Antifection

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  1. HIV-1 attachment inhibitor

    BMS-663068 tris is an HIV-1 attachment inhibitor in development for the treatment of HIV-1 infection.
  2. HIV protease inhibitor

    Fosamprenavir Calcium Salt is a phosphate ester prodrug of the antiretroviral protease inhibitor amprenavir, with improved solubility over the parent molecule and a potential for reduced pill burden on current dosing regimens; GW433908G is the calcium salt of the prodrug.
  3. HIV protease inhibitor

    Tipranavir, a nonpeptidic HIV protease inhibitor (NPPI), inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-PI-resistant HIV-1 isolates.
  4. Protein synthesis inhibitor

    Blasticidin S is a nucleoside antibiotic isolated from Streptomyces griseochromogenes. Blasticidin S is a potent inhibitor of protein synthesis in both prokaryotic and eukaryotic cells.
  5. Topoisomerase inhibitor

    Zabofloxacin hydrochloride (DW-224a) is a novel fluoronaphthyridone quinolone that is considered a potent antibacterial candidate for clinical trials.
  6. efflux pump inhibitor

    PAβN dihydrochloride (MC-207110 dihydrochloride) is an efflux pump inhibitor.
  7. SDHI Inhibitor

    Boscalid is a succinate dehydrogenase inhibitor that exhibits significant antifungal activity. By binding to the ubiquinone-binding site of mitochondrial complex II in fungi, Boscalid disrupts ATP production and aerobic respiration, effectively controlling a range of plant fungal diseases, such as gray mold, sclerotinia rot, and powdery mildew. In addition to its agricultural applications, research indicates that Boscalid induces apoptosis and alters lipid metabolism while causing mitochondrial dysfunction, oxidative stress, and ROS accumulation in zebrafish models. Furthermore, it demonstrates chronic toxicity and impacts foraging behavior in honeybees, alongside exhibiting genotoxic and cytotoxic effects in cellular systems.
  8. Bacterial Inhibitor

    Citrinin is a mycotoxin known for its role as a bacterial inhibitor. It exhibits a range of biological activities, including the regulation of immune cell populations, induction of apoptosis and autophagy in immune cells, and modulation of toll-like receptor expression and cytokine production. Citrinin also induces oxidative stress, leading to apoptosis in oocytes, while low doses demonstrate neuroprotective effects against glutamate-induced excitotoxicity in rat cortical neurons. This compound's diverse mechanisms make it a valuable reagent for research in immunology, neurobiology, and antibacterial applications.
  9. Virus Protease Inhibitor

    Anthraquinone acts primarily as a viral protease inhibitor, exhibiting multifaceted biological activities including anticancer, anti-inflammatory, diuretic, anti-arthritic, antifungal, antibacterial, antimalarial, and antioxidant properties. This compound plays a crucial role in plant metabolism by impacting the electron transport chain, thereby inhibiting energy transfer during photosynthesis. Additionally, anthraquinone intercalates into DNA and inhibits topoisomerase II, leading to cell death through apoptosis. This diverse profile supports its applications in various fields of chemical and biological research.
  10. Fungal Inhibitor

    Mancozeb is a potent fungicide that operates primarily by inhibiting fungal growth in a variety of agricultural products, including cereals, vegetables, fruits, and ornamental plants. In addition to its antifungal properties, Mancozeb has been shown to activate the Keap1/Nrf2 signaling pathway, leading to liver damage in mice. It alters cellular metabolism through the upregulation of lactate dehydrogenase and cytochrome c, resulting in induced apoptotic pathways, particularly in ovarian cells. This compound is of significant interest in studies related to reproductive toxicity and cellular metabolism.
  11. HIV Protease Inhibitor

    Indinavir is a selective inhibitor of HIV-1 protease, displaying a Ki value of 0.54 nM, making it a potent antiviral agent. In addition to its primary role in HIV treatment, Indinavir has demonstrated anticancer properties by inhibiting matrix metalloproteinases (MMPs) and promoting anti-angiogenic effects, alongside inducing apoptosis in cancer cells. Furthermore, Indinavir has shown inhibitory activity against the SARS-CoV 3CL protease, expanding its potential applications in viral research.
  12. Bacterial/Fungal Inhibitor, Preservative Agent

    Methylisothiazolinone is a potent bacterial and fungal inhibitor with significant applications as a preservative agent. It activates matrix metalloproteinases (MMPs) in human bronchial epithelial cells, leading to apoptosis and an inflammatory response. Additionally, this compound is linked to the exacerbation of atopic dermatitis in mice through the disruption of Th2/Th17-related immune responses. Furthermore, Methylisothiazolinone has been shown to induce mitochondrial damage in the endothelium of rat cerebral blood vessels, highlighting its potential impact on vascular health.
  13. Bacterial Inhibitor

