Métabolisme

<p>PR280 is a potent inhibitor of dihydroceramide desaturase 1 (Des1) with an IC50 of 700 nM. It forms hydrogen bonds with amino acid residues of Des1, while its cyclopropenone group may coordinate with the iron center, stabilizing its binding at Des1's active site. This inhibits the ceramide biosynthesis pathway, preventing dihydroceramide (dhCer) from converting into ceramide. PR280 can be used in research related to sphingolipid metabolism disorders, including cancer and metabolic diseases.</p>

<p>Endogenous metabolite: 1-myristoyl-2-stearoyl-sn-glycero-3-phosphocholine, a phosphatidylcholine example.</p>

<p>α-Amylase/α-Glucosidase-IN-11 (Compound 5d) is an isoxazoline-indigo hybrid with notable antidiabetic properties. It acts as a competitive inhibitor of the key digestive enzymes α-amylase (IC50 = 30.39 μM) and α-glucosidase (IC50 = 65.1 μM). Additionally, it does not penetrate the blood-brain barrier.</p>

<p>4β-hydroxy Cholesterol is a useful organic compound for research related to life sciences. The catalog number is T21530 and the CAS number is 17320-10-4.</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>Transketolase-IN-6 (Compound 6bj) serves as a lead compound for herbicides. It achieves approximately 80% root inhibition in redroot pigweed (Amaranthus retroflexus) and green foxtail (Setaria viridis). Moreover, Transketolase-IN-6 is an effective inhibitor of transketolase (TK).</p>

<p>Gemopatrilat is a an vasopeptidase inhibitor.</p>

α-Glucosidase-IN-67 (compound 5k) is a potent inhibitor of α-glucosidase, exhibiting IC50 values of 0.31 µM for α-glucosidase and 4.51 µM for α-amylase. This compound shows potential for research in type 2 diabetes.

<p>SGK1-IN-3 hydrochloride (compound 3a) is an efficacious, orally bioavailable SGK1 inhibitor. The serine/threonine kinase SGK1 acts as an activator of the β-catenin pathway and strongly stimulates cartilage degradation, being upregulated under genomic control in diseased osteoarthritic cartilage. SGK1-IN-3 hydrochloride holds potential for osteoarthritis research.</p>

<p>α-Glucosidase-IN-46 is a potent inhibitor of α-glucosidase, with an IC50 of 26.0 μM. This compound is applicable in the research of Type 2 diabetes.</p>

Fmoc-Cys-Asp10 (TFA) is a non-releasable oligopeptide linker involved in synthesizing releasable oligopeptide linkers. These releasable linkers are used to deliver drugs to fracture-targeting oligopeptides, thereby reducing the healing time of fractured femurs.

α-Glucosidase-IN-58 (Compound 6d) is an α-glucosidase inhibitor with an IC50 of 1.47 μM.

<p>Desmethylazelastine, Azelastine's metabolite; 97% protein bound; 54-hour half-life; treats allergies, asthma, diabetes, SARS-CoV-2.</p>

<p>alpha-1,3-Galactosyltransferase (GTB) synthesizes α-Gal epitopes by transferring galactose to specific acceptors.</p>

α-Amylase/α-Glucosidase-IN-13 (Compound 5d) is a dual inhibitor of α-amylase and α-glucosidase, and is useful in diabetes research.

<p>(+)-Menthofuran is a useful organic compound for research related to life sciences and the catalog number is T125544.</p>

<p>1,3-Diphenethylurea (N,N'-Bis(phenethyl)urea) is a marine derived natural products found in Lissoclinum patella.</p>

<p>(Ile8)-Oxytocin acetate is a neurohypophysial hormone analog of oxytocin produced in marsupials.</p>

<p>CH3OCO-D-CHA-Gly-Arg-pNA acetate serves as a chromogenic substrate for Factor Xa, as documented in sources [1] [2].</p>

hDHODH-IN-8: potent hDHODH inhibitor, IC50 = 16 nM, antiproliferative, soluble, may research lymphoma.

HexokinaseIIVDACbinding domain peptide (Hxk2VBD peptide) is a cell-permeable peptide derived from the hexokinase II VDAC binding domain. This peptide inhibits the mitochondrial localization of hexokinase 2 (HXK2) and also suppresses neurotrophic factor-induced axon growth.

α-Amylase/α-Glucosidase-IN-14 is an orally bioactive inhibitor of α-amylase and α-glucosidase, with IC50 values of 45.53 μM and 27.73 μM, respectively.

