Lauryl-LF 11, N-terminally acylated analogue of LF11, is a peptide with antibacterial activity[1].
Danofloxacin Mesylate(CP76136-27 mesylate) is a fluoroquinolone antibacterial for veterinary use.Target: AntibacterialDanofloxacin is a synthetic antibacterial agent of the fluoroquinolone class, acts principally by the inhibition of bacterial DNA-gyrase, which is necessary for supercoiling of DNA to provide a suitable spatial arrangement of DNA within the bacterial cell. The minimum inhibitory concentration of danofloxacin against 90% (MIC90) of contemporary European and North American field isolates of Pasteurella haemolytica, Pasteurella multocida and Haemophilus somnus, the most important bacterial respiratory pathogens of cattle, is 0.125 μg/ml [1]. Danofloxacin shows protective dose (PD50) of 0.38, 0.8, 2.42 mg/kg for P. multocida, E. coli and S. choleraesuis in in vivo mouse protection assay [2].
LASV inhibitor 3.3 (LAMP1 inhibitor 3.3) is a specific inhibitor of Lassa fever virus (LASV, IC50=1.8 uM), inhibits LASV GP-mediated infection and cross-links to the LASV receptor, LAMP1, in cells; does not inhibits the GP-mediated infection of LCMV, LuJo virus (LUJV) or Junin virus (JUNV), Ebola virus (EBOV) or vesicular stomatitis virus (VSV); inhibits LAMP1 binding to LASV GP, which is cholesterol-dependent and sensitive to 3.3 inhibition; LASV inhibitor 3.3 is a competitive inhibitor of cholesterol binding to LAMP1.
Laninamivir (R 125489) is a potent influenza neuraminidase (NA) inhibitor with IC50s of 0.90 nM, 1.83 nM and 3.12 nM for avian H12N5 NA (N5), pH1N1 N1 NA (p09N1) and A/RI/5+/1957 H2N2 N2 (p57N2), respectively[1].
Antitubercular agent-20 (Compound 2d) is an orally active antitubercular agent. Antitubercular agent-20 shows excellent activity against MTB H37Rv and MDR-MTB strains (MIC: ＜0.016 µg/ml). Antitubercular agent-20 has low cytotoxicity and good tolerance in BALB/c mice[1].
SARS-CoV-2-IN-39 (compound 21) is a SARS-CoV-2 inhibitor with an EC50 of 1 μM. SARS-CoV-2-IN-39 against SARS-CoV-2 by inhibiting of SKP2 protein and stabilizing BECN1[1].
DM8966 exhibits potent antibacterial activity against gram-positive and -negative bacteria.
HIV-1 inhibitor-23 (compound 12a) is a highly potent HIV-1 non-nucleoside reverse transcriptase inhibitor, with EC50s of 24.9 nM and 10.4 nM for HIV-1 WT and HIV-1 K103N, respectively. HIV-1 inhibitor-23 has low cytotoxicity (CC50 > 221 μM) and a favorable in vitro microsomal stability[1].
Cibacron Blue 3G-A is an anthraquinone dye, inhibits the R46 β-lactamase with a Ki value of 1.2 uM[1].
Antileishmanial agent-7 (compound 23) is a potent antileishmanial agent. Antileishmanial agent-7 shows antileishmanial activity against Leishmania donovani and L-6, with IC50 values of 6.89 and 259 μM, respectively[1].
RRx-001 is a potent inhibitor of G6PD. RRx-001 shows potent antimalarial, although as a single agent, the drug sensitivity testing indicated that higher dose of RRx-001 was required to inhibited 50 % of the parasite's activity (IC50 = 0.14 ± 0.04 ug/ml).IC50 value: 0.14 ± 0.04 ug/ml [1]Target: G6PDin vitro: RRx-001 is a novel, systemically non-toxic, epigenetic anticancer agent for multiple tumour types, with activity mediated through increased nitric oxide (NO) production and PPP inhibition. [1]in vivo: RRx-001is a novel, nonexplosive molecule modified from a class of solid rocket propellants, has shown promise as a novel cancer therapeutic agent in a number of cell lines and tumor models. In mouse models, RRx-001 administered intravenously as a single agent was equipotent to cisplatin while better tolerated. RRx-001 also showed activity as a radiosensitizer in both in vitro and in vivo models. The activity of RRx-001 is thought to be associated with a nucleophilic substitution by circulating thiol compounds and covalent binding of RRx-001 to cysteinyl residues in Hb, followed by the generation of nitrogen oxides. [2]
Antifungal agent 73 (compound A32) is an antifungal agent for azole-resistant candidiasis. Antifungal agent 73 disrupts the fungal cell wall and cell membrane. Antifungal agent 73 shows potent in vivo antifungal activity against pathogenic fungi and fluconazole-resistant strains[1].