    Oligomycin B is an antibiotic derived from marine Streptomyces, primarily acting as an inhibitor of ATP synthase in eukaryotic cells. Its mechanism of action leads to a decrease in ATP production, resulting in cellular stress and the induction of apoptosis. Oligomycin B is widely utilized in research focused on mitochondrial function, energy metabolism, and apoptosis-related studies.
  14. Bacterial Inhibitor

    Lactoferrin (17-41) acetate is a peptide derived from residues 17-41 of bovine lactoferrin, primarily functioning as a bacterial inhibitor. It exhibits potent antimicrobial activity against various microorganisms, including Gram-positive and Gram-negative bacteria, viruses, protozoa, and fungi. In addition to its antimicrobial properties, Lactoferrin (17-41) acetate also demonstrates antitumor activities, making it a valuable reagent in studies related to infection control and cancer research.
  15. Bacterial Transcription Inhibitor

    GKL003 is a bacterial transcription inhibitor that targets the interaction interface of RNA polymerase (RNAP) and the sigma factor, with a Ki value of 5.79 nM. By specifically binding to the RNAP β' clamp helix region at the σA factor binding site, GKL003 disrupts the formation of the RNAP holoenzyme and inhibits bacterial transcription initiation complexes. This compound effectively inhibits the growth of both Gram-positive and Gram-negative bacterial strains, including those that are drug-resistant, making it a valuable tool for research applications in microbiology and antibiotic resistance studies.
  16. DENV Polymerase Inhibitor

    NITD-2 is a selective inhibitor of dengue virus (DENV) polymerase, specifically targeting the RNA-dependent RNA polymerase (RdRp) to impede RNA elongation. This compound exhibits potent antiviral activity against DENV, making it a valuable tool for research focused on understanding dengue virus replication and developing therapeutic strategies. Its limited ability to penetrate cell membranes can be an important consideration for in vitro experimental design.
  17. Dengue Virus Protease Inhibitor

    SP-471P is a potent inhibitor of the dengue virus (DENV) protease, exhibiting EC50 values of 5.9 μM, 1.4 μM, 5.1 μM, and 1.7 μM against DENV1, DENV2, DENV3, and DENV4, respectively, with a CC50 exceeding 100 μM. This compound effectively reduces DENV viral RNA synthesis, making it a valuable tool for research in dengue virus biology and antiviral therapeutic development.
  18. Bacterial Inhibitor

    Mequindox is an antimicrobial agent that functions as a bacterial inhibitor by selectively targeting and inhibiting DNA synthesis. This compound demonstrates significant genotoxic and carcinogenic effects in murine models, making it a valuable tool for studying bacterial resistance mechanisms and the potential impacts of antimicrobial agents on genetic material. Its applications extend to research on the safety and efficacy of antimicrobial treatments in various biological systems.
  19. Bacterial Inhibitor

    Silver sulfadiazine is a sulfonamide antibiotic that functions as a bacterial inhibitor through dual mechanisms. The sulfa moiety inhibits bacterial folate absorption, thereby disrupting essential DNA synthesis. Additionally, silver ions released from silver sulfadiazine bind to and disrupt DNA structures, preventing bacterial DNA replication. This compound is widely used in research applications focusing on bacterial growth inhibition and antimicrobial studies.
  20. Bacterial Inhibitor

    Fenvalerate is a highly effective bacterial inhibitor, primarily functioning as a protein phosphatase 2B (calcineurin) inhibitor, with an IC50 of 2-4 nM for PP2B-Aα. As a pyrethroid ester, it exhibits significant insecticidal and acaricidal properties. This compound is utilized in various research applications to study protein phosphatase signaling pathways and to explore potential therapeutic targets in bacterial infections.
  21. Calcineurin Phosphatase Inhibitor

    Dibefurin is a potent inhibitor of calcineurin phosphatase, a critical regulator of calcium-dependent signaling pathways. This fungal metabolite has demonstrated significant biological activity in various cellular processes, making it a valuable tool for studying immune response and neuronal signaling. Its application extends to research focused on autoimmune diseases and neurodegenerative disorders, where calcineurin activity plays a pivotal role.
  22. IMPase Inhibitor

