Otros inhibidores

<p>MiTMAB, a selective dynamin inhibitor, targets the interaction between dynamin and phospholipids.</p>

<p>Compound A, a potent TLR8 agonist, exhibits an EC50 of 0.052 µM and promotes the production of IL-12p40 in human PBMCs with an EC50 of 0.031 µM.</p>

<p>GW-475151 inhibits human neutrophil elastase (HNE).</p>

<p>C.I. Vat Black 27 is a black dye.</p>

<p>12(Z),15(Z)-Heneicosadienoic acid, an ω-6 very long-chain polyunsaturated fatty acid, serves as a positional isomer of heneicosadienoic acid, which is scarcely found in living organisms.</p>

<p>Elisidepsin (PM02734), a cyclic depsipeptide, exhibits antineoplastic activity by inhibiting cancer cell proliferation and is under research for the treatment</p>

<p>WAY-325485 is an active molecule.</p>

<p>1,2,3-Tritridecanoyl glycerol, a synthetic triacylglycerol featuring tridecanoic acid at the sn-1, sn-2, and sn-3 positions, serves as a standard for relative triacylglycerols quantification in C. elegans fat stores and as an internal standard in quantifying triacylglycerols in serum and liver of adult rat offspring exposed to dietary conjugated linoleic acids during and post-gestation.</p>

<p>NAS-181 free base is a 5-HT(1B) receptor antagonist.</p>

<p>TIE-2/VEGFR-2 kinase-IN-4, a benzimidazole derivative, serves as a potent inhibitor of the tyrosine kinase receptors TIE-2 and VEGFR-2, exhibiting inhibitory</p>

<p>SAS-0132 is a modulator/antagonist of sigma2R/TMEM97 and has potential for treating TBIs, Alzheimer's disease, and neuropathic pain.</p>

<p>Arachidonoyl chloride, a derivative of arachidonic acid, serves as an intermediate in synthesizing arachidonic acid derivatives.</p>

<p>D-threo-PDMP inhibits glucoceramide synthase, cutting cell surface glycosphingolipids and hindering neurite growth.</p>

<p>Compound 2 (MRV03-068) is a selective colibactin-activated peptidase (ClbP) inhibitor, preventing the genotoxic effects of colibactin on eukaryotic cells, with</p>

<p>NPBA, a potassium K2P channel TASK-3 (KCNK9) agonist, concurrently functions as a blocker of the tandem pore domain weak inward rectifying K+ channel (TWIK2). This compound effectively inhibits NLRP3 inflammasome activation in macrophages [1].</p>

<p>Crisdesalazine (AAD 2004) is an inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1).</p>

<p>XY-4, a derivative of 1-palmitoyl lysophosphatidic acid (1-palmitoyl LPA094) and an agonist of peroxisome proliferator-activated receptor γ (PPARγ), effectively</p>

<p>TRC160334 is a HIF hydroxylases inhibitor.</p>

<p>Ubiquitination-IN-1 is an inhibitor of ubiquitination and Cksl-Skp2 protein-protein interaction (IC50: 0.17 μM).</p>

<p>15-Hydroxy Pentadecanoic Acid Methyl Ester is a hydroxylated fatty acid methyl ester (FAME) crucial for synthesizing musk-odored macrocyclic lactones, specifically cyclopentadecanolide and exaltolide [Matreya, LLC. Catalog No. 1882].</p>

<p>CAY10502 inhibits cPLA2α (85 kDa), crucial in inflammation/arachidonic cascade, with 4.3 nM IC50, reducing arachidonic acid in human platelets.</p>

<p>SARS-CoV-2 3CLpro-IN-10(5d) inhibits 3CL protease: 190 nM (SARS-CoV-2), 790 nM (SARS-CoV-1), 70 nM (MERS-CoV), and has broad-spectrum antiviral effects.</p>

<p>1-Tridecanoyl-rac-glycerol, a monoacylglycerol featuring tridecanoic acid at the sn-1 position, serves as an internal standard for quantifying mono- and diacylglycerols in buttermilk.</p>

<p>ICMT-IN-36 (compound 40) serves as an ICMT inhibitor, with an IC50 value of 0.181 μM [1].</p>

<p>Estrone 3-methyl ether is an active molecule that can be used in life science related research. The CAS number of Estrone 3-methyl ether is 1624-62-0.</p>

<p>WAY-328127 is an active molecule, exhibiting an inhibitory effect on the (11β-hydroxysteroid dehydrogenase type 1) [(11β-HSD1)] enzyme.</p>

<p>HBY-793 is an HIV-1 proteinase inhibitor.</p>

<p>Prothipendyl hydrochloride serves as an orally active compound for researching mental symptoms in the elderly, such as anxiety [1].</p>

<p>Antitumor agent-29 is a hepatocyte-targeting prodrug with demonstrated efficacy and minimal toxicity in anticancer applications.</p>

<p>1,3-Dinervonoyl glycerol, a diacylglycerol, features nervonic acid at the sn-1 and sn-3 positions.</p>

