Otros inhibidores

<p>LEI105 is a potent, highly selective, and reversible inhibitor of DAGL-α and DAGL-β.</p>

<p>pppApG serves as an initial substrate for the synthesis of vRNA (viral RNA) and cRNA (complementary RNA), with applications in influenza virus research [1].</p>

<p>M04 acts as a stimulator of interferon genes (STING) agonist, effectively inducing IFN reporter gene expression in HEK293T cells equipped with wild-type human STING. Its activity is specific, not affecting HEK293T cells with the R71H-G230A-R293Q (HAQ) human STING variant or mouse RAW 264.7 cells, showcasing allelic- and species-dependent effects at a concentration of 75 µM. This compound also stimulates the production of TNF-α, IL-10, IL-1β, and IL-12p70 in human peripheral blood mononuclear cells (PBMCs). At 50 µM, M04 enhances human monocyte-derived dendritic cells' expression of HLA-DR (MHC class II receptor) and co-stimulatory molecules CD40, CD80, and CD86, improving T cell cross-priming in an ex vivo assay.</p>

<p>Docosahexaenoic acid alkyne, an ω-alkyne derivative of docosahexaenoic acid, enables Cu(I)-catalyzed cycloaddition with azide-containing molecules for efficient click chemistry applications. It can be further utilized to produce alkyne-modified products like glycerophospholipids. Additionally, this compound permits the monitoring of fatty acid metabolism in cells through click chemistry linkage to fluorophores.</p>

<p>A-320436 is an H3 receptor antagonist that may affect cognition.</p>

<p>Δ17-6-keto Prostaglandin F1α (Δ17-6-keto PGF1α), a cyclooxygenase (COX) metabolite produced from eicosapentaenoic acid (EPA) in a variety of tissues including seminal vesicles, lungs, polymorphonuclear leukocytes, and ocular tissues, alongside other 3-series COX products from EPA such as PGF3α, PGE3, and thromboxane B3, is potentially linked to a lower occurrence of glaucoma in individuals consuming a marine-rich (EPA-rich) diet.</p>

<p>CAY10455, an analog of arachidonoyl ethanolamide (anandamide; AEA), is non-fluorescent extracellularly but exhibits bright fluorescence at 530 nm inside cells due to esterase-mediated cleavage. Its uptake by C6 glioma cells is competitively inhibited by AEA and its analogs, suggesting that CAY10455 and AEA utilize the same transporter. Conversely, CAY10455 also inhibits the uptake of tritiated AEA, further indicating competition for the AEA transporter.</p>

<p>1-Palmitoyl-2-docosahexaenoyl-sn-glycero-3-PE, a phospholipid comprising palmitic acid (at the sn-1 position) and docosahexaenoic acid (at the sn-2 position), is present in the nucleus of mouse liver but absent from mitochondria. Notably, its levels in pre-term infant plasma are lower compared to those in maternal or fetal plasma.</p>

<p>1,3-Diarachidonoyl glycerol, a diacylglycerol with arachidonic acid at the sn-1 and sn-3 positions, exhibits cytotoxicity toward 3Y1 and E1A-3Y1 cells at concentrations of 8 to 16 µg/ml.</p>

<p>Angiogenesis Inhibitor 4 is a potent agent for inhibiting angiogenesis, with potential applications in cancer research [1].</p>

<p>Cis-indatraline hydrochloride (cis-Lu 19-005) is an active compound utilized in the research of neurodegenerative diseases [1].</p>

<p>1-Palmitoyl-3-linolenoyl-rac-glycerol, a diacylglycerol with palmitic acid and α-linolenic acid at the sn-1 and sn-3 positions respectively, is present in both the peel and pulp of unripe Dwarf Cavendish bananas.</p>

<p>PCSK9-IN-20 (Compound 3i) is a PCSK9 inhibitor exhibiting an IC50 value of 3.96 µM, shown to reduce PCSK9 and enhance LDLR protein levels in vitro [1].</p>

<p>ZH8659 is a Gq agonist targeting the trace amine-associated receptor 1 (TAAR1) and has potential applications in schizophrenia research [1].</p>

<p>PBD dimer-2 (compound 2c), a C8-linked pyrrolobenzodiazepine dimer, has the capability to span an extra base pair and cross-link the 5′-Pu-GA(T/A)TC-Py sequence. It serves as a potential payload for antibody–agent conjugates (ADCs) and is under research for cancer treatments [1] [2].</p>