Dimetridazole-d3 (1,2-Dimethyl-5-nitroimidazole-d3) is a deuterium labeled Dimetridazole. Dmetridazole, a nitroimidazole-based antibiotic, combats protozoan infections[1].
Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease[2].
Anhydrotetracycline shows dose-dependent and potent inhibition of tetracycline destructases in vitro[1].
12-O-Methylcarnosic acid (12-Methoxycarnosic acid), a diterpene carnosic acid isolated from the acetone extract of Salvia microphylla, is an active constituent of 5α-reductase inhibition with an IC50 value of 61.7 μM. 12-O-Methylcarnosic acid inhibits proliferation in LNCaP cells. 12-O-Methylcarnosic acid has antioxidant, anti-cancer and antimicrobial activity[1][2].
Benzoic acid-d5 is a deuterium substitute for Benzoic acid. Benzoic acid is an aromatic alcohol that occurs naturally in many plants and is a common additive in food, beverages, cosmetics and other products. Benzoic acid can act as a preservative by inhibiting bacteria and fungi[1][2].
Falcipain-2/3-IN-2 (Compound 12) is a dual falcipain-2 and falcipain-3 inhibitor[1].
Antileishmanial agent-10 (Compound 7h) is an antiprotozoal agent[1].
Colistin is a polypeptide antibiotic which inhibits gram-negative bacteria by binding to lipopolysaccharides and phospholipids in the outer cell membrane of gram-negative bacteria.
Hikizimycin is a potent anthelmintic and antibacterial natural product.
Triflumezopyrim, a mesoionic insecticide, has high efficiency at a low dosage, and is mainly used to control hopper species. Triflumezopyrim mainly acts on the nicotinic acetylcholine receptor (nAChR) inhibition, which is very highly 44 efficient, rapidly effective, and nearly nontoxic to nontarget arthropods[1].
2,4′-Dichloroacetanilide is a fungistatic agent. 2,4′-Dichloroacetanilide inhibits T. asteroides with a MIC value of 6.25 μg/mL[1].
IMP-1088 is a potent, selective human N-myristoyltransferase with IC50 of less than 1 nM for both HsNMT1 and HsNMT2, inhibits Rhinoviruses (RVs) capsid myristoylation in cells; pharmacological and rapidly inhibits host-cell N-myristoylation, potently and efficiently block RV replication (IC50=17 nM) without cytotoxicity; potently blocks a key step in viral capsid assembly, to deliver a low nanomolar antiviral activity against multiple RV strains, poliovirus and foot and-mouth disease virus, and protection of cells against virus-induced killing.
2'-Deoxyuridine-d2-1 is the deuterium labeled 2'-Deoxyuridine[1]. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. A known use of 2'-Deoxyuridine is as a precursor in the synthesis of Edoxudine[2].
β-?Solamarine is an antibacterial agent[1].
HEX3 is a fragment of the adenoviral hexon. Hexon is the major capsid protein of adenovirion and is comprised of three identical polypeptide chains.
7-Methoxy-β-carboline-1-propionic acid (compound 46) is a cytotoxic and antimalarial compound. 7-Methoxy-β-carboline-1-propionic acid can be extracted from the roots of Eurycoma longifolia[1].
R-10015, a broad-spectrum antiviral compound for HIV infection, acts as a potent and selective inhibitor of LIM domain kinase (LIMK) and binds to the ATP-binding pocket, with an IC50 of 38 nM for human LIMK1[1].
UKI-1 is a novel synthetic inhibitor of the urokinase-type plasminogen activator system. It can also inhibits the invasive capacity of carcinoma cells. (Ki=0.41 μM)In vitro : A decrease of tumor cell invasion by up to 50% was achieved in both models with the SCCHN line FaDu and the cervical carcinoma line HeLa after treatment with UK1.