LeuRS-IN-1 hydrochloride is a potent, orally active M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS) inhibitor. LeuRS-IN-1 hydrochloride has IC50 and Kd values of 0.06 μM, 0.075 μM for M.tb LeuRS, respectively[1]. LeuRS-IN-1 hydrochloride inhibits human cytoplasmic LeuRS (IC50=38.8 μM), and HepG2 protein synthesis (EC50=19.6 μM)[2].
4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, is an antiretroviral agent which is potent against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity[1].
AB-729, a nucleoside analogue, is an RNA interference (RNAi). AB-729 conjugates to a trimer of N-acetylgalactosamine (GalNAc) ligand that promotes uptake into hepatocytes via the asialoglycoprotein receptor (ASGR). AB-729 inhibits viral replication and reduces HBV antigens[1][2].
Cleistanthin B (Diphyllin O-glucoside) is an orally active arylnaphthalene lignan lactone glycoside. Cleistanthin B exhibits anti-SARS-CoV-2 effects in Vero cells, with EC50 of 6.51 µM. Cleistanthin B also exhibits antitumor, diuretic and antihypertensive effects in vivo[1][2][3][4].
Monaschromone, a polyketide metabolite, significantly inhibits the growth of B. cinerea, A. solani, M. oryzae, and G. saubinettii, with the MIC values ranging from 6.25 to 12.5 μM[1].
Capreomycin is a macrocyclic peptide antibiotic. Capreomycin can be used for anti-multidrug-resistant-tuberculosis research. Capreomycin can inhibit phenylalanine synthesis in in mycobacterial ribosomes translation[1][2]
Caulilexin C is a phytoalexin from crucifers with antifungal activity[1].
Bephenium hydroxynaphthoate is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis; B-type AChR activator.
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively[1].
Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females.
IDR-1 is an antimicrobial peptide that is active against Gram-positive and Gram-negative bacteria. IDR-1 counters infection by selective modulation of innate immunity without obvious toxicities. IDR-1 has anti-inflammatory and anti-infective properties, enhances the levels of monocyte chemokines, and attenuates pro-inflammatory cytokine release[1][2].
Potassium guaiacolsulfonate hemihydrate is an orally active expectorant used for acute respiratory tract infections. Potassium guaiacolsulfonate hemihydrate helps loosen mucus and used for a cough caused by the common cold, infections or allergies in combination with other drugs[1][2].
Bethoxazin(Bethoguard) is a new broad spectrum industrial microbicide with applications in material and coating preservation.IC50 value:Target: MicrobicideBethoxazin potently inhibited the catalytic activity of yeast DNA topoisomerase II and the growth of yeast BY4742 cells at low micromolar concentrations. bethoxazin may exert its microbicidal action by reacting with sensitive endogenous sulfhydryl biomolecules of microbial cells.
Nybomycin, an antibiotic, exhibits antiphage and antibacterial properties. Nybomycin binds to DNA and induces a unique morphological change to mycobacterial bacilli leading the bacterial cell death[1][2].
Urease-IN-8 (Compound 5e) is a competitive Urease inhibitor (IC50: 3.51 μM, Ki: 3.11 μM). Urease-IN-8 can be used for research of peptic and gastric ulcers[1].
Graveoline (Rutamine) is an anti-cancer agent that can trigger apoptosis and autophagy in skin melanoma cells. Graveoline also exhibits antifungal activity[1].
Cap-dependent endonuclease-IN-14 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-14 inhibits the replication of influenza virus. Cap-dependent endonuclease-IN-14 has the potential for the research of viral infections caused by influenza viruses (extracted from patent CN113620948A, compound 1-c)[1].
XMP-629 (XOMA-629), a cationic α-helical peptide, is a potent endotoxin inhibitor. XMP-629 exhibits broad-spectrum antimicrobial activity via an immunomodulatory mechanism. XOMA 629 has antimicrobial activity against Propionibacterium acnes, Staphylococcus aureus and Streptococcus pyogenesand[1][2].
Tolnaftate is a synthetic thiocarbamate used as an anti-fungal agent. Target: AntifungalTolnaftate blocked sterol biosynthesis in fungal cells and cell extracts, with accumulation of squalene. This point of action was confirmed by the direct inhibition of microsomal squalene epoxidase from Candida albicans [1]. Tolnaftate inhibited sterol biosynthesis, At 100 microM, tolnaftate caused up to a 30% release of intracellular [14C]aminoisobutyric acid [2].
epi-Equisetin, a secondary metabolite, has antibacterial activity[1].
HIV-1 inhibitor-34 (compound 5q) is a potent and selective HIV-1 inhibitor with an EC50 of 6.4 nM for HIV-1 and a CC50 of 16 μM in MT-4 cells. HIV-1 inhibitor-34 can be used for researching AIDS[1].
Methyl tanshinonate is a tanshinone, that can be isolated from Salvia miltiorrhiza (S. miltiorrhiza) Bunge (Lamiaceae). Methyl tanshinonate is a potent inhibitor of Mpro enzyme in SARS-CoV (IC50 = 21.1 µM). Methyl tanshinonate can be used for diabetes and SARS-CoV research[1][2][3].
Ritonavir-d6 (ABT 538-d6) is the deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM[1][2].
anti-TB agent 1 is a potent and orally active anti-tuberculosis agent, with MICs of < 2 nM against the Mtb strains H37Rv, rRMP and rINH[1].
Mupirocin(BRL-4910A) is an antibiotic of the monoxycarbolic acid class; effective against Gram-positive bacteria, including MRSA.
EP2 is an antimicrobial peptide. EP2 has antibacterial and antifungal activities. EP2 inhibits E. gallinarum, P. pyocyanea, A. baumanii, K. terrigena with a MIC value of 11.4 μg/mL[1].
Spirodiclofen is a broad spectrum acaricide acting via lipid biosynthesis inhibition (LBI) with no cross resistance to currently available acaricides and with additional insecticidal properties.
Xanthatin is isolated from Xanthium strumarium leaves. Xanthatin exhibits strong antitumor activities against a variety of cancer cells through apoptosis persuasion and shows anti-inflammatory activities by inhibiting PGE2 synthesis and 5-lipoxygenase activity[1]. Xanthatin is a potent and orally active inhibitor of VEGFR2 kinase activity with an IC50 of 3.8 μM and prominently blocks the phosphorylation of VEGFR2 at Tyr951 site. Xanthatin inhibits angiogenesis and has the potential for the investigation of breast cancer[2].
Ectoine is a natural cell protectant, an amino acid derivate produced by bacteria living under extremely harsh environmental conditions. Ectoine serves as an osmoregulatory compatible solute, increasing the hydration of the skin surface and stabilizing lipid layers, which is useful in skincare[1]. Ectoine demonstrates a good safety profile for the treatment of allergic rhinitis[2].
Nevirapine-d3 (BI-RG 587-d3) is the deuterium labeled Nevirapine. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM[1].