<p>UNC3474, a small molecule ligand, selectively interacts with the aromatic methyl-lysine binding cage of the tumor protein 53BP1 Tudor domain (TT), exhibiting a</p>

<p>18-Carboxy dinor Leukotriene B4 (18-carboxy dinor LTB4) represents a β-oxidation metabolite of Leukotriene B4 (LTB4). Initially, LTB4 is metabolized in the liver to 20-carboxy LTB4, which subsequently undergoes β-oxidation to form 18-carboxy dinor LTB4.</p>

<p>3-Hydroxy Undecanoic Acid Methyl Ester, a hydroxylated fatty acid methyl ester, is present in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers synthesized by P. oleovorans, P. putida, and D. tsuruhatensis [Matreya, LLC. Catalog No. 1730].</p>

<p>Sterculic acid methyl ester, an ester derivative of sterculic acid known for inhibiting Δ9 desaturase, has been found to adversely affect and exhibit toxicity towards R. opacus bacteria at a concentration of 0.75 mM. It not only hampers bacterial growth but also modifies fatty acid composition by reducing stearate and oleate levels, increasing the palmitate ratio, and decreasing overall fatty acid content at 0.25 or 0.5 mM concentrations. Additionally, at 50 ppm, Sterculic acid methyl ester enhances the tumor growth-promoting effects of aflatoxin Q1 in rainbow trout, indicating a synergistic interaction between the two compounds. [Matreya, LLC. Catalog No. 1236]</p>

<p>(±)-N-desmethyl Venlafaxine, a minor active metabolite of venlafaxine, serves as a selective norepinephrine and serotonin reuptake inhibitor (SNRI). Generated through the metabolization by the cytochrome P450 (CYP) isoform CYP3A4, it exhibits reuptake inhibition of norepinephrine and serotonin in rat synaptosome preparations, demonstrated by IC50 values of 4.7 and 1.6 µM, respectively. Clinically, it has been shown to counteract reserpine-induced hypothermia in mice, displaying efficacy at a minimum effective dose (MED) of 10 mg/kg.</p>

<p>VU0155069 hydrochloride (CAY10593 hydrochloride) is a potent and selective inhibitor of phospholipase D (PLD), exhibiting IC50 values of 46 nM for PLD1 and 933 nM for PLD2. It effectively inhibits the migration of both human and mouse breast cancer cell lines [1] [2].</p>

<p>MOMBA is a selective orthosteric agonist specifically targeting engineered human free fatty acid 2 (hFFA2) receptors, particularly those modified as designer</p>

<p>Salbutamol (albuterol), a selective β2-adrenergic partial agonist, serves as a bronchodilator widely used in various clinical scenarios and to counteract doping abuse. Its process impurity, Albuterol methyl ether, may be present in urine samples, highlighting the importance of detection and chemical analysis.</p>

<p>5-Oxo Leukotriene B4 (5-oxo LTB4) serves as an intermediate metabolite in the production of 12-oxo LTB4.</p>

<p>F-amidine is a selective inhibitor of protein arginine deiminases (PADs), specifically targeting PAD1 and PAD4 with in vitro IC50 values of 29.5, 350, and 21.6 µM for PAD1, PAD3, and PAD4, respectively. It irreversibly inactivates all four PAD subtypes by covalently modifying an active site cysteine crucial for enzymatic activity, with kinact/KI values of 2,800, 380, 170, and 3,000 M^-1min^-1. Additionally, F-amidine demonstrates cytotoxicity against HL-60, MCF-7, and HT-29 cancer cell lines, with IC50s of 0.5, 0.5, and 1 μM, respectively.</p>

<p>(R)-Necrocide 1 (compound (R)-38) is a potent anticancer agent with antiproliferative activity [1].</p>

<p>H-(Gly)3-Lys(N3)-OH (hydrochloride) is a click chemistry reagent renowned for its high yield, specificity, and simplicity, making it an ideal choice for creating bindings among nucleic acids, lipids, proteins, and other molecules across various research domains.</p>

<p>WAY-232897 is an active compound utilized in the investigation of amyloid diseases and synucleinopathies.</p>

<p>Prohexadione calcium (BX-112) is a plant growth regulator that inhibits gibberellin biosynthesis in plants [1] [2].</p>

<p>Tegolimod fumarate is an immunomodulator [1].</p>

<p>Alpertine HCl is a small molecule compound with anti-neuropathic properties.</p>

