DHFR-IN-1 (compound 12) is a potent and selective DHFR (dihydrofolate reductase)inhibitor, with an IC50 of 40.71 nM. DHFR-IN-1 exhibits promising antibacterial activity against gram-positive and gram-negative bacteria. DHFR-IN-1 exhibits moderate antifungal activities. DHFR-IN-1 exhibits a high synergistic effect with Levofloxacin (HY-B0330), where the FIC (fractional inhibitory concentration index) value is 0.249[1].
Dafsolimab (SPV-T3a) is an IgG2a murine monoclonal antibody (anti-CD3). Dafsolimab can induce cell death through modulation and activation of the CD3/T cell receptor complex. Dafsolimab can be used for the research of graft-versus-host disease (GVHD)[1].
DC07090 dihydrochloride is a low toxicity, potent, reversible and competitive non-peptidyl human enterovirus 71 3C protease inhibitor with an IC50 and a Ki value for 21.72 μM and 23.29 μM. DC07090 dihydrochloride could also inhibit coxsackievirus A16 (CVA16) replication with an EC50 value of 27.76 μM[1].
Influenza A virus-IN-1 is a dihydropyrrolidones derivative and is a potent inhibitor against wide subtypes of influenza A virus (IAV) with IC50 values from 3.11 μM to 7.13 μM. Influenza A virus-IN-1 efficiently inhibits replication of IAV, up-regulates the expression of key antiviral cytokines IFN-β and antiviral protein MxA[1].
Faldaprevir-d6 is deuterium labeled Faldaprevir.
Isotanshinone I has inhibitory activity against α-glucosidase and formation of AGE, with IC50s of 1.13, 0.432 μM for α-glucosidase and AGE, respectively.
Suc-AAPE-pNA is a chromogenic substrate of glutamyl endopeptidase. Suc-AAPE-pNA can be used to test glutamyl endopeptidase activity[1].
Antituberculosis agent-3 (Compound 2) is an antituberculosis agent. Antituberculosis agent-3 shows anti-mycobacterial activity, and can inhibit M. tuberculosis H37Rv strain growth (MIC=12.5 μg/mL)[1].
Rustmicin (Galbonolide A) is a potent antifungal agent. Rustmicin inhibits inositol phosphoceramide synthase. Rustmicin shows antifungal activity[1].
Reutericyclin (Reutericycline), a unique tetramic acid, is an antibiotic produced by some strains of Lactobacillus reuteri. Reutericyclin (Reutericycline) exhibits a broad inhibitory spectrum including Lactobacillus spp., Bacillus subtilis, B. cereus, Enterococcus faecalis, Staphylococcus aureus, and Listeria innocua[1][2].
(1R)-α-Pinene is a volatile monoterpene with antimicrobial activities. (1R)-α-Pinene reduces Bacillus cereus population growth, and exhibits repellent effects[1][2].
Cyclopyrimorate, a highly effective bleaching herbicide for weed control in rice fields, targets homogentisate solanesyltransferase (HST). HST is a downstream enzyme of 4-hydroxyphenylpyruvate dioxygenase in the plastoquinone (PQ) biosynthesis pathway[1][2].
EBOV-IN-1 (com 3.47) is an adamantane dipeptide piperazine and an inhibitor of Ebola virus (EBOV). EBOV-IN-1 targets Niemann-Pick C1 (NPC1) and inhibits its binding to the EBOV glycoprotein (GP) that activates and mediates viral penetration into host cells, thereby inhibiting EBOV infection. EBOV-IN-1 inhibits pseudotyped EBOV infection with an IC50 of 13 nM[1].
Penicillin V-d5 (Phenoxymethylpenicillin-d5) is the deuterium labeled Penicillin V. Penicillin V (Phenoxymethylpenicillin) is an orally active antibiotic. Penicillin V inhibits the growth of Streptococci, C. difficile and S. aureus. Penicillin V can be used for the research of otitis, sinusitis, pharyngitis and tonsillitis[1][2][3][4].
Apelin-17(human, bovine) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ[1][2][3].
