Metabolismo

<p>Z-Pro-prolinal, an orally active PREP inhibitor, IC50: 0.4 nM in porcine.</p>

<p>9c(i472) blocks 15-LO-1 (IC50=0.19μM), lowers NF-κB in RAW-Blue cells, &amp; cuts Nos2/lipid peroxidation in RAW 264.7 at 0.2-5μM.</p>

<p>Levothyroxine acyl glucuronide (Thyroxine Acyl-β-D-glucuronide), the acyl glucuronide formation of thyroxine (T4), an endogenous metabolite.</p>

<p>THX6 is an activator of human mitochondrial protease ClpP, with an EC50 of 1.18 μM. It displays cytotoxicity in ONC201-resistant SU-DIPG-VI cells, with an IC50 of 0.13 μM. THX6 inhibits the expression of mitochondria-related proteins (such as parkin, TFAM, NRF1, SDHA), leading to impaired mitochondrial function. Additionally, THX6 affects cell membrane lipid metabolism and exhibits antitumor potential.</p>

<p>hMAO-B-IN-4 is a selective, reversible and blood–brain barrier (BBB) penetrable inhibitor of human monoamine oxidase-B (hMAO-B, IC50=0.067 μM, Ki= 0.03 μM, hMAO</p>

<p>α-Glucosidase-IN-89 (8g) is an inhibitor of α-glucosidase, with an IC50 of 0.5 μM and a Ki of 0.46 μM.</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>MPO-IN-6 (compound ADC) is an electrophilic agent with excellent antioxidant and anti-inflammatory properties. It acts as an inhibitor of myeloperoxidase (MPO), dipeptidyl peptidase-4 (DPP-4), and α-glucosidase (α-GD), with IC50 values of 10 μM, 31.02 μM, and 46.05 μM, respectively. MPO-IN-6 may serve as a potential cardiovascular protective agent.</p>

<p>Ribose 5-phosphate: Intermediate in oxidative PPP, final in non-oxidative PPP, used for nucleotide and nucleic acid synthesis.</p>

<p>Pyruvate kinase is a glycolytic enzyme that catalyzes the conversion of phosphoenolpyruvate and ADP to pyruvate and ATP [1] .</p>

<p>(R,S)-Carvedilol glucuronide is a racemic mix, metabolized by UGT1A1, UGT2B4, and UGT2B7.</p>

<p>DSPE-PEG5000-APRPG is a PEG compound composed of DSPE and the APRPG peptide, utilized for drug delivery.</p>

<p>Toddacoumalone, a natural PDE4 inhibitor, shows promise for inflammatory disease research.</p>

<p>Impurity B is a byproduct of Calcitriol, the active hormone form of vitamin D3 and VDR activator.</p>

<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>DP-1 hydrochloride is a degradation product of SDC-TRAP-0063, a fragment of Ganetespib, a heat shock protein 90 (HSP90) inhibitor with antitumor activity.</p>

<p>Propiverine N-oxide is the primary metabolite of propiverine hydrochloride, and it influences bladder contraction and saliva secretion in miniature pigs.</p>

<p>Isomer-Turosteride, a novel 5α-reductase inhibitor, reduces prostate DHT and has anticancer properties without raising T levels.</p>

<p>Decanoyl coenzyme A (Decanoyl CoA) serves as a primer for the fatty acid elongation system in Mycobacterium smegmatis [1].</p>

<p>Gluconapin serves as a precursor to sulforaphane, an effective anticancer isothiocyanate. It has been found to reduce the increase in plasma triglycerides induced by corn oil consumption in mice.</p>