<p>AMG-7549 is a disrupter of Glucokinase−Glucokinase Regulatory Protein (GK−GKRP) binding.</p>

<p>APO-6619 is an iron chelator inhibiting growth of multiple bacteria, potentially treating infections.</p>

<p>Sphingosine (d18:1), an amino alcohol, is chiefly recognized for its 18-carbon unsaturated hydrocarbon chain. Nevertheless, in mammalian tissues, both sphingosine and its variant, dihydrosphingosine, feature hydrocarbon chains ranging from 12 to 26 carbons. Sphingosine (d15:1) represents a naturally rare variant, serving as an internal standard for chromatographic or spectrometric analyses of sphingoid compounds.</p>

<p>Azidoacetic Acid (2-Azidoacetic acid) (compound 92-1), a click chemistry reagent featuring an azide group, serves as a versatile small molecule tool in the synthesis of PROTAC [1].</p>

<p>JTT 130 is an agent of hypolipidemic. It inhibits microsomal triglyceride transfer protein.</p>

<p>Durlobactam is a drug candidate for beta-lactamase inhibitor.</p>

<p>Thioacetanilide (NSC-36984) possesses potential anti-inflammatory and analgesic activities.</p>

<p>Palmitoleoyl 3-carbacyclic phosphatidic acid (3ccPA 16:1) serves as a moderately effective autotaxin (ATX) inhibitor, exhibiting an IC50 value of 620 nM. This compound finds utility in melanoma research[1].</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>17-Phenyl trinor Prostaglandin F2αdiethyl amide (17-phenyl trinor PGF2αdiethyl amide) is a Prostaglandin F2α(PGF2α) analog characterized by the substitution of the C-1 carboxyl group with an N-diethyl amide. Prostaglandin (PG) esters and N-ethyl amides have demonstrated ocular hypotensive properties, with N-ethyl amides introduced as alternative options for PG hypotensive prodrugs. Studies indicate that both bovine and human corneal tissues can convert N-ethyl amides of various PGs into their free acid forms at a rate of approximately 2.5 µg/g corneal tissue/hr. However, dialkyl amides like 17-phenyl trinor PGF2αdiethyl amide resist conversion by corneal amidase, showing no detectable transformation into free acids. This characteristic suggests their potential as valuable investigative tools for assessing the intrinsic intraocular hypotensive activities of PG amides.</p>

<p>Etidocaine Hydrochloride (W19053) is a long-acting anesthetic and a blocker of the voltage-gated sodium channel.</p>

<p>Mdl 27013 is a derivative of methoxysuccinyl-alanyl-alanyl-prolyl-valine.</p>

<p>ICMT-IN-41 (compound 20) serves as a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), demonstrating an IC50 value of 0.069 μM [1].</p>

<p>YKL-5-124 TFA is a potent, selective, irreversible and covalent inhibitor of CDK7 (IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively).</p>

<p>Sunepitron Free Base, a 5-HT1A agonist/α₂-antagonist, halted in Phase III for depression/anxiety.</p>

<p>C10 Ceramide (d18:1/10:0) is a lipid molecule that can be used in life science related research. The CAS number of C10 Ceramide (d18:1/10:0) is 111122-57-7.</p>

<p>Kv3 modulator 4 is a Kv3.1 (pEC50=5.45) and Kv3.2 modulator .Cyclobutyl structure.</p>

<p>JWH 368 is a (1-naphthoyl)pyrrole cannabinoid (CB) known for its potent activation of central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors, with Ki values of 16 and 9.1 nM, respectively. Its physiological, neurological, and toxicological properties have yet to be evaluated, indicating that this compound is strictly intended for forensic and research applications.</p>

<p>Riboxin (IDP), an orally administered purine derivative known as hypoxanthine riboside, exhibits antihypoxic and antihyperthermic effects.</p>

<p>CGP 55845: potent, selective GABAB blocker, IC50=5 nM, hinders agonist binding, reduces GABA/glutamate release.</p>

<p>1,2-Distearoyl-3-butyryl-rac-glycerol is a triacylglycerol characterized by the presence of stearic acid at the (sn-1) and (sn-2) positions and butyric acid at the (sn-3) position, notably identified within butterfat.</p>

<p>1-Aminodecylidenebis-phosphonic acid, with its potent inhibitory effect on acid sphingomyelinase (IC50= 20 nM), shows selectivity by being less effective against neutral sphingomyelinase (IC50= &gt;100 μM). Additionally, it entirely prevents dexamethasone-induced apoptosis in HepG2 cells.</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>Prostaglandin F2αethyl amide (PGF2α-NEt), a PGF2α analog featuring an N-ethyl amide modification at the C-1 carboxyl group, possesses ocular hypotensive activity similar to PG esters. Introduced as alternative prostaglandin ocular hypotensive prodrugs, PGF2α-NEt and other PG N-ethyl amides, contrary to claims of not converting to free acids in vivo, have been demonstrated by our laboratory studies to undergo conversion by bovine and human corneal tissue into the respective free acids at a rate of approximately 2.5 µg/g corneal tissue/hr. This suggests PGF2α-NEt is expected to elicit typical PGF2α free acid intraocular effects, albeit with slower hydrolysis kinetics characteristic of PG N-amides.</p>