    L-671776 is a non-competitive inhibitor of inositol monophosphatase (IMPase), a critical enzyme in the phosphoinositide signaling pathway. This compound, derived from the fungal strain ATCC 20928B, exhibits significant potential for modulating inositol levels and can be utilized in studies investigating mood disorders, neurodegenerative diseases, and other conditions linked to inositol metabolism. Its application in biochemical research can help elucidate the role of IMPase in cellular signaling processes.
  23. PTP1B Inhibitor

    Deoxyfunicone is a potent inhibitor of protein tyrosine phosphatase 1B (PTP1B), demonstrating an IC50 value of 24.3 µM through direct active site binding. This secondary fungal metabolite exhibits notable anti-inflammatory properties, making it a valuable tool for research into metabolic regulation and the treatment of inflammatory diseases. Its mechanism of action positions it as a significant compound for studies focused on diabetes and obesity-related conditions.
  24. HIV Integrase Inhibitor

    Equisetin is an N-methylserine-derived acyl tetramic acid that functions as a potent HIV integrase inhibitor. It specifically interferes with the activity of HIV-1 integrase and demonstrates notable inhibition of 11β-HSD1 and Dnp-stimulated ATPase, with an IC50 of approximately 8 nmol per mg of protein. Additionally, Equisetin exhibits significant antibacterial properties, anti-inflammatory effects, and potential benefits in managing lipid-associated disorders while also showcasing cytotoxic activity. This compound is valuable for research applications focused on HIV treatment and the exploration of antimicrobial and anti-inflammatory mechanisms.
  25. HIV Protease Inhibitor

    Indinavir sulfate ethanolate is a selective inhibitor of HIV-1 protease, demonstrating a potent Ki of 0.54 nM for the target enzyme. Beyond its antiviral activity, this compound has shown potential in anticancer research through the inhibition of MMPs-2 activation, anti-angiogenic effects, and promotion of apoptosis. Additionally, Indinavir sulfate ethanolate acts as an inhibitor of the SARS-CoV 3CLpro enzyme, highlighting its diverse biological activity and relevance in multiple research applications.
  26. Bacterial Inhibitor

    (Z)-Methyl tetradec-9-enoate functions as a bacterial inhibitor, primarily exerting its cytotoxic effects in human prostate cancer LNCaP cells through the induction of apoptosis and necrosis. Isolated from S. repens fruit extract, this compound also demonstrates antifungal activity, effectively inhibiting the germination of Candida albicans with a minimum inhibitory concentration (MIC) of 9 μM in vivo. Its applications extend to studies in both cancer research and microbiology, making it a valuable reagent for understanding cellular processes and developing therapeutic strategies.
  27. CYP51 Inhibitor

    Antifungal agent 136 is an irreversible inhibitor of fungal lanosterol 14α-demethylase (CYP51). It demonstrates potent antifungal activity against drug-resistant strains of Candida albicans and effectively downregulates IL-6 expression. This compound holds potential for research applications in the fields of fungal infection and inflammatory diseases.
  28. Fungal Inhibitor

    Filipin III is a pentaene macrolide antifungal antibiotic featuring a 28-membered ring, primarily derived from various Streptomyces species including S. filipinensis, S. avermitilis, and S. miharaensis. This compound targets membrane sterols, leading to significant alterations in membrane structure, which disrupts fungal cell integrity. Filipin III is widely utilized in research to study fungal infections and to explore mechanisms of antifungal resistance.
  29. Actin Polymerization Inhibitor

    Latrunculin B is an actin polymerization inhibitor commonly derived from marine algae. It modulates the electrophysiological properties of pulmonary veins and has been shown to reduce stretch-induced arrhythmias. Additionally, Latrunculin B exhibits antifungal and antiprotozoal activities, making it a valuable reagent for research in cell biology and pharmacology.
  30. Fungal Inhibitor

    Phenazine-1-carboxylic acid functions as a potent antifungal agent, targeting fungal pathogens effectively. In addition to its antifungal properties, it demonstrates anticancer activity by promoting apoptosis in cancer cells through the modulation of reactive oxygen species (ROS) generation. Phenazine-1-carboxylic acid also influences cytokine expression, upregulating IL-8 and ICAM-1 while inhibiting RANTES and MCP-1 release, indicating potential immunomodulatory effects. This compound is valuable for research in anti-infection strategies, cancer therapy, and immune response modulation.
  31. Fungal Inhibitor

    Sakuranetin is a cherry flavonoid phytoalexin that acts as a potent fungal inhibitor. It exhibits strong antifungal properties, along with notable anti-inflammatory and antioxidative activities. Additionally, Sakuranetin has demonstrated efficacy in ameliorating LPS-induced acute lung injury, making it a valuable compound for research in inflammation and respiratory disorders.
  32. Tropone Derivatives; Tyrosinase Inhibitor; Virus Inhibitor; Funga Inhibitor

