Parbendazole-d3 is the deuterium labeled Parbendazole. Parbendazole is a potent inhibitor of microtubule assembly, destabilizes tubulin, with an EC50 of 530 nM, and exhibits a broad-spectrum anthelmintic activity.
(+)-α-Tocopherol is a vitamin E derivative. vitamin E is a fat-soluble antioxidant.
Alafosfalin is an inhibitor of cell wall biosynthesis. Alafosfalin is a phosphonodipeptide with antibacterial properties[1].
Octanoylcarnitine chloride is a homolog of acetylcarnitine chloride. Octanoylcarnitine chloride can enhance absorption of drugs from gastrointestinal tract[1].
SCH 38519 is a platelet aggregation inhibitor. SCH 38519 inhibits thrombin-induced aggregation of human platelets with an IC50 of 68 μg/mL. SCH 38519 is also active against Gram-positive and Gram-negative bacteria [1].
Dimethyl L-glutamate (Dimethyl glutamate), a membrane-permeable analog of Glutamate, can stimulate insulin release induced by Glucose. Dimethyl L-glutamate suppresses the KATP channel activities. Dimethyl L-glutamate inhibits E. gracilis growth and causes abnormal cell division. Dimethyl L-glutamate can be used in the research of diabetes, glucose transport, phosphorylation, and further metabolism[1][2][3][4].
Antiviral agent 14 is an antiviral agent against the tobacco mosaic virus (TMV) and cucumber mosaic virus (CMV). The EC50 values of Antiviral agent 14 against TMV and CMV with EC50 values of 135.5 μg/mL and 178.6 μg/mL, respectively[1].
XSJ2-46, 5'-amino NI analog, is an antiviral agent. XSJ2-46 has anti-Zika virus activity. XSJ2-46 exhibits reasonable inhibition of RNA-dependent RNA polymerases (RdRp) with an IC50 value of 8.78 μM[1].
Avibactam sodium is a covalent and reversible β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
Eravacycline dihydrochloride (TP-434 dihydrochloride) is a potent and broad-spectrum antibacterial agent.
KKL-10 is a small-molecule ribosome rescue inhibitor with broad-spectrum antimicrobial activity against bacteria.
5-Bromo-2′-deoxy-2′-fluorouridine (Example 1), a 5-halo analog, is potential as an antiviral agent[1].
Mildiomycin is a Streptoverticillium rimofaciens antibiotic against powdery mildew of barley. Mildiomycin inhibits some Mycobacterium and Rhodotorula growth, but fails against most fungi and bacteria[1].
Teixobactin is a potent antibiotic. Teixobactin shows antibacterial activity for gram-negative bacteria. Teixobactin inhibits cell wall synthesis by binding to a highly conserved motif of lipid II and lipid III[1][2][3].
A2ti-1 is a selective and high-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 24 μM[1]. A2ti-1 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-1 prevents human papillomavirus type 16 (HPV16) infection[2].
Human β-defensin-2 (HβD-2) is a small cysteine-rich cationic skin-antimicrobial peptide (SAP) produced by a number of epithelial cells.Human β-defensin-2 has antimicrobial activity against gram-negative bacteria and Candida, but not gram-positive Staphylococcus aureus[1]. Human β-defensin-2 can be used for the study of colitis[2].
N-Butyryl-DL-homocysteine thiolactone is an N-acyl homoserine lactone (AHL) analogue. N-Butyryl-DL-homocysteine thiolactone shows potential adverse effect and toxicity on bacteria. AHLs are potent inhibitors of biofilm formation and virulence factors, and has been used for degrading microbial communities, reducing bacterial pathogenicity[1][2].
ent-11β-Hydroxyatis-16-ene-3,14-dione (compound 11) is a diterpenoid from the fresh roots of Euphorbia jolkinii. ent-11β-Hydroxyatis-16-ene-3,14-dione has anti-RSV activity[1].
Pritelivir mesylate (BAY 57-1293 mesylate), an inhibitor of the viral helicase-primase complex, exhibits antiviral activity in vitro and in animal models of herpes simplex virus (HSV) infection. Pritelivir mesylate is active against herpes simplex virus types 1 and 2 (HSV-1 and HSV-2) with the IC50 of 0.02 μM against HSV1-2[1].
5,7,8-Trimethoxycoumarin is an anti-Parasite agent with IC50s of 25.5 μM and 57.7 μM against Trypanosoma cruzi and L. amazonensis, respectively[1].
Lactacystin, an antibiotic Streptomyces spp. metabolite, is a potent and selective proteasome inhibitor with an IC50 of 4.8 μM for 20S proteasome. Lactacystin also inhibits the lysosomal enzyme cathepsin A[1]. Lactacystin inhibits cell growth and induces neurite outgrowth[2].
SARS-CoV-2-IN-20 (Compound 1a) is a potent inhibitor of SARS-CoV-2 with an EC50 of 6.5 μM. SARS-CoV-2-IN-20 has the potential for the research of infection diseases[1].
HBV-IN-15 is a potent inhibitor of covalently closed circular DNA (cccDNA). cccDNA serves as the template for viral RNA transcription and subsequent viral DNA generation. HBV-IN-15 is a flavone derivative. HBV-IN-16 has the potential for the research of HBV infection (extracted from patent WO2020052774A1, compound 2)[1].
Hesperetin 7-O-glucoside is produced by the enzymatic conversion of Hesperidin. Hesperetin 7-O-glucoside is a potent human HMG-CoA reductase inhibitor and also effectively inhibits the growth of Helicobacter pylori. Antihypertensive effect[1][2].
AN11251 is a potent and oral active anti-Wolbachia agent with potential for treatment of onchocerciasis and lymphatic filariasis, with EC50 values of 1.5 nM in LDW1 cell lines and 15 nM in C6/36 cell lines[1].
β-Caryophyllene-d2 is deuterium labeled β-Caryophyllene. β-Caryophyllene is a CB2 receptor agonist.
Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ[1][2][3][4].
Oxynitidine is an HBV inhibitor (ID50=30.8 µg/mL), which can effectively inhibit the DNA replication activity of HBV. Oxynitidine can be used in the study of viral infections[1].