<p>α-Amylase/α-Glucosidase-IN-9 (compound 5h) is a dual inhibitor of α-amylase (IC50= 16.4 μM) and α-glucosidase (IC50= 31.6 μM).</p>

<p>Xanthine oxidase-IN-13 (Compound 10) is a selective inhibitor of xanthine oxidase, with an IC50 of 149.56 μM for bovine xanthine oxidase. It is utilized in the study of inflammatory arthritis.</p>

<p>hCA/VEGFR-2-IN-3 (compound 8j) is an indolinonylbenzenesulfonamide with potential as a dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2.</p>

<p>MK-4074 is a liver-specific acetyl-CoA carboxylase ACC1 and ACC2 inhibitor(IC50 of 3 nM).</p>

PFKFB3-IN-2 is a 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) inhibitor.

<p>Kijanimicin: antitumor, antibiotic with unique activity against Gram-positive, anaerobic bacteria, and malaria.</p>

<p>DSPE-PEG2000-WYRGRL is a PEG compound composed of DSPE and the cartilage-targeting peptide (WYRGRL). The peptide WYRGRL can specifically bind to type II collagen α1. DSPE-PEG2000-WYRGRL is utilized for drug delivery.</p>

<p>α-Amylase/α-Glucosidase-IN-15 (compound 6C) is an orally active inhibitor of α-glucosidase (α-Glucosidase) and α-amylase (α-amylase), with IC50 values of 21 μM and 61 μM, respectively.</p>

<p>α-Amylase/α-Glucosidase-IN-12 (compound 10k) is a dual inhibitor targeting α-glucosidase and α-amylase, with IC50 values of 34.52 nM and 24.62 nM, respectively. This inhibitor is designed based on [triazolo[4,3-b][1,2,4]triazine and holds potential for diabetes research.</p>

<p>DSPE-PEG2000-CCK8 is a PEG compound comprising DSPE and Cholecystokinin-8 (CCK8). Cholecystokinin-8 exhibits peptide activity responsible for regulating gallbladder contractions and digestive system functions. DSPE-PEG2000-CCK8 is applicable for drug delivery.</p>

<p>Sorbifolin is a flavone glucoside from Pterogyne nitens with myeloperoxidase inhibition (IC50: 19.2 nM) and radical scavenging effects.</p>

Transketolase-IN-5 (compound 6ba) is an inhibitor of transketolase. It exhibits herbicidal activity against Amaranthus retroflexus, Setaria viridis, and Digitaria sanguinalis.

<p>Fasnall HCl is a selective FASN inhibitor that acts through its co-factor binding sites.</p>

<p>Oglemilast (GRC 3886) suppresses pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo.</p>

<p>DSPE-PEG1000-NGR is a PEG compound composed of DSPE and the Asn-Gly-Arg (NGR) peptide. The NGR peptide has the capability to target the CD13 antigen present in tumor vasculature. DSPE-PEG1000-NGR can be utilized for drug delivery.</p>

<p>FZQ-21 (Compound 70P) is an inhibitor of the water-soluble epoxide hydrolase (sEH), with an IC50 value of 4 nM. The IC50 for inhibiting human sEH is 1.5 nM, which is comparable to that of EC5026 (1.7 nM). FZQ-21 is utilized in sepsis research.</p>

Girentuximab (G250) is an anti-carbonic anhydrase IX (CAIX) monoclonal antibody with anti-cancer activity for the study of uroepithelial carcinoma PET (ZiPUP).

<p>E 6080 HCl is a 5-lipoxygenase inhibitor and can be used to study bronchial diseases.</p>

<p>PTP1B-IN-27 (Compound 7i) is an inhibitor of protein tyrosine phosphatase 1-B (PTP-1B) with an IC50 of 8.2 µM. Additionally, it inhibits α-glucosidase with an IC50 of 120 µM and exhibits competitive inhibition characteristics (Ki=118 µM).</p>

<p>Tetranor-PGEM, the primary urinary byproduct of PGE1 and PGE2, marks PGE2 production; humans excrete 7-40 μg daily.</p>

<p>5-Aminolevulinic acid: heme synthesis intermediate, photosensitizer, antineoplastic, prodrug, treats actinic keratosis with blue light.</p>

<p>Compound 5C, referred to as Pkm2-in-4, is a selective PKM2 inhibitor (IC50 = 0.35 µM) that modulates pyruvate-dependent respiration and promotes mitochondrial</p>

<p>CAIR, an E. coli metabolite, helps identify its PurE active site and aids in fungal purine synthesis.</p>