    Tropolone is a seven-membered non-benzenoid aromatic compound recognized for its role as a tyrosinase inhibitor, exhibiting an IC50 value of 0.4 μM. This compound demonstrates significant anti-viral and anti-fungal properties, making it effective in a variety of therapeutic applications. Additionally, Tropolone shows enhanced effects when used in conjunction with nucleos(t)ide analogs. Its potential for research in osteosarcoma emphasizes its importance in the exploration of new treatments.
  33. Antifungal Antibiotic/Complex III Inhibitor

    Myxothiazol is an antifungal antibiotic that acts as an inhibitor of mitochondrial electron transport chain complex III (bc1 complex). It demonstrates potent antifungal activity against various yeasts and fungi, exhibiting effective growth inhibition at concentrations ranging from 0.01 to 3 μg/ml. This compound is valuable for research applications focused on mitochondrial function and the mechanisms of antifungal resistance.
  34. β-1,3-Glucan Inhibitor

    Ibrexafungerp is an orally active β-1,3-glucan synthesis inhibitor with demonstrated antifungal properties. Its mechanism targets the cell wall biosynthesis pathway of fungi, making it valuable in research on Candida and Aspergillus infections. This compound is a promising candidate for studies focused on antifungal resistance and the development of new antifungal therapies.
  35. Antibacterial Agent/eEF2K Inhibitor

    Cefatrizine is a broad-spectrum cephalosporin antibiotic that primarily targets bacterial infections while also acting as an eEF2K inhibitor. This compound exhibits anti-proliferative activity in human breast cancer cells, inducing endoplasmic reticulum stress and subsequent cell death. Cefatrizine is a valuable reagent for research applications in understanding mechanisms of cancer therapy and exploring antibacterial efficacy.
  36. Ras Inhibitor

    (-)-Rasfonin is a natural fungal secondary metabolite that acts as an inhibitor of small G protein Ras. It exhibits significant biological activities, including the induction of apoptosis, necrosis, and autophagy in ACHN cells, a renal carcinoma cell line. This compound is instrumental for research focused on cellular death pathways and therapeutic strategies targeting Ras-mediated signaling in cancer.
  37. Superoxide Anion Inhibitor

    Tanzawaic acid B is a potent inhibitor of superoxide anion production, derived from the fungal source Penicillium citrinum. This compound has been demonstrated to mitigate oxidative stress by targeting superoxide radicals, making it valuable for research in oxidative damage and related pathologies. Its biological activity provides a useful tool for studying the effects of reactive oxygen species in various cellular models.
  38. HIV-1 RT Inhibitor

    Apricitabine is a selective inhibitor of HIV-1 reverse transcriptase (RT) with a Ki value of 0.08 μM. It also exerts inhibitory effects on DNA polymerases α, β, and γ, with corresponding Ki values of 300 μM, 12 μM, and 112.25 μM. Demonstrating significant antiretroviral efficacy and favorable tolerability, Apricitabine shows a reduced potential for resistance development in patients with antiretroviral-naive HIV infection. This compound is applicable for research in the mechanisms of HIV-1 replication and antiviral drug development.
  39. DENV Inhibitor

    DENV-IN-4 is a potent inhibitor of Dengue Virus (DENV), exhibiting an EC50 value of 4.79 µM in Vero cells with a selectivity index greater than 20.9. This compound effectively reduces the expression levels of DENV2 in a concentration-dependent manner and inhibits RNA-dependent RNA polymerase (RdRp) enzymatic activity. DENV-IN-4 is valuable for research applications focused on understanding DENV pathogenesis and developing antiviral therapies.
  40. DNA Synthesis/HSV/HIV-1 Inhibitor

    16,16-Dimethyl prostaglandin A1 is a prostaglandin analog that primarily inhibits DNA synthesis. It demonstrates significant antiviral activity by reducing viral replication in both herpes simplex virus (HSV) and HIV-1 infection models. This compound serves as a valuable tool for research focused on cancer biology and viral pathogenesis.
  41. DENV/ZIKV Inhibitor

    Antiviral agent 36 is a potent inhibitor of dengue virus (DENV) and Zika virus (ZIKV), demonstrating effective antiviral activity. It inhibits viral replication with EC50 values of 100 nM for ZIKV-FLR, 90 nM for ZIKV-HN16, 210 nM for DENV-2, and 120 nM for DENV-3. This compound serves as a valuable tool for research focused on the therapeutic development and understanding of DENV and ZIKV infections.
  42. DENV Inhibitor

