1g-244

1G244 is an inhibitor of DPP8 9 with antiatherosclerotic and antimyeloma properties. 1G244 had the IC50 values of 14 and 53 nM against DPP8 and DPP9, and The Ki values for 1G244 were 0.9 and 4.2 nM for DPP8 and DPP9

Antibacterialagent 244 is a compound that exhibits broad-spectrum antibacterial activity and oral efficacy, primarily targeting Gram-positive bacteria with a minimum inhibitory concentration (MIC) of 1-4 μg mL. It possesses low hemolytic toxicity (HC50 of 111.6 μg mL). The mode of action for Antibacterialagent 244 involves disrupting the bacterial transmembrane potential and increasing membrane permeability, which leads to the leakage of cellular contents such as DNA and proteins, ultimately causing bacterial death. This compound is useful in research related to infections caused by Gram-positive bacteria.

Decanal, 2-methylene- is a biochemical.

3-hydroxy Myristic acid methyl ester is a hydroxylated fatty acid methyl ester that has been found in E. camaldulensis and E. torelliana extracts. [1] It is active against M. tuberculosis (MIC = 49.5 μg ml) and is non-cytotoxic to Vero cells (IC50 = >100 μM). 3-hydroxy Myristic acid methyl ester is also a volatile compound that contributes to the aroma of red wild strawberries (F. pentaphylla) but is not present in cultivated strawberries (Fragaria x ananassa).[2] Reference:[1]. Lawal, T.O., Adeniyi, B.A., Adegoke, A.O., et al. In vitro susceptibility of Mycobacterium tuberculosis to extracts of Eucalyptus camaldulensis and Eucalyptus torelliana and isolated compounds. Pharm. Biol. 50(1), 92-98 (2012).[2]. Duan, W., Sun, P., Chen, L., et al. Comparative analysis of fruit volatiles and related gene expression between the wild strawberry Fragaria pentaphylla and cultivated Fragaria × ananassa. Eur. Food Res. Technol. 244(1), 57-72 (2018).

NHC-triphosphate triammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) as a triphosphate form[1]. NHC-triphosphate triammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA[1][2]. In an intracellular metabolism assay, HCV replicon cells are treated with 10 μM 3H-labeled NHC, and intracellular nucleotide levels are determined after 1, 2 and 8 hours incubations. NHC is rapidly convered into the mono-, di-, and triphosphate forms, and NHC-TP reaches up to 71.12 pM after 8 hours[1].NHC-triphosphate triammonium (NHC-TP) (5-40 μM) absence leads to full-length polymerization products, it can be a weak alternative substrate. In addition, incorporation of NHC-TP instead of CTP increases the molecular weight of the polymerization product by 16 (one extra oxygen) for each event and an obvious electrophoretic shift is observed in cell-free HCV NS5B polymerization reactions[1].Huh-7 cells are incubated with (10-50 μM; 4 h) NHC or a McGuigan phosphoramidate prodrug of NHC. Intracellular levels of the parental compounds and phosphorylated metabolites are measured using LC-MS/MS. Small amounts of NHC-monophosphate (MP) and NHC-diphosphate (DP) can be observed, while NHC-triphosphate triammonium remains the most abundant metabolite[2].NHC-triphosphate triammonium (NHC-TP) metabolite may directly target the viral polymerase and behave as a nonobligate chain terminator. It plays a prominent role in inhibiting early negative-strand RNA synthesis, either through chain termination or mutagenesis, which may in turn interfere with correct replicase complex formation. [1]. Stuyver LJ,et al. Ribonucleoside analogue that blocks replication of bovine viral diarrhea and hepatitis C viruses in culture.Antimicrob Agents Chemother. 2003 Jan;47(1):244-54. [2]. Maryam Ehteshami, et al. Characterization of β-d- N4-Hydroxycytidine as a Novel Inhibitor of Chikungunya Virus.

Pyrithiamine hydrobromide, an inhibitor of thiamine metabolism that acts as a substrate for thiamine pyrophosphate kinase, causes neurologic symptoms similar to wernickke - korsakoff syndrome in animals.

Glycerophosphorylethanolamine is an active phosphodiester metabolite of phosphatidylethanolamine.1,2It promotes aggregation of amyloid-β (1-40) (Aβ40)in vitro, and levels of glycerophosphorylethanolamine are elevated in postmortem brains isolated from patients with Alzheimer's disease. 1.Klunk, W.E., Xu, C.J., McClure, R.J., et al.Aggregation of β-amyloid peptide is promoted by membrane phospholipid metabolites elevated in Alzheimer's disease brainJ. Neurochem.69(1)266-272(1997) 2.Blusztajn, J.K., Lopez Gonzalez-Coviella, I., Logue, M., et al.Levels of phospholipid catabolic intermediates, glycerophosphocholine and glycerophosphoethanolamine, are elevated in brains of Alzheimer's disease but not of Down's syndrome patientsBrain Res.536(1-2)240-244(1990)