<p>hDHODH-IN-13 (compound w2), an inhibitor of human dihydroorotate dehydrogenase (hDHODH), exhibits an IC50 of 173.4 nM and has potential research applications in</p>

<p>DSPE-PEG1000-ANG is a PEG compound composed of DSPE and a dual-targeting ligand (Angiopep-2, ANG). ANG demonstrates high LRP1 binding efficiency and has been utilized for targeting glioma delivery. DSPE-PEG1000-ANG is suitable for drug delivery applications.</p>

<p>ICMT-IN-35 (compound 10n), an ICMT inhibitor with an IC50 value of 0.8 μM, is a FTPA-triazole derivative.</p>

Photo-DL-lysine is a photo-reactive amino acid based on DL-lysine used to capture proteins that are post-translationally modified by lysine binding.

<p>4,5-Dimethylthiazole exhibits inhibitory against mitochondrial respiration in liver cells and can be used in biochemical experiments and drug synthesis.</p>

<p>DSPE-PEG2000-EB1 is a PEG compound composed of DSPE and the pH-responsive transmembrane peptide (EB1). It is utilized for drug delivery.</p>

<p>Carbonic anhydrase inhibitor18 (Compound 9) is an inhibitor of human carbonic anhydrase (hCA) isozymes, with Ki values of 604.8 nM for hCA I, 333.6 nM for hCA II, 1.9 nM for hCA IX, and 6.7 nM for hCA XII. Carbonic anhydrase inhibitor18 is applicable in cancer research.</p>

Poly(4-vinylphenol) is an endogenous metabolite.

<p>Sarcinapterin is a coenzyme isolated from Methanosarcina barkeri.</p>

<p>hCA/VEGFR-2-IN-4 (compound 15b), an indolinylbenzenesulfonamide, serves as a potential dual inhibitor targeting cancer-related human carbonic anhydrases hCA IX/</p>

<p>Selective NOX1 inhibitor; IC50 at 20 nM; spares NOX2/4/5 and xanthine oxidase; reduces HT-29 O2- and hinders VEGF-induced cell migration.</p>

Phosphate acetyltransferase, an enzyme, reversibly transfers acetyl groups to CoA, aiding in acetate assimilation/dissimilation.

<p>SCD1 inhibitor-3 (ML-270) is a highly effective and orally available compound that inhibits SCD1 with remarkable safety.</p>

<p>Glycogen phosphorylase-IN-2 (compound 9C) is an inhibitor of glycogen phosphorylase, with a Ki value of 1.9 nM and an IC50 value of 4 nM.</p>

<p>10-FTHF is a donor of formyl groups in anabolism used as a substrate in formyltransferase reactions, which is important in purine biosynthesis.</p>

<p>PTPN22-IN-2 (Compound 8b-19) is a PTPN22 inhibitor with an IC50 of 250 nM and is applicable in immunoregulation research.</p>

<p>Folcysteine, a cysteine derivative, may fight tumors, aids in DNA synthesis, repair, methylation, and acts as a folate cofactor.</p>

<p>DSPE-PEG1000-KAA is a PEG compound comprised of DSPE and the CKAAKNK (KAA) peptide. The CKAAKNK peptide specifically binds to tumor vasculature in RIP-Tag2 transgenic mice. DSPE-PEG1000-KAA is applicable for drug delivery.</p>

<p>D-LDH is an oxidoreductase turning D-lactate into pyruvate, using NAD+/NADP+; prevalent in bacteria and fungi, key for biochemical research.</p>

<p>PTP1B-IN-22 is a protein tyrosine phosphatase 1B (PTP1B) inhibitor that inhibits glucose uptake in skeletal muscle L6 myotubes.</p>

<p>Hydroxy bosentan (Ro 48-5033), a Bosentan metabolite, is liver-processed with 10-20% of its activity.</p>

<p>DPPS is a negatively charged diacyl-phospholipid used to create cationic vesicles and liposomes.</p>

<p>Aclimostat (ZGN-1061) is a MetAP2 inhibitor with strong preclinical results, improving obesity-related metrics and gene expression.</p>

<p>Antibacterialagent 218 (compound d28) is an orally active inhibitor of sterol 24-C-methyltransferase with an IC50 value of 0.273 μM. It also displays antifungal activity against Candida albicans SC5314, with an IC50 of 0.25 μg/mL.</p>

<p>α-Glucosidase-IN-49 (compound C23) is a potent inhibitor of α-Glucosidase, with an IC50 of 0.52 μM. This compound exhibits oral bioactivity, effectively lowering blood glucose levels and enhancing glucose tolerance in mice.</p>

