Metabolism

EpoY (SD-142) is an irreversible inhibitor of the primary brain microtubule-associated tyrosine carboxypeptidase (TCP), a complex formed by vasohibin-1 (VASH1) and small vasohibin-binding protein (SVBP). By inhibiting TCP with an IC50 value of approximately 500 nM, EpoY effectively reduces the levels of detyrosinated α-tubulin, which is crucial for microtubule dynamics and neuronal differentiation. This inhibition results in significant differentiation defects and is linked to potential issues related to cancer and cardiomyopathy.

3-Ferrocenylpropionic anhydride is extensively used in compound synthesis, serving as an intermediary for producing various bioactive compounds. Additionally, by modulating specific enzyme activities, 3-Ferrocenylpropionic anhydride has demonstrated potential anti-tumor properties.

Lipid 12T-O14 is a lipid nanoparticle that facilitates the delivery of local mRNA vaccines and systemic mRNA agents.

FTI-2153 TFA inhibits farnesyltransferase with high selectivity (IC50: 1.4 nM), over 3000x more than Rap1A processing.

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.

Gcase activator 2 is a β-glucocerebrosidase activator that induces dimerization of GCase, increases lysosomal substrate metabolism.

DG013A inhibits ERAP1 & ERAP2 (IC50: 33 nM & 11 nM) to research autoimmune diseases & cancer.

1-Stearoyl-sn-glycerol 3-phosphate sodium, a biologically active phospholipid, plays a crucial role in regulating cell motility, proliferation, invasion, survival, and the production of growth factors through interactions with G protein-coupled receptors (GPCR). Synthesized during the formation of membrane phospholipids, this compound typically has a low plasma concentration (approximately 100nM) and originates from various cell types, including activated platelets, epithelial cells, leukocytes, neuronal cells, and tumor cells. Its distinctive structure features stearic acid at the sn-1 position and a hydroxyl group at the sn-2 position.

D-2-Phosphoglyceric acid is a crucial metabolic intermediate known for its role in enhancing cellular energy metabolism and regulating biosynthesis. It plays a key role in both glycolysis and photosynthesis, which are essential for cellular energy supply. Additionally, D-2-Phosphoglyceric acid serves as a biomarker for monitoring metabolic states in various organisms.

Pyrocatechol sulfate, a phenolic metabolite found in human plasma, is associated with the intake of specific foods such as berries and the state of the gut microbiome. It serves as a potential urinary biomarker for kidney function, dialysis clearance rates, whole grain consumption, and regular coffee intake. Additionally, in conjunction with other phenolic sulfates, pyrocatechol sulfate plays a role in regulating various biological functions, including those related to brain health and the rhythmic beating of cardiac cells.

CK1δ-IN-6 (Compound 303) is an inhibitor of Casein kinase 1δ, with potential applications in Alzheimer's disease research.

PDE5-IN-8 (compound 2) is an inhibitor of PDEs.

(6S)-CP-470711 (Compound 8) acts as an inhibitor of sorbitol dehydrogenase (SDH) in both humans and rats, exhibiting inhibitory concentrations (IC50) of 19 nM and 27 nM, respectively. Additionally, (6S)-CP-470711 has been shown to ameliorate diabetes in rats induced by Streptozotocin.

Compound LE-77, known as FXR/CES2 modulator 1, functions as a dual regulator that activates FXR and inhibits CES2. It effectively mitigates the intestinal toxicity of irinotecan.

Thioquinapiperifil dihydrochloride is a potent, selective PDE-5 inhibitor (IC50: 0.074 nM) for research.

JA2 is an inhibitor of metalloendopeptidase 24.15 that enhances the hypotensive response to bradykinin in rats.

α-Amylase-IN-1 is an α-Amylase inhibitor (IC50: 0.5509 μM).

Nomelidine, the active N-demethylated metabolite of zimelidine, has been used as an antidepressant and analgesic.

MCTR3, derived from DHA via maresin 1 in macrophages, hastens tissue healing and reduces inflammation and eicosanoids post-E. coli infection in mice.