Escin IA is a triterpene saponin isolated from horse chestnut, which inhibits HIV-1 protease with IC50 values of 35 μM. Escin IA has anti-TNBC metastasis activity, and its action mechanisms involved inhibition of epithelial-mesenchymal transition process by down-regulating LOXL2 expression[1][2].
2'-Deoxy-L-guanosine selectively inhibits D-Thymidine phosphorylation catalyzed by HSV 1 thymidine kinase.2'-Deoxy-L-guanosine is the L-configuration of 2'-Deoxyguanosine (HY-17563)[1].
ETX0462 is a gram-negative chemotype antibiotic. ETX0462 has potent in vitro and in vivo activity against Pseudomonas aeruginosa plus all other Gram-negative ESKAPE pathogens, Stenotrophomonas maltophilia and biothreat pathogens[1].
Ogalvibart (C-135-LS) is a humanized anti-SARS-CoV-2 monoclonal antibody (IgG1 type). Ogalvibart binds to the spike (S) glycoprotein receptor-binding domain (RBD) of SARS-CoV-2. Ogalvibart in combination with C144LS (1:1 ratio) shows good preventive activity and can effectively block the development of COVID19 in a rhesus monkey disease model[1].
Docaravimab is an antibody, targeting ERA (Evelyn-Rockitniki-Abelseth) glycoprotein ectodomain epitope G-III. Docaravimab can be used in research of Rabies[1].
SDZ285428 is a CYP51 inhibitor. SDZ285428 inhibits Trypanosoma cruzi (TC) CYP51 with I/E2 <1 (5 min) and I/E2=9 (1 h). SDZ285428 inhibits Trypanosoma brucei (TB) CYP51 with I/E2 <1 (5 min) and I/E2=35 (1 h)[1].
STING agonist-26 (CF508) is a non-nucleotide small-molecule STING agonist. STING agonist-23 activates STING, increases phosphorylation of STING, TBK1 and IRF3. STING agonist-23 promotes the levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. STING agonist-23 exhibits activity against SARS-CoV series strains[1].
Hycanthone is an effective antischistosomai drug.
Clesrovimab (MK1654) is a fully human, anti-RSV fusion (RSV F) glycoprotein monoclonal antibody. Clesrovimab has the potential for the research of respiratory syncytial virus infection[1][2].
Vanillic acid is a flavoring agent found in edible plants and fruits. Vanillic acid inhibits NF-κB activation. Anti-inflammatory, antibacterial, and chemopreventive effects[1].
PfGSK3/PfPK6-IN-1 (compound 23e) is a potent inhibitor of plasmodial kinases PfGSK3 and PfPK6, with IC50s of 97 nM and 8 nM, respectively. PfGSK3/PfPK6-IN-1 exerts antiplasmodial activity against blood stage Pf3D7 parasites with an EC50 value of 1.4 mM[1].
Colistin A is a major component of Colistin. Colistin is a polymyxin antibiotic and can be used to combat infections caused by problematic gram-negative bacteria[1].
Pseudomonic acid D is a microbial inhibitor. Pseudomonic acid D potently inhibits mycoplasmas and bacterial pathogens. Pseudomonic acid D can be produced by fermentation with Pseudomonas fluorescens[1].
(±)-Praeruptorin A is the di-esterified product of cis-khellactone (CKL) and the major active ingredient in Peucedani Radix which consists of the dried roots of Peucedanum praeruptorumDunn (Apiaceae). (±)-Praeruptorin A has been widely employed as one of the famous traditional Chinese medicines (TCMs) for the treatment of cough with thick sputum and dyspnea, nonproductive cough and upper respiratory infections for centuries in China. (±)-Praeruptorin A has dramatically therapeutic effects on hypertension mainly through acting as a Ca2+-influx blocker[1].
SARS-CoV-2-IN-62 (Compound R3b) is an inhibitor of SARS-CoV-2 replication and has low cytotoxicity. SARS-CoV-2-IN-62 inhibits viral replication in Vero E6 cells and Calu-3 cells, with EC50 values of 2.97 μM and 3.82 μM, respectively[1].