Boc-AAG-pNA is a glycine endopeptidase substrate. Boc-AAG-pNA can be used to test the amidase activity glycine endopeptidase[1].
Sulfamethazine is a sulfonamide antibacterial.Target: AntibacterialSulfamethazine is an antibiotic used to treat bronchitis, prostatitis and urinary tract infections. Sulfamethazine blocks the synthesis of dihydrofolic acid by inhibiting dihydropteroate synthase. In addition, sulfamethazine is a structural analog and competitive antagonist of para-aminobenzoic acid (PABA) and can inhibit normal bacterial utilization of PABA for the synthesis of folic acid, which is an important metabolite in DNA synthesis [1, 2].
SC75741 is a broad and efficient NF-κB inhibitor with an IC50 of 200 nM for p65[1]. SC75741 blocks influenza viruses (IV) replication in non-toxic concentrations. SC75741 impairs DNA binding of the NF-κB subunit p65, resulting in reduced expression of cytokines, chemokines, and pro-apoptotic factors. SC75741 subsequently inhibits caspase activation and blocks caspase-mediated nuclear export of viral ribonucleoproteins[2].
Emetine dihydrochloride hydrate is an anti-protozoal drug previously used for intestinal and tissue amoebiasis.
NBD-557 is a potentially HIV-1 inhibitor.IC50 Value: Target: HIVNBD-557, is small molecule organic compounds with drug-like properties. It showed potent cell fusion and virus-cell fusion inhibitory activity at low micromolar levels. A systematic study showed that NBD-557 target viral entry by inhibiting the binding of HIV-1 envelope glycoprotein gp120 to the cellular receptor CD4 but did not inhibit reverse transcriptase, integrase, or protease, indicating that they do not target the later stages of the HIV-1 life cycle to inhibit HIV-1 infection. NBD-557 potent inhibitors of both X4 and R5 viruses tested in CXCR4 and CCR5 expressing cell lines, respectively, indicating that its anti-HIV-1 activity is not dependent on the coreceptor tropism of the virus. A surface plasmon resonance study, which measures binding affinity, clearly demonstrated that NBD-557 bind to unliganded HIV-1 gp120 but not to the cellular receptor CD4. NBD-557 was active against HIV-1 laboratory-adapted strains including an AZT-resistant strain and HIV-1 primary isolates, indicating that NBD-557 can potentially be further modified to become potent HIV-1 entry inhibitors.
Antibacterial agent 116 is a benzophenone-containing salicylanilide compound. Antibacterial agent 116 has potent antibacterial activity by inhibiting the peptidoglycan formation. Antibacterial agent 116 is used as a photoaffinity probe to label Acinetobacter baumannii penicillin-binding protein (PBP1b), block the propagation pathway to disrupt the growth of peptidoglycan chain[1].
Bacitracin Zinc is a dephosphorylation of the C55-isoprenyl pyrophosphate interference for inhibition of cleavage of Tyr from Met-enkephalin with IC50 of 10 μM.Target: AntibacterialBacitracin is a mixture of related cyclic polypeptides produced by organisms of the licheniformis group of Bacillus subtilis var Tracy. Its unique name derives from the fact that the bacillus producing it was first isolated in 1943 from a knee scrape from a girl named Margaret Tracy. As a toxic and difficult-to-use antibiotic, bacitracin doesn't work well orally. However, it is very effective topically. Bacitracin is synthesised via the so-called nonribosomal peptide synthetases (NRPSs), which means that ribosomes are not involved in its synthesis [1, 2].
Pentosan Polysulfate is a semi-synthetic drug used to treat various medical conditions including thrombi and interstitial cystitis.
Cefilavancin (TD-1792) is a potent multivalent glycopeptide-cephalosporin heterodimer antibiotic with effective activity against Gram-positive bacteria. Cefilavancin has been used to research skin infections[1][2][3].
Enrofloxacin is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
Velpatasvir-d7 (GS-5816-d7) is the deuterium labeled Velpatasvir. Velpatasvir (GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.16 μM[2].
β-Lactamase-IN-6 is a β-Lactamase inhibitor that shows high antibacetrial activity.
Kuwanon G is a flavonoid isolated from Morus alba, acts as a bombesin receptor antagonist, with potential antimicrobial activity[1][2].
4-Methoxycinnamaldehyde (p-Methoxycinnamaldehyde), an active constituent of Agastache rugosa, exhibits cytoprotective activity against respiratory syncytial virus (RSV) in human larynx carcinoma cell line. 4-Methoxycinnamaldehyde effectively inhibits cytopathic effect of RSV with an estimated IC50 of 0.055 μg/mL[1].
A potent TLR7/8 agonist and cytokine inducer; stimulates type I interferon (IFN) and other cytokines such as TNF-alpha, IL-12, and IFN-gamma from rat peripheral blood mononuclear cells; induces IL-12 and COX-2 expression in mDC from HIV+ and HIV- individuals, and inhibits H3N2 influenza viral replication in the nasal cavity; potentiates NK cytotoxicity, and shows antitumor effects in scid/B6 mice and scid/NOD mice.