<p>PI5P4Kα-IN-1 (Compound 13) is a phosphatidylinositol 5-phosphate 4-kinase (PI5P4K) inhibitor, displaying IC50 values of 2 μM for PI5P4Kα and 9.4 μM for PI5P4Kβ</p>

<p>PBR28, a TSPO modulator, holds potential for preventative research in Pulmonary Arterial Hypertension (PAH) and is instrumental in brain positron emission</p>

<p>Dimethylamiloride is a specific inhibitor of antiporters [1].</p>

<p>1,2-Dioleoyl-3-lauroyl-rac-glycerol-13C3 is designed as an internal standard for the quantification of 1,2-dioleoyl-3-lauroyl-rac-glycerol, employable with GC- or LC-MS techniques. This compound is a type of triacylglycerol featuring oleic acid at the sn-1 and sn-2 positions, and lauric acid at the sn-3 position, and has been identified in date seed oil and the fat body of male B. lapidarius bumblebees.</p>

<p>XLR11, a synthetic cannabinoid (CB) featuring a tetramethylcyclopropyl group, exhibits enhanced affinity for the CB2 receptor, common among synthetic CBs for its receptor affinity. XLR11 degradant, a frequent impurity identified in GC-MS analysis of XLR11-containing samples, originates from the thermal decomposition of XLR11, leading to an opened ring structure. This change results in a distinct fragment ion in mass spectrometry, being 15 amu heavier than XLR11's base peak. Such a signature is indicative of a McLafferty rearrangement in the degradant, a reaction not observed in the parent compound.</p>

<p>2-(((Benzo[d][1,3]dioxol-5-ylmethylene)amino)oxy)-N-(m-tolyl)acetamide represents a bioactive chemical entity.</p>

<p>Oleoyl-L-alpha-lysophosphatidic acid sodium salt is an essential cell membrane biosynthetic metabolite that mediates signal transduction by interacting with G</p>

<p>ICMT-IN-19 (compound 53) serves as a potent inhibitor of ICMT, demonstrating an IC50 value of 0.026 μM [1].</p>

<p>2-O-Ethyl PAF C-16, a homolog of Platelet-activating Factor (PAF) and competitive ligand for the Platelet-activating Factor Receptor (PAFR), inhibits the binding of PAF antagonist WEB 2086 to PAFR with an IC50 of 21 nM [1].</p>

<p>ICMT-IN-53 (compound 12) is an ICMT inhibitor exhibiting an IC50 of 0.96 μM, alongside favorable PAMPA permeability and antiproliferative properties.</p>

<p>17β-Hydroxywortmannin is an orally active phosphatidylinositol-3-kinase (PI-3-kinase) inhibitor, exhibiting an IC50 of 0.5 nM and notably suppresses osteoclast resorption at an IC50 of 10 nM. Additionally, it demonstrates antitumor activity.</p>

<p>N-didesmethyl Loperamide, an active metabolite of the peripheral μ1-opioid receptor agonist loperamide, impedes electrically induced contractions in isolated</p>

<p>Prostaglandin K2 (PGK2), a 9,11-diketone derivative, results from PGE2 or PGD2 oxidation. Its biological presence remains speculative; however, it demonstrates resistance to in vitro metabolism by 15-hydroxy PGDH.</p>

<p>TLR7 agonist 15 (compound 16b) is a potent activator of mouse macrophages and hPBMCs, demonstrating an EC50 of 18 nM.</p>

<p>PTC258 is a specific, orally active modulator of the splicing of the Elongator complex protein 1 gene (ELP1), enhancing its expression both in vitro and in vivo</p>

<p>Aspartyllysine, a hydrophilic dipeptide in wheat and fish, is excreted by kidneys via H+/peptide transport.</p>

<p>FTI-2600 is a farnesyltransferase inhibitor.</p>

<p>2,3-Dinor-8-iso Prostaglandin F1α (2,3-dinor-8-iso PGF1α), an isoprostane and active metabolite of arachidonic acid deriving its formation from non-enzymatic</p>

<p>SIM010603, an oral RTK inhibitor, targets Kit, VEGFR-2, PDGFR-β, RET, FLT3 (IC50: 5.0-68.1 nmol/l), inhibits cell proliferation and angiogenesis.</p>

<p>p-SCN-Bn-HOPO: superior (89)Zr ImmunoPET chelator, low background, high tumor contrast, minimal bone uptake in BT474 breast cancer scans.</p>

<p>Plecstatin-1, an organoruthenium compound, serves as a potent anti-cancer agent that selectively targets plectin—a scaffold protein and cytolinker—within tumor</p>