<p>Eubulus-A80 is a anti-tumor agent (WO2021/183702, Compound A80).</p>

<p>5(S)-HpETE is a PUFA made by 5-LO from arachidonic acid, metabolized into LTA4, a key leukotriene precursor.</p>

<p>LYP-8 is a potent NAMPT degrader that achieves a maximum degradation rate of 97% in NAMPT within SKOV-3 cells at a concentration of 0.5 μM. LYP-8 also demonstrates anticancer activity both in vitro and in vivo.</p>

<p>DSPE-PEG2000-pPB is a PEG compound comprised of DSPE and the cyclic oligopeptide (pPB). The pPB component exhibits a high binding affinity for PDGFRβ, which is overexpressed on activated hepatic stellate cells (HSC). DSPE-PEG2000-pPB is utilizable for drug delivery applications.</p>

<p>ω-Muricholic acid (ω-MCA) is a murine-specific secondary bile acid.</p>

<p>DSPE-PEG2000-K237 is a PEG compound consisting of DSPE and the KDR-targeting peptide (K237). K237 functionally disrupts the interaction between VEGF and KDR receptors, resulting in significant biological effects such as inhibition of angiogenesis and tumor growth. DSPE-PEG2000-K237 is applicable in drug delivery.</p>

<p>VM4-037 is a PET imaging agent used for carbonic anhydrase IX.</p>

<p>Camellianin B, a flavonoid from Camellianin A, has antioxidant effects and blocks ACE.</p>

<p>DSPE-PEG5000-M2pep is a PEG compound composed of DSPE and the M2 macrophage-targeting peptide (M2pep). Serving either as a monovalent or multivalent ligand, M2pep is conjugated with pro-apoptotic peptides to direct toxicity specifically toward M2 macrophages. DSPE-PEG5000-M2pep is applicable for drug delivery.</p>

<p>hCA/Wnt/β-catenin-IN-1 (Compd 15) serves as an inhibitor with selective affinity for hCA isoforms II, IX, and XII, exhibiting K i values of 33.6, 24.1, and 6.8</p>

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

<p>DSPE-PEG2000-PP1 is a PEG compound composed of DSPE and the PP1 peptide. The PP1 peptide specifically targets inflammatory atherosclerotic plaques. DSPE-PEG2000-PP1 is utilized in drug delivery applications.</p>

<p>YF704 (compound 4w), a selective allosteric inhibitor of SHP2, exhibits antiproliferative effects and induces apoptosis in cancer cells with an IC50 of 0.25 μM.</p>

<p>Dihomo-γ-Linolenic acid methyl ester is the methyl ester form of Dihomo-γ-Linolenic acid which has anti-inflammatory and anti-proliferative effects.</p>

<p>hCA IX-IN-1 inhibits hCA I/II/IX/XII with Ki of 331.4/28.4/9.4/17.8 nM, has anticancer properties.</p>

<p>Cyperine is a useful organic compound for research related to life sciences. The catalog number is T125020 and the CAS number is 33716-82-4.</p>

<p>DSPE-PEG2000-CSTSMLKAC is a PEG compound composed of DSPE and CSTSMLKAC. CSTSMLKAC can mediate phage selective homing to ischemic heart tissue. DSPE-PEG2000-CSTSMLKAC is suitable for drug delivery.</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>AminopeptidaseN inhibitor 2 is an APN inhibitor (IC50: 4.3 μM) with antitumor properties.</p>

<p>Pyrindolol, a S. alboverticillatus metabolite, inhibits bovine β-galactosidase at 2 μg/ml in acid; not effective on other species' enzymes.</p>

UAA crosslinker 2 is a phenylalanine derivative.

<p>Aeruginosin B is a biochemical.</p>

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

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

<p>D-Fructose 1-phosphate disodium salt, a derivative of fructose, serves as a crucial intermediate in glucose metabolism.</p>

<p>MCU-i11 is a novel negative modulator of the MCU, binding MICU1 and impairing muscle cell growth.</p>

<p>Fellutanine A is a useful organic compound for research related to life sciences. The catalog number is T129801 and the CAS number is 175414-35-4.</p>

<p>Triethyl phosphate is a chemical compound. It can be called "phosphoric acid, triethyl ester".</p>

<p>5-Methoxyresorcinol (Flamenol) is a chemical intermediate.</p>

<p>β-Cryptoxanthin is isolated from Satsuma mandarin orange with an anti-stress effect. It is an oxygenated carotenoid and an antioxidant.</p>