Fluoroquinolonic acid is a bacteriostatic antibiotic. Fluoroquinolonic acid has broad-spectrum activity against Gram-positive and Gram-negative bacteria[1].
Mefloquine hydrochloride is a quinoline antimalarial drug that is structurally related to the antiarrhythmic agent quinidine. IC50 Value: 1 microM ( for K+ channel) [1]Target: AntiparasiticMefloquine is widely used in both the treatment and prophylaxis of Plasmodium falciparum malaria. MQ can induces oxidative stress in vitro. Evidence indicates that reactive oxygen species (ROS) may be used as a therapeutic modality to kill cancer cells [2].in vitro: Mefloquine inhibitedKvLQT1/minK channel currents with an IC50 value of approximately 1 microM. Mefloquine slowed the activation rate of KvLQT1/minK and more block was evident at lower membrane potentials compared with higher ones. HERG channel currents were about 6-fold less sensitive to block by mefloquine (IC50 = 5.6 microM). Block of HERG displayed a positive voltage dependence with maximal inhibition obtained at more depolarized potentials [1]. MQ has a highly selective cytotoxicity that inhibits PCa cell growth. MQ-mediated ROS simultaneously downregulated Akt phosphorylation and activated extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK) and adenosine monophosphate-activated protein kinase (AMPK) signaling in PC3 cells [2]. in vivo: Pregnant rats were treated orally with AS (15 and 40 mg/kg body weight (bwt)/day), MQ (30 and 80 mg/kg bwt/day) and AS/MQ (15/30 and 40/80 mg/kg bwt/day) on days 9-11 post coitum (pc). The dams were euthanized on day 12 pc and gestational and embryos histological parameters were evaluated [3].Clinical trial: Activity of Mefloquine Against Urinary Schistosomiasis . Phase 2
Dihydroartemisinic acid (Dihydroqinghao acid), isolated as a natural product from Artemisia annua, is a biosynthetic precursor to the antimalarial agent Artemisinin[1].
Clavulanate potassium is a potent β-lactamase inhibitor and acts as an antibiotic[1][2].
Clemastanin B, a lignin, has potent anti-influenza activities by inhibiting the virus multiplication, prophylaxsis and blocking the virus attachment. Clemastanin B targets viral endocytosis, uncoating or ribonucleoprotein (RNP) export from the nucleus. Clemastanin B has antioxidant and anti-inflammatory activities[1][2][3].
HBV-IN-32 is a potent cccDNA (covalently closed circular DNA) inhibitor. HBV-IN-32 shows anti-HBV activity with an IC50 value of 0.14 µM for HBsAg. HBV-IN-32 inhibits cell growth[1].
Nifurtoinol is a nitrofuran-derivative antibiotic with antibacterial effects. Nifurtoinol can be used for the research of urinary tract infections[1][2].
Polygalasaponin XXXI (Onjisaponin F) is an effective adjuvant for intranasal administration of influenza Influenza hemagglutinin (HA) vaccine to protect influenza virus infection[1].
Homoembelin is an antimicrobial compound and has the potential for MDR bacterial infection research[1].
Cycloheximide (Naramycin A) is an eukaryote protein synthesis inhibitor, with IC50s of 532.5 nM and 2880 nM for protein synthesis and RNA synthesis in vivo, respectively.
o-Vanillin (2-Vanillin) is a nature product, could be extracted from Vanilla planifolia, Pinus koraiensis fruit. o-Vanillin is a potent antifungal agent. o-Vanillin inhibits the growth of mycelia by disrupting the integrity of cell walls and cell membranes. o-Vanillin inhibits Doxorubicin (HY-15142A)- and 4-hydroperoxycyclophosphamide-induced NF-κB activation[1][2].
Rezafungin acetate (Biafungin acetate) is a next-generation, broad-spectrum, and long-lasting echinocandin. Rezafungin acetate shows potent antifungal activity against Candida spp., Aspergillus spp., and Pneumocystis spp.[1][2].
N-Acetyltyramine is a quorum-sensing inhibitor (QSI) compound produced by V. alginolyticus M3-10. N-Acetyltyramine is capable of inhibiting the QS of C. violaceum ATCC 12472. N-acetyltyramine reverses resistance in Doxorubicin-resistant leukemia P388 cells[1][2].
Nargenicin A1 is an antibiotic agent against various Gram-positive bacteria. Nargenicin A1 shows anti-inflammatory activity. Nargenicin A1 protects HINAE cells against Tacrolimus (HY-13756)-induced DNA damage and apoptosis. Nargenicin A1 can also be used for the research of acute myeloid leukemia[1].
LHF-535 is an antiviral agent extracted from patent WO2013123215A2, Compound 38, has EC50s of <1 μM, <1 μM, <1 μM, and 1-10 μM for Lassa, Machupo, Junin, and VSVg virus, respectively[1].