<p>1,3-Dielaidoyl-2-oleoyl glycerol is a triacylglycerol consisting of elaidic acid at the sn-1 and sn-3 positions and oleic acid at the sn-2 position.</p>

<p>BIM 23056 TFA, a potent linear octapeptide antagonist of sst3 and sst5 somatostatin receptors, exhibits inhibition constants (K_i) of 10.8 for sst3 and 5.7 for</p>

<p>L-739943 is a growth hormone secretagogue.</p>

<p>DG046 is a potent ERAP1 inhibitor, a phosphinic pseudopeptide with unique π-stacking stabilization in the active site.</p>

<p>Linoleoyl ethanolamide phosphate is an intermediate in the biosynthesis of linoleoyl ethanolamide, generated through phospholipase C-mediated hydrolysis of N-acylphosphatidylethanolamine. Linoleoyl ethanolamide phosphate, along with other endogenous N-acylethanolamines, is thought to regulate food intake by selectively prolonging feeding latency and post-meal interval [Linoleoyl Ethanolamide Phosphate].</p>

<p>GNN14490, a substrate for human pancreatic lipase, is utilized to create monomolecular films for enzyme assay studies.</p>

<p>AMD-3329 is a potent anti-HIV agent that blocks virus replication by targeting CXCR4, a key receptor for X4 viruses' entry.</p>

JNJ-10258859 is a potent, and selective phosphodiesterase type 5 inhibitor with a K(i) of 0.23 nM.

<p>Wee1 Inhibitor I is an ATP-binding site-targeting Wee1 inhibitor.</p>

<p>Plomestane is a selective inhibitor of aromatization in human breast tissue and may provide a mechanism for controlling estrogen responsive processes.</p>

<p>PAT1inh-B01, a selective SLC26A6 inhibitor, impedes PAT1 (a Cl-/HCO3- exchanger) activity, with an IC50 of 350 nM, effectively inhibiting anion exchange.</p>

<p>HV-723 fumarate is an alpha-1 adrenoceptor antagonist.</p>

<p>Ro 10-4548 is a bioactive chemical.</p>

<p>5α-Pregnane-3α,20α-diol, an active metabolite of progesterone, is synthesized through intermediates 5α-pregnane-20α-ol-3-one and 5α-pregnane-3α-ol-20-one from</p>

<p>WAY-313318 is an active compound.</p>

<p>Ent-Entecavir, an enantiomeric impurity of Entecavir (an oral HBV drug), inhibits HBV replication as a reverse transcriptase inhibitor.</p>

<p>4-(3,4-Difluorobenzo)curcumin (CDF) is a semisynthetic coumarin noted for its antiparasitic and anticancer properties.</p>

<p>FK-143 is a 5-alpha reductase inhibitor.</p>

<p>Acetylaleuritolic acid, a pentacyclic triterpenoid from Garcinia miniata leaves, inhibits P-388 leukemia.</p>

<p>RR-RJW100: potent LRH-1 &amp; SF-1 agonist; studies metabolic disorders, diabetes, liver disease, IBD.</p>

<p>1-Myristoyl-2-lauroyl-rac-glycerol is a diacylglycerol featuring myristic acid at the sn-1 position and lauric acid at the sn-2 position.</p>

<p>8,12-iso-iPF2α-VI, an isoprostane, arises from non-enzymatic, free radical-induced peroxidation of membrane lipids. It is the predominant isoprostane formed during lipid peroxidation and serves as a biomarker for oxidative stress. Detectable in hepatic tissue post CCl4-induced oxidative damage, 8,12-iso-iPF2α-VI levels are also elevated in the urine, blood, and cerebrospinal fluid of Alzheimer's disease patients.</p>

<p>WAY-659873 is an active molecule.</p>

<p>TrkA-IN-4, a potent, orally active and allosteric TrkA inhibitor, is a prodrug of TrkA-IN-3 . TrkA-IN-4 exhibits potent antinociceptive effects [1] .</p>

<p>STING agonist-10 is a potent activator of the STING small molecule cyclic urea class (EC50: 2600 nM).STING activation is a highly promising immunotherapy.</p>

<p>RO4583298 is a highly potent dual NK1/NK3 receptor antagonist with in vivo activity.</p>

<p>Sulfonterol is a Bronchodilator.</p>

<p>Oxicodegol HCl is a mu-opioid agonist used in the treatment of Moderate to Severe Chronic Low Back Pain</p>

