Metabolism

Lipid PPz-2R1 is an ionizable cationic lipid employed in crafting lipid nanoparticles (LNPs) for mRNA delivery both in vitro and in vivo. LNPs with lipid PPz-2R1, encapsulating an mRNA reporter, target the lungs preferentially over the heart, liver, spleen, and kidneys in mice. Additionally, these LNPs, when encapsulating mRNA encoding phosphatase and tensin homolog (PTEN), enhance PTEN protein levels in PTEN-deficient Lewis lung carcinoma (LLC) cells. In an orthotopic murine LLC model, these Lipid PPz-2R1-containing LNPs, carrying PTEN mRNA, reduce tumor growth either when administered alone or alongside an antibody against programmed cell death protein 1 (PD-1).

Cephapirinlactone is a metabolite of the antibiotic Cephapirin.

CYP1B1-IN-2 (compound 9j) is a highly potent and selective inhibitor of CYP1B1, a cytochrome P450 enzyme. It exhibits an IC50 value of 0.52 nM [1].

Glycerophosphoglycerol is a precursor in phospholipid synthesis. By enhancing phospholipid formation, it aids in the reconstruction and proliferation of membrane structures in tumor cells. Glycerophosphoglycerol holds promise for research in breast cancer cells.

TKL-IN-2 (Compound 7m) is a TKL inhibitor with an IC50 of 0.11 mg/L against SvTKL. It exhibits excellent herbicidal activity against Digitaria sanguinalis and Amaranthus retroflexus, while being safe for corn, wheat, soybean, and cotton. TKL-IN-2 is suitable for research in weed control in crop fields.

ACLY-IN-1 (compound 55) is a potent ACLY inhibitor with an IC50 of 8.3 nM, and it can be utilized in hyperlipidemia research.

NAZ2329: Cell-permeable, targets R5 RPTPs, inhibits hPTPRZ1 (IC50=7.5 μM) & hPTPRG (IC50=4.8 μM), hampers glioblastoma growth, affects stem cell traits.

WR 199507 trihydrobromide is a primary aminoquinoline metabolite that induces the formation of methemoglobin in canine erythrocyte lysates.

hCAIX/XII-IN-15 (Compound 17β) is an inhibitor of hCA IX and hCA XII, exhibiting Ki values of 0.42 and 4.37 μM, respectively. It demonstrates a pro-apoptotic effect in multiple myeloma cells.

HIV-1 inhibitor-40 (4ab) is a potent NNRTI (EC50: 1.9 nM), non-toxic in vivo, and a sensitive CYP inhibitor.

HIF-1/2α-IN-1, an orally active compound, functions as an inhibitor of HIF-2α.

Carbonic anhydrase inhibitor28 (Compound 11) serves as an inhibitor for the Pseudomonas aeruginosa carbonic anhydrase. It exhibits antibacterial activity, with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of 0.5 and 1 μg/mL, respectively, against P. aeruginosa. Carbonic anhydrase inhibitor28 is utilized in research focused on anti-infection applications.

ONL-1204 is a small molecule, CD95 antigen inhibitor (Fas inhibitor) being developed by ONL Therapeutics for the treatment of retinal detachment.

Casein Kinase II Inhibitor IV HCl promotes keratinocyte differentiation, potential for skin disorder therapy.

Imipramine Blue chloride is an effective anti-invasive agent capable of inhibiting glioma invasion. It suppresses the production of reactive oxygen species (reactive oxygen species) mediated by NADPH oxidase.

PF-07202954, a weakly basic diacylglycerol O-acyltransferase 2 (DGAT2) inhibitor, exhibits an inhibition concentration half-maximum (IC50) of 10 nM against

Desmonomethylpromazine is a demethylated metabolite of Promazine that can penetrate the brain. It enters red blood cells and tissues via passive diffusion and is distributed in organs such as the lungs, liver, and kidneys in rats.

7-Hydroxyrisperidone (7-RispOH) is a metabolite of Risperidone. Risperidone acts as a 5-HT2 receptor blocker, an inhibitor of P-glycoprotein (P-Glycoprotein), and an antagonist of the dopamine D2 receptor.

Inosine 5'-diphosphate sodium, a purine ribonucleoside diphosphate with inosine as its nucleobase, plays a role in intracellular energy metabolism and signal transduction processes.

Phocaecholic acid, a bile acid, has been identified in the bile of ducks (A. platyrhynchos).