10,11-Dehydrocurvularin is an antibiotic and a strong activator of the heat shock response, a conserved evolutionary mechanism that maintains protein homeostasis via the overexpression of heat shock factor 1 (HSF1) and various chaperones including heat shock protein 90 (Hsp90). 10,11-Dehydrocurvularin inhibits TGF-β signalling pathway. Anti-tumorous activity[1][2].
Olanexidine hydrochloride is a monobiguanide compound with bactericidal activity. Olanexidine probably binds to the cell membrane, destroys membrane integrity. Olanexidine hydrochloride is active against a wide range of bacteria, including Gram-positive and Gram-negative bacteria. Olanexidine exhibits the bactericidal concentration of 109 μg/mL for Gram-positive bacilli[1].
Sulfanitran-13C6 is the 13C6 labeled Sulfanitran. Sulfanitran is an antibacterial and anticoccidial agent used in poultry feeds. Sulfanitran also is a multidrug resistance protein 2 (MRP2) stimulator that can increase the affinity of MRP2 for estradiol-17-β-D-glucuronide (E217βG).
Antibacterial agent 40 is an antibacterial agent (extracted from patent WO2015159265A1, compound C) [1].
Bombinin-Like Peptide (BLP-1) is an antimicrobial peptide from Bombina species.
AT-9010 tetrasodium, a triphosphate active metabolite of AT-527, is a potent inhibitor of NiRAN (a function essential for viral replication). AT-9010 tetrasodium can inhibit SARS-CoV-2 replication[1].
Macatrichocarpin A is a flavanone with anti-bacterial activity. Macatrichocarpin A inhibits Bacillus subtilis with MIC value of 26.5 μM. Macatrichocarpin A can be isolated from the leaves of Macaranga trichocarpa[1].
NSC10010 hydrochloride inhibits gammaherpesvirus associated B-lymphomas growth through activation of NF-kB and c-Myc-mediated signaling pathways. NSC10010 hydrochloride induces necrotic cell death in gammaherpesvirus infected B-cells. NSC10010 hydrochloride is also an inhibitor of Mtb ClpC1 ATPase[1][2].
2'-O-Methylcytidine is a 2'-substituted nucleoside as a inhibitor of HCV replication. 2'-O-Methylcytidine inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro, in a manner that is competitive with substrate nucleoside triphosphate[1].
Nafcillin, an antibiotic, is a reversible inhibitor of β-lactamase. Nafcillin exhibits bactericidal activity, and can be used for the research of staphylococcal infections[1][2][3][4].
L-Lysine6-13C (dihydrochloride) is a 13C-labeled Sulfamethoxypyridazine.
Tyrothricin is a polypeptide antibiotic mixture isolated from Bacillus brevis and consists of tyrocidines and gramicidins. Tyrothricin shows activity against bacteria, fungi and some viruses. Tyrothricin containing formulations are used in sore throat agents and in agents for the healing of infected superficial and small-area wounds[1].
Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle[1].
Ivermectin is a widely used antiparasitic agent in human and veterinary medicine. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs).
Sulfamerazine(RP-2632) is a sulfonamide antibacterial.Target: AntibacterialSulfamerazine, the monomethyl derivative of sulfadiazine, is 2-sulfanilamido-4-methylpyrimidine. Sulfamerazine is a sulfonamide drug that inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA) for binding to dihydropteroate synthetase (dihydrofolate synthetase). Sulfamerazine is bacteriostatic in nature. Inhibition of dihydrofolic acid synthesis decreases the synthesis of bacterial nucleotides and DNA [1].
Antifungal agent 35 (compound 24) is a potent antifungal agent. Antifungal agent 35 is a potent enhancer of antifungal activity of Fluconazole against C. albicans[1].
2'-Deoxyuridine-d2 is the deuterium 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]
ABC-1 is a phosphorylated analogue and a potential antiviral agent against Newcastle disease virus (NDV). ABC-1 has potent antiviral activity[1][2].
Penicillin V (Potassium)-d5 is the deuterium labeled Penicillin V Potassium[1]. Penicillin V Potassium (Phenoxymethylpenicillin potassium salt) is an orally active antibiotic. Penicillin V Potassium inhibits the growth of Streptococci, C. difficile and S. aureus. Penicillin V Potassium can be used for the research of otitis, sinusitis, pharyngitis and tonsillitis[2][3][4][5].