    DENV-IN-7 is a flavone analog that functions as a dengue virus (DENV) inhibitor, demonstrating an EC50 value of 70 nM. This compound exhibits low toxicity to normal cells while maintaining effective antiviral activity against DENV. It is suitable for research applications focused on the development of therapeutics for dengue virus infections.
  43. Bacterial DNA Gyrase/Topo IV Inhibitor

    GC-072 is a selective inhibitor of bacterial DNA gyrase and Topoisomerase IV, demonstrating potent antibacterial activity. This 4-oxoquinolizine antibiotic exhibits efficacy against a wide range of bacterial strains, including Gram-positive, Gram-negative, and multidrug-resistant organisms. Importantly, GC-072 does not interfere with human topoisomerases I and II, making it a suitable candidate for studying bacterial infections. Its bactericidal action against Burkholderia pseudomallei is significant, as it supports dose-dependent survival rates in mice during lethal inhalational models, highlighting its potential in melioidosis research.
  44. HIV-1 Reverse Transcriptase Inhibitor

    R82913 (9-Cl-TIBO) is a selective inhibitor of HIV-1 reverse transcriptase, demonstrating significant antiviral activity against both RNA and DNA templates crucial for viral replication. This compound effectively inhibits the replication of various HIV-1 strains in CEM cells, with a median IC50 value of 0.15 μM. It serves as a valuable reagent for research applications focused on HIV therapy development and reverse transcriptase inhibition studies.
  45. Bacterial DNA Gyrase B Inhibitor

    DNA Gyrase-IN-3 is a specific inhibitor of bacterial DNA gyrase B, exhibiting IC50 values ranging from 5.41 to 15.64 µM against E. coli DNA gyrase. This compound demonstrates significant anti-tubercular and antibacterial activity, making it a valuable tool for microbial research. Its mechanism of action is relevant in studies aimed at developing new antibacterial agents targeting bacterial DNA replication and transcription processes.
  46. Bacterial Inhibitor

    CI-990 (PD-131112) is a selective inhibitor of bacterial DNA gyrase, targeting key enzymes involved in DNA replication and repair. It exhibits potent antibacterial activity and is especially relevant for studying Enterococcal infections, including endocarditis and sepsis. This compound can serve as a valuable tool in microbiological research to understand bacterial resistance mechanisms and develop therapeutic strategies.
  47. Dengue Viral Replication Inhibitor

    DENV-IN-2 is a potent inhibitor of dengue viral replication, demonstrating exceptional activity against all four serotypes of the dengue virus. With an EC50 ranging from 0.013 to 0.029 nM, it shows remarkable efficacy in suppressing viral activity. This compound is valuable for research applications targeting dengue virus pathogenesis and developing antiviral strategies.
  48. Bacterial Transcription Inhibitor

    CUHK242 is a selective bacterial transcription inhibitor that effectively disrupts RNA synthesis within bacterial cells. It demonstrates a minimum inhibitory concentration (MIC) of 2 μg/mL against the B. subtilis reporter strain BS2019 and exhibits antimicrobial activity against Staphylococcus aureus. This compound is useful for research applications focused on understanding bacterial gene expression and studying the mechanisms of antibiotic resistance.
  49. DENV Inhibitor

    DENV-IN-6 is a powerful inhibitor of dengue virus (DENV) serotypes I-IV, exhibiting effective antiviral activity with EC50 values of 17.5, 13.20, 6.8, and 11.41 μM, respectively, for the inhibition of viral replication. Additionally, DENV-IN-6 demonstrates notable activity against HIV-1 IIIB, with an EC50 of 0.0181 µM and a cytotoxicity (CC50) of 64.92 µM. This compound serves as a valuable tool for research into antiviral therapies targeting DENV and HIV-1.
  50. HIV Inhibitor

    Fozivudine tidoxil is an orally active HIV inhibitor designed as a thioether lipid-zidovudine (ZDV) conjugate. This compound exhibits potent anti-HIV activity by incorporating into the newly synthesized DNA strand during viral replication, leading to irreversible binding to viral reverse transcriptase and disruption of the reverse transcription process. In addition to its antiviral properties, Fozivudine tidoxil is also a versatile click chemistry reagent, capable of undergoing copper-catalyzed azide-alkyne cycloaddition (CuAAc) and strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with suitable alkyne or DBCO/BCN-containing molecules, making it valuable for chemical biology applications.

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