<p>13,14-Dihydro-19(R)-hydroxy Prostaglandin E1 (13,14-dihydro-19(R)-hydroxy PGE1) is posited as a theoretical metabolite resulting from the action of ω-1 hydroxylase on 13,14-dihydro PGE1. Its biosynthesis and biological activity remain unreported in scientific literature.</p>

<p>CK 3197 is a selective positive inotropic agent for the treatment of congestive heart failure. It has hemodynamic and myocardial energetic effects.</p>

<p>Mivazerol hydrochloride is an alpha 2-adrenoceptor agonist.</p>

<p>NT113: ERBB inhibitor, penetrates brain, hinders GBM growth (high EGFR/EGFRvIII), targets ERBB/Akt phosphorylation in vivo/in vitro.</p>

<p>Perfluorodecanesulfonic Acid (PFDS) is a perfluoroalkyl substance that can be found in S. namaycush.</p>

<p>Prezatide copper (also known as Bisprezatide copper or Iamin) serves as an inhibitor of hair loss and is recognized for its multiple wound-healing properties as</p>

<p>1-Myristoyl-3-oleoyl-rac-glycerol is a diacylglycerol featuring myristic acid (at the sn-1 position) and oleic acid (at the sn-3 position).</p>

<p>ZL0513: orally active, BRD4 BD1 inhibitor with strong in vivo results and good pharmacokinetics for treating inflammation.</p>

<p>Activated A Subunit is instrumental in synthesizing exon skipping oligomer conjugates, which are designed to specifically pair with chosen sequences within the</p>

<p>MNG-14a, an amphiphilic compound, facilitates the isolation and determination of both function and structure of membrane proteins [1].</p>

<p>7-Hydroxy Etodolac, an inactive metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor etodolac, serves no active function in the drug's pharmacological effects.</p>

<p>METTL3-IN-5 (Compound 13) serves as an inhibitor of METTL3 and demonstrates efficacy in suppressing MOLM-13 cell growth with an IC50 of less than 2 μM.</p>

<p>Zaldaride (free base) is a calmodulin antagonist.</p>

<p>VRT-534 is a compound that selectively targets connexin 26 (Cx26), demonstrating dose-responsive binding to both wild-type (WT) Cx26 and the mutant Cx26 K188N,</p>

<p>FPL-65447 HCl is a D1 agonist for renal/cardiac failures and sepsis treatment.</p>

<p>Latanoprost, the isopropyl ester of 17-phenyl-13,14-dihydro prostaglandin F2α, serves as a prodrug for the free acid form, a potent FP receptor agonist in the eye. Isopropyl 5-(diphenylphosphoryl)pentanoate may exist as a potential trace impurity in commercial latanoprost preparations.</p>

<p>Meclizine N-oxide, a metabolite of the histamine H1 receptor antagonist meclizine (1), also acts as a degradation product and potential impurity in commercial meclizine preparations (2).</p>

<p>Oxycodegol phosphate is a mu-opioid agonist used in the treatment of Moderate to Severe Chronic Low Back Pain</p>

<p>Bt-sch is an imaging agent based on D1 and D2 receptors of dopamine.</p>

<p>JWH 020, a cannabimimetic indole derivative of WIN 55,212-1, exhibits notably weaker affinities for the cannabinoid receptors CB1 and CB2 (128 and 205 nM, respectively) compared to WIN 55,212-2 (1.89 and 0.28 nM, respectively). The in vivo effects of JWH 020 have not been studied. This compound is designed for forensic and research purposes.</p>

<p>BR103354: potent FAP inhibitor, IC50 of 14 nM, oral bioavailability 48.4%, minimal hERG risk, potential anti-diabetic and anti-NASH agent.</p>

<p>Porcn-IN-2 (Example 107) is a potent Wnt pathway inhibitor, exhibiting an IC50 of 0.05 nM.</p>

<p>XM 323 is an inhibitor of clinical isolates of HIV-1 in vitro and represents a novel class of non-peptidyl inhibitors of HIV-1 protease.</p>

<p>PD 121373, a Benzothiopyrano-indazole, inhibits nucleic acid synthesis, equally affecting DNA/RNA.</p>

<p>PGF1β, a biochemical compound, functions as a pivotal mediator in inflammatory processes and plays an integral role in uterine contractions. It exhibits significant regulatory effects on platelet aggregation and vasodilation, demonstrating its critical importance in cardiovascular health. Additionally, PGF1β contributes to the regulation of kidney function and electrolyte balance, illustrating its widespread impact across various physiological systems.</p>