Triflumuron is a potent chitin synthesis inhibitor. Triflumuron shows the efficacy in emergence inhibition (EI) against Culex quinquefasciatus and Aedes albopictus, with EI50 values of 5.28 and 1.59 μg/L, respectively. Triflumuron can be used as an insecticide. Triflumuron represents a potential tool for the control of disease vectors in public health[1].
Sulfadimethoxine D4 is a deuterium labeled Sulfadimethoxine (Sulphadimethoxine). Sulfadimethoxine is a sulfonamide antibiotic used to treat many infections including treatment of respiratory, urinary tract, enteric, and soft tissue infections[1].
10-DEBC hydrochloride is a selective Akt inhibitor, with an IC50 of 1.28 μM. 10-DEBC hydrochloride is a novel anti-TB compound[1][2].
Rifapentine (Priftin; DL 473) is an antibiotic compound used in the treatment of tuberculosis.Target: AntibacterialRifapentine inhibits DNA-dependent RNA polymerase activity in susceptible cells. Specifically, it interacts with bacterial RNA polymerase but does not inhibit the mammalian enzyme. A review of alternative regimens for prevention of active tuberculosis in HIV-negative individuals with latent TB found that a weekly, directly observed regimen of rifapentine with isoniazid for three months was as effective as a daily, self -administered regimen of isoniazid for nine months. But the rifapentine-isoniazid regimen had higher rates of treatment completion and lower rates of hepatotoxicity . However the rates of treatment-limiting adverse events were higher in the rifapentine-isoniazid regimen [1].
Iclaprim-d6 (AR-100-d6) is the deuterium labeled Iclaprim. Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 μg/mL.
Justicidin C is an antiviral lignan. Justicidin C shows strong antiviral activity against vesicular stomatitis virus and low cytotoxicity against rabbit lung cells (RL-33)[1].
Ketoconazole is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.Target: CYP3A4 CYP24A1Ketoconazole, an imidazole anti-fungal agent, has often produced features of androgen deficiency including decreased libido, gynecomastia, impotence, oligospermia, and decreased testosterone levels, in men being treated for chronic mycotic infections [1]. Ketoconazole also is a cytochrome P450 inhibitor [2].Ketoconazole (KTZ), on the antischistosomal potential of these quinolines against Schistosoma mansoni infection by evaluating parasitological, histopathological, and biochemical parameters. Mice were classified into 7 groups: uninfected untreated (I), infected untreated (II), infected treated orally with PZQ (1,000 mg/kg) (III), QN (400 mg/kg) (IV), KTZ (10 mg/kg)+QN as group IV (V), HF (400 mg/kg) (VI), and KTZ (as group V)+HF (as group VI) (VII). KTZ plus QN or HF produced more inhibition (P<0.05) in hepatic CYP450 (85.7% and 83.8%) and CYT b5 (75.5% and 73.5%) activities, respectively, than in groups treated with QN or HF alone. This was accompanied with more reduction in female (89.0% and 79.3%), total worms (81.4% and 70.3%), and eggs burden (hepatic; 83.8%, 66.0% and intestinal; 68%, 64.5%), respectively, and encountering the granulomatous reaction to parasite eggs trapped in the liver.[3] CYP24A1 inhibitor enhances antiproliferative effects, increases systemic calcitriol exposure, and promotes the activation of caspase-independent apoptosis pathway.[4]
Zegruvirimat is an antiviral agent. Zegruvirimat has antiviral activity[1].
Dehydroacetic acid is an organic compound, classified as a pyrone derivative and is used mostly as a fungicide and bactericide.
Oxytetracycline calcium is an antibiotic belonging to the tetracycline class. Oxytetracycline calcium potently inhibits Gram-negative and Gram-positive bacteria. Oxytetracycline calcium is a protein synthesis inhibitor and prevents the binding from aminoacil-tRNA to the complex m-ribosomal RNA. Oxytetracycline calcium also possesses anti-HSV-1 activity[1][2][3].
PqsR/LasR-IN-1 (Compound 2a) is a potent inhibitor of PqsR and LasR systems in P. aeruginosa. PqsR/LasR-IN-1 also inhibits hERG with the IC50 of 6.77 µM[1].