Metabolismo

<p>NU227326 is a PROTAC degrader of indoleamine 2,3-dioxygenase 1 (IDO1) with a DC50 value of 4.5 nM. It effectively degrades IDO1 in U87 and GBM43 cells, with DC50 values of 7.1 nM and 11.8 nM, respectively. NU227326 exhibits favorable pharmacokinetic properties, with a plasma half-life of 5.7 hours and a brain tissue half-life of 11.8 hours. (Pink: ligand for target protein IDO1 ligand-1; Black: linker; Blue: ligand for E3 ligase Cereblon).</p>

<p>Beauverolide Ja: cyclotetradepsipeptide, CaM inhibitor; Kd 0.078 μM, Ki 0.39 μM; from Isaria fumosorosea.</p>

<p>'(2α,3β,4α)-2,3,19-Trihydroxyurs-12-ene-23,28-dioic acid, a saponin isolated from Rubus ellipticus var.</p>

<p>Promothiocin A is an antibiotic.</p>

<p>(±)-Hexanoylcarnitine chloride is a fatty acid metabolite that breaks down fatty acids into small compounds that can be utilized by the body.</p>

<p>VDR agonist 3 (Compound E15) is a potent activator of the vitamin D receptor (VDR). It effectively inhibits the activation of hepatic stellate cells (HSC) via VDR. In a model of liver fibrosis induced by CCl4 in mice, VDR agonist 3 significantly alleviates liver fibrosis without causing hypercalcemia.</p>

<p>Dextranase, a glucan hydrolase, breaks down α-(1,6)-glucosidic bonds in dextran, useful in food, sugar modification, medicine, and more.</p>

<p>Berninamycin D, a cyclic peptide derived from Streptomyces bernensis through fermentation, is recognized as a fungal metabolite [1].</p>

<p>Methylcardol triene, a phenolic compound present in cashew nut shell liquid, demonstrates α-glucosidase inhibition (IC50= 39.6 µM) and exhibits schistosomicidal properties by eliminating 100% of adult S. mansoni worms within 24 hours at 100 and 200 µM concentrations. Moreover, it serves as a precursor for synthesizing mono- and bis-benzoxazines.</p>

<p>Beauveriolide I, a cyclodepsipeptide from Beauveria, inhibits lipid droplet and cholesterol synthesis in mouse macrophages; IC50=0.78 μM.</p>

<p>Phenolic acid is an endogenous metabolite.</p>

<p>OPC18750 HCl is a phosphodiesterase inhibitor with positive inotropic effects that can be used to study asthma, cancer, diabetes, and psychiatric disorders.</p>

<p>Cortisol sulfate sodium, a Cortisol metabolite, binds specifically to intracellular transcortin.</p>

<p>Xanthine oxidase-IN-8 (Icarisids J) (Compound 7) serves as an inhibitor of xanthine oxidase, exhibiting an inhibitory concentration (IC50) value of 29.71 μM [1</p>

<p>Irsenontrine (E2027) maleate is a selective and orally active inhibitor of phosphodiesterase 9 (PDE9). It can be utilized in the study of neurological diseases.</p>

<p>Glycerol phosphate dehydrogenase catalyzes the conversion of dihydroxyacetone phosphate to α-glycerol phosphate [1] .</p>

<p>Myristoyl coenzyme A lithium, a compound marked by lithium in its myristoylated form, plays a crucial role in the biochemical mechanism of myristoylation, essential for both viral functionalities and tumor growth in colon epithelial cells. This process is predominantly governed by N-myristoyltransferase (NMT), which exhibits increased activity in colon epithelial tumors compared to normal cells. The activity of NMT is significantly influenced by the reduction of coenzyme A (CoA), a vital regulator that enhances NMT's ability to induce myristoylation, unlike its oxidized form which impedes this process. Consequently, Myristoyl coenzyme A serves as an inhibitor to the demyristoylation activity, showcasing its potential as an anticancer and antiviral agent.</p>

<p>5A2-SC8 TFA is an ionizable amino lipid used in lipid nanoparticles (LNPs), offering high delivery potential and low in vivo toxicity. It effectively delivers small RNAs, such as siRNA and miRNA, to tumor cells. Moreover, 5A2-SC8 TFA LNPs provide unique delivery paths for RNA within the liver, enhancing therapeutic outcomes in cancer models.</p>

<p>GS-493: Specific SHP2 inhibitor, very potent (IC50=71 nM), 29x affinity vs. SHP1, 45x vs. PTP1B; hinders cancer cell growth/movement.</p>

<p>α-Muricholic acid is the most abundant primary bile acid in rodents.</p>