrophage chitotriosidase) and acidic mammalian chitinase (AMCase) with IC50s of 8.3 and 3.4 μM, respectively[1].
RSV L-protein-IN-4 (Compound C) is a noncompetitive RSV polymerase inhibitor (IC50: 0.88 μM). RSV L-protein-IN-4 shows antiviral activity against RSV strains (EC50: 0.25 μM)[1].
Phosphoglycerate kinase (PGK), namely phosphoglycerate kinase, is a glycolytic enzyme commonly used in biochemical research. Phosphoglycerate kinase can catalyze the reversible transfer of phosphate groups from 1,3-bisphosphoglycerate (1,3-BPG) to ADP to generate 3-phosphoglycerate (3-PG) and ATP. At the same time, it can also participate in gluconeogenesis, catalyzing the opposite reaction to produce 1,3BPGA and ADP. Phosphoglycerate kinase is involved in energy metabolism, interaction with nucleic acid, tumor progression, cell death and virus replication and other related processes[1].
Levofloxacin N-oxide is a minor metabolite of Levofloxacin (HY-B0330). Levofloxacin N-oxide does not exhibit significantly genotoxic risks. Levofloxacin is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria[1][2].
TCS PrP Inhibitor 13, an antiprion agent, is a cellular prion protein (PrPC) inhibitor. TCS PrP Inhibitor 13, as a protease-resistant form of prion protein (PrP-res) accumulation inhibitor, shows an IC50 value of 3 nM in both ScN2a and F3 cell lines. TCS PrP Inhibitor 13 induces Schwannoma cells apoptosis[1].
Saquinavir-d9 (Ro 31-8959-d9) is the deuterium labeled Saquinavir. Saquinavir(Ro 31-8959) is an HIV Protease inhibitor used in antiretroviral therapy. Saquinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.36 μM[1][2].