Zoxamide (RH-7281) is an oomycete fungicide. Zoxamide arrests nuclear division in Phytophthora capsici germlings and destroyed the microtubule cytoskeleton[1][2].
2'-Deoxyuridine-2′-13C is the 13C labeled 2'-Deoxyuridine. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. A known use of 2'-Deoxyuridine is as a precursor in the synthesis of Edoxud[1]
c[Arg-Arg-Arg-Arg-Nal-Nal-Nal] (Compound 9C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 25 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively[1].
Prostaglandin A2 (PGA2), a human endogenous metabolite of PGE2, is an antitumor agent. Prostaglandin A2 induces p53-dependent Apoptosis. Prostaglandin A2 also has antiviral activity[1][2][3].
Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing[1]. Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK[2]. Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer[3].
HIV-1 protease-IN-1 (Compound 1e) is a potent inhibitor of HIV-1 protease with an IC50 of 90 pM. HIV-1 protease-IN-1 demonstrates antiviral activity with EC50 value of 89 nM against B-HIV. HIV-1 protease-IN-1 exhibits activity with EC50 value of 13.59 nM against C-HIV strain ZM246. HIV-1 protease-IN-1 shows remarkable activity with EC50 value of 8.23 nM against C-HIV strain Indie[1].
Z-Antiepilepsirine is an amide alkaloid that can be found in Piper capense L.f. Z-Antiepilepsirine shows antiplasmodial activity with an IC50 value of 27 µM for W2 strain of Plasmodium falciparum[1].
FR182024 is a cephem derivative with potent anti-Helicobacter pylori activities[1].
Triclosan D3 is the deuterium labeled Triclosan. Triclosan is an antibacterial and antifungal agent found in consumer products, including soaps, detergents, toys, and surgical cleaning treatments[1][2].
3-O-Methylgalangin (Galangin 3-methyl ether) is a natural flavonoid compound from the rhizome of Alpinia officinarum (AO) with antibacterial activities, which also inhibits pancreatic lipase[1][2].
Gageotetrin C is an antimicrobial peptide derived from the marine bacterium Bacillus subtilis. Gageotetrin C is more active against fungi (MIC value is 0.02-0.04 μM) [1].
Amprolium hydrochloride is a coccidiostat used in poultry, is a thiamine analogue and blocks the thiamine transporter of Eimeria species by blocking thiamine uptake it prevents carbohydrate synthesis.
SARS-CoV-IN-3 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-3 shows anti-Coronavirus activity with an EC50 of 3.6 μM in Vero cells. SARS-CoV-IN-3 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 11.7 and 20.4 nM; and IC90s of 29.19 and 56 nM; respectively. SARS-CoV-IN-3 reduces HIV-1-induced cytopathic effect with an EC50 of 10 μM in MT-4 cells[1].
cis-ACCP is an orally active antimetastatic matrix metalloproteinase-2 (MMP-2) selective inhibitor. cis-ACCP can inhibit MMP-2 and MMP-9 with IC50 values of 4 μM and 20 μM, respectively. cis-ACCP can be used for the research of a variety of chronic diseases[1].
(S)-Tenofovir ((S)-GS 1278) is the less active S-enantiomer of Tenofovir. Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV)[1].
Oxytetracycline hydrochloride is an antibiotic belonging to the tetracycline class. Oxytetracycline hydrochloride potent inhibits Gram-negative and Gram-positive bacteria. Oxytetracycline hydrochloride is a protein synthesis inhibitor and prevents the binding from aminoacil-tRNA to the complex m-ribosomal RNA. Oxytetracycline hydrochloride also possesses anti-HSV-1 activity[1][2][3].
(R)-Praziquantel D11 is the deuterium labeled (R)-Praziquantel. (R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human 5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal eutomer[1].
Methoprene is a juvenile hormone (JH) analog, does not kill insects, acts as an insect growth regulator, interferes with an insect's lifecycle and prevents it from reaching maturity or reproducing, is a biological pesticide.
Sulconazole mononitrate ((±)-Sulconazole mononitrate), an imidazole derivative, is a broad-spectrum fungicide and is inhibitory to certain gram-positive anaerobes. Sulconazole mononitrate can be used for the research of dermatomycoses, pityriasis versicolor, and cutaneous candidiasis[1][2].
Physcion (Parietin) is an anthraquinone isolated from traditional Chinese medicine Radix et Rhizoma Rhei, acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC50 and a Kd of 38.5 μM and 26.0 μM, respectively[1][2]. Physcion (Parietin) exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects[2].
SARS-CoV-2 3CLpro-IN-15 (compound a) is a beta-nitrostyrene coronavirus SARS-CoV-2 inhibitor that targets the SARS-CoV-2 3CL protease (3CLpro). SARS-CoV-2 3CLpro-IN-15 inhibits viral replication and transcription and plays a key role in the discovery of anti-COVID-19 lead compounds[1].
Guaijaverin is a urease inhibitor with an IC50 of 120 μM. Guaijaverin shows antioxidant and anti-Streptococcus mutans activities[1][2][3].
Maleic Acid is a Glutamate Decarboxylase (GAD) inhibitor of E. coli and L. monocytogenes.
Nalidixic Acid-d5 is the deuterium labeled Nalidixic acid. Nalidixic acid, a quinolone antibiotic, is effective against both gram-positive and gram-negative bacteria. Nalidixic acid acts in a bacteriostatic manner in lower concentrations and is bactericidal in higher concentrations. Nalidixic acid inhibits a subunit of DNA gyrase and topoisomerase IV and reversibly blocks DNA replication in susceptible bacteria[1].
Sorivudine (BV-araU) is an orally active synthetic pyrimidine nucleoside antimetabolite drug. Sorivudine derives its antiviral activity from selective conversion by a specific thymidine kinase present in certain DNA viruses to nucleotides, which can in turn interfere with viral DNA synthesis[1].
Cetylpyridinium chloride monohydrate is a cationic quaternary ammonium compound, used in some types of mouthwashes, toothpastes, throat and nasal sprays, is an antiseptic that kills bacteria and other microorganisms, effective in preventing dental plaque and reducing gingivitis.
Thymidine 5′-diphosphate (dTDP) is the key product of pyrimidine synthesis in organisms. Thymidine 5′-diphosphate is produced by thymidylate kinase (TMPK) catalyzed phosphorylation of 5′-thymidine monophosphate (dTMP), which requires ATP and Mg2+. Thymidine 5′-diphosphate is further catalyzed by TMPK to thymidine 5′-triphosphate (dTTP). TMPK activity can be detected by measuring the level of Thymidine 5′-diphosphate[1][2].
Rapanone is a natural benzoquinone. Rapanone exhibits a broad spectrum of biological actions, including anti-tumor, antioxidant, anti-inflammatory, antibacterial and antiparasitic. Rapanone also is a potent and selective human synovial PLA2 inhibitor, with an IC50 of 2.6 μM[1][2][3][4].
Quinate is an antiarrhythmic agent. Quinate is a potent, orally active, selective cytochrome P450db inhibitor. Quinate is also a K+ channel blocker with an IC50 of 19.9 μM. Quinate can be used for malaria research[1][2][3].
Temocillin, a 6-alpha-methoxy penicillin derivative, is a semisynthetic beta-lactam antibiotic with a spectrum of activity against most aerobic Gram-negative bacteria[1].