KPC-2-IN-1, boronic acid derivative, is a potent KPC-2 inhibitor with Ki of 0.032 μM. KPC-2-IN-1 enhances the activity of cefotaxime in KPC-2 expressing E. coli. KPC-2-IN-1 exhibits well tolerated in human HEK-293 cells, which can be used for the study of E. coli resistance to β-lactam antibiotics[1][2].
Cyclo(Phe-Pro) (Cyclo(phenylalanylprolyl)), a Vibrio vulnificus quorum-sensing molecule, inhibits retinoic acid-inducible gene-I (RIG-I) polyubiquitination, through its specific interaction with RIG-I, to blunt IRF-3 activation and type-I IFN production. Cyclo(Phe-Pro) (Cyclo(phenylalanylprolyl)) enhances susceptibility to hepatitis C virus (HCV), as well as Sendai and influenza viruses[1].
Ibuzatrelvir (PF-07817883) is an antiviral agent, targeting to SARS-CoV-2 3CL protease. Ibuzatrelvir can be used to inhibit COVID-19[1].
(±)-Phrymarolin II is a promising new class of plant virus (tobacco mosaic virus) inhibitors.
Anti-infective agent 5 (compound 74) is an orally active inhibitor of Trypanosoma cruzi with an IC50 value of 0.10 μM. Anti-infective agent 5 effectively reduces parasite burden in vivo. Anti-infective agent 5 can be used for the research of infection[1].
Hepatitis b virus pre-s region (120-145) is a preS2 peptide that inhibits the binding of single-chain Fv fragment (scFv) or IgG to r-HBsAg[1].
Eberconazole nitrate is a dichlorinated imidazole derivative with antifungal activity. Eberconazole nitrate is more active than Clotrimazole, Ketoconazole, and Miconazole. Eberconazole nitrate has the potential for the research of dermatophytoses with a topical administration[1].
Extracellular death factor (EDF) is the only single signaling molecule involved in Escherichia coli quorum sensing, and can initiate MAZEF-mediated cell death. Extracellular death factor significantly amplifies the endoribonucleolytic activities of both MazF and ChpBK[1].
DL-Syringaresinol ((±)-Syringaresinol), a lignin, inhibits UVA-induced upregulation of MMP-1 by suppressing MAPK/AP-1 signaling in human HaCaT keratinocytes and dermal fibroblasts (HDFs). DL-Syringaresinol has antiphotoaging properties against UVA-induced skin aging. DL-Syringaresinol exhibits weak antimycobacterial activity against Mycobacterium tuberculosis H37Rv[1][2].
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria[2]. Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
Peceleganan is an artificial antimicrobial cecropin A (1-10) × melittin B (3-18) hybrid (10+16)-peptide analogue. Peceleganan inhibits wound infection[1].
Omaciclovir (H2G) is a potent and selective inhibitor of herpesvirus replication. Omaciclovir is a nucleoside analog with antiviral activity[1].
Oxindole (Indolin-2-one) is an aromatic heterocyclic building block. 2-indolinone derivatives have become lead compounds in the research of kinase inhibitors.
Bonducellpin D is a furanoditerpenoid lactone isolated from Caesalpinia minax. Bonducellpin D exhibits broad-spectrum inhibition potential against SARS-CoV Mpro and MERS-CoV Mpro, with an Ki of 467.11 and 284.86 nM, respectively. Bonducellpin D also exhibits moderate anti-cancer activity in vitro[1][2][3].
Fluopyram is a succinate dehydrogenase inhibitor fungicide, inhibits the growth of F. virguliforme isolates with mean EC50 of 3.35 µg/mL[1].
Chamigrenol is a Na+/K+-ATPase inhibitor with an IC50 value of 15.9 μg/mL. Chamigrenol shows strong inhibitory activities against Gram-positive and Gram-negative bacteria except Escherichia coli, with MIC values of 50 µg/mL[1].
Antcin-B is a potent inhibitor of 3CLPro with high affinity. Antcin-B can be used in study SARS-CoV-2[1].
Remdesivir O-desphosphate acetonide impurity is an impurity of Remdesivir. Remdesivir (GS-5734), a nucleoside analogue with effective antiviral activity and is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro[1][2].
Hymeglusin, as a fungal β-lactone antibiotic, is a HMG-CoA synthase inhibitor (IC50 = 0.12 μM). Hymeglusin covalently modifies the active Cys129 residue of the enzyme[2][3].
Cefsulodin (SCE-129) sodium is a third generation β lactam antibiotic and member of the cephems subgroup of antibiotics. Cefsulodin sodium inhibits cell wall synthesis by competitively inhibiting penicillin binding protein (PBP) cross-linking and transpeptidation of peptidogly. Cefsulodin sodium is a potent tyrosine phosphatase inhibitor against mPTPB, a virulent phosphatase from Mycobacterium tuberculosis, with an IC50 value of 16 μM[1][2][3][4].
Cyclopropavir (Filociclovir; ZSM-I-62; MBX-400) is a broad-spectrum anti-herpesvirus compound, has good antiviral activity against cytomegalovirus (CMV), herpes simplex virus (HHV)-6 and HHV-8 with EC50s of 0.7 μM to 8 μM[1].
M4284 (M-4284) is a high-affinity biphenyl mannoside FimH inhibitor with HAI of 16 nM in hemagglutination assay; reduces intestinal colonization of genetically diverse UPEC isolates, while simultaneously treating UTI, without notably disrupting the structural configuration of the gut microbiota; reduces UTI89 levels in the gut and urinary tracts of mice.
Metallo-β-lactamase-IN-6 is a potent VIM-Type metallo-β-lactamase inhibitor with IC50s of 0.56 μM, 29.50 μM and 5.78 μM for VIM-2, VIM-1 and VIM-5. Metallo-β-lactamase-IN-6 displays potent synergistic antibacterial activity with Meropenem against engineered Escherichia coli strains and intractable clinically isolated Pseudomonas aeruginosa producing VIM-2 MBL[1].
N-(β-ketocaproyl)-L-Homoserine lactone is a component of quorum regulatory sensing[1].
Hamamelitannin, a polyphenol extracted from the bark of Hamamelis virginiana, is a quorum-sensing (QS) inhibitor. Hamamelitannin increases antibiotic susceptibility of staphylococcus aureus biofilms by affecting peptidoglycan biosynthesis and eDNA release[1][2].
Quinaldopeptin, a quinomycin antibiotic isolated from the culture of Streptoverticillium album strain, is highly active against Gram-positive bacteria and anaerobes and strongly cytotoxic against cultured B16 melanoma cells[1].
Fumagillol is a direct precursor of fumagillin. Fumagillin, as an antimicrobial agent, is a potent and selective inhibitor of angiogenesis[1].
Pyromeconic acid is an antifungal substance[1].
PI3Kδ-IN-13 (compound 89) is a PI3Kδ inhibitor (IC50=2.6 nM). PI3Kδ-IN-13 can be used in the research of cell proliferation diseases such as cancer, infection, inflammation and autoimmune diseases[1].
Panobinostat lactate is a potent and orally active non-selective HDAC inhibitor. Panobinostat lactate has antineoplastic activities. Panobinostat lactate effectively disrupts HIV latency. Panobinostat lactate induces cell apoptosis and autophagy. Panobinostat lactate can be used for the study of refractory or relapsed multiple myeloma[1][2][3][4][5].