<p>All-cis-4,7,10,13,16-Docosapentaenoic acid ethyl ester (all-cis-4,7,10,13,16-DPA ethyl ester) is a derivative of docosapentaenoic acid (DPA), an omega-3 fatty acid prevalent in fish oils. This ethyl ester form is commonly included in dietary supplements formulations to enhance omega-3 fatty acid intake.</p>

<p>19(R)-hydroxy Prostaglandin E2 (19(R)-hydroxy PGE2), present in the semen of primates, including humans, acts as a potent smooth muscle relaxant and is a selective agonist for the EP2 receptor. It exhibits an EC50 value of 200 nM for relaxing cat tracheal rings that express EP2 receptors.</p>

<p>HCT-116-IN-1, a γ-lactam-fused pyridone derivative, exhibits anticancer properties, demonstrating significant cytotoxicity towards HCT116 cells, with an IC50</p>

<p>8(S)-HETE activates mouse keratinocyte PKC (IC50: 100 μM) and PPARα (&gt;0.3 μM); identified by chiral HPLC in murine skin.</p>

<p>THB is a glucocorticoid with anti-inflammatory effects, acting on GC receptors; its isomers vary between male and female rat brains.</p>

<p>N-Nitrosomethylisopropylamine, a type of N-nitrosamine, has been shown to induce tumor formation in mice.</p>

<p>Fluocortin butyl ester is a topical corticosteroid without systemic effects, effective in treating perennial rhinitis.</p>

<p>WAY-221060-A is an active molecule.</p>

<p>1,2-Dioleoyl-3-lauroyl-rac-glycerol, a triacylglycerol, comprises oleic acid at the sn-1 and sn-2 positions and lauric acid at the sn-3 position. It is identified in the date seed oil and the fat body of male B. lapidarius bumblebees.</p>

<p>Temelimab (GNbAC-1) is a monoclonal antibody targeting endogenous retroviruses in humans, used for studying multiple sclerosis (MS) and type 1 diabetes (T1D).</p>

<p>1,3-Dipalmitoyl-2-docosahexaenoyl glycerol, a triacylglycerol, features palmitic acid at the sn-1 and sn-3 positions and docosahexaenoic acid at the sn-2 position. Its dietary administration (30 g/kg) has been shown to decrease hepatic triglyceride and cholesterol levels in mice.</p>

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

<p>MOTS-c is a mitochondria-derived polypeptide (MDP) that has anti-damage and anti-inflammatory effects by activating the AMPK pathway and inhibiting the MAP</p>

<p>L-690488 has more effective cell penetration than L-690330. L-690488 is a prodrug of L-690330 and is a selective inositol monophosphatase (IMPase) inhibitor.</p>

<p>Example 2 (RXFP1 receptor agonist-8) is a potent RXFP1 receptor agonist that suppresses cAMP production in HEK293 cells expressing human RXFP1, exhibiting an</p>

<p>6-Hydroxy Bexarotene, an oxidative metabolite of bexarotene, serves as a high-affinity ligand for retinoid X receptors (RXRs), specifically binding to RXRα, RXRβ, and RXRγ, as well as to the retinoic acid receptor α (RARα) with dissociation constants (Kds) of 3.46, 4.21, 4.83, and 8.17 μM, respectively. It demonstrates selective activation of RXRα, RXRβ, and RXRγ over RARα, RARβ, and RARγ in vitro, with half-maximal effective concentrations (EC50s) of 398, 356, 420, 4,414, 2,121, and 2,043 nM, respectively.</p>

<p>PARP-2-IN-1 is a potent and selective inhibitor of PARP-2(IC50 of 11.5 nM).</p>

<p>Indimilast blocks PDE4, reducing lung inflammation and bronchiectasis, possibly treating COPD.</p>

<p>WAY-323756 is a research-active molecule utilized in the study of amyloid diseases and synucleinopathies.</p>

<p>SW106 blocks PTHR1 cAMP signaling, not affecting mutant PTHR1-T410P/H223R.</p>

<p>ONO-AE3-208 is an EP4 receptor antagonist with a Ki of 1.3 nM, exhibiting less potent activity against EP3, FP, and TP receptors (Ki values of 30, 790, and 2,400 nM, respectively), while showing no effect on other prostanoid receptors. In wild type mice, treatment with ONO-AE3-208, in conjunction with 3% dextran sodium sulfate, results in severe colitis characterized by epithelial loss, crypt damage, and inflammation, thereby mimicking the effects of EP4 deletion. Further, this compound has been utilized to investigate the role of EP4 signaling in various biological contexts, including immune and autoimmune responses, inflammation, and cancer.</p>

<p>ADL 08-0011, a μ-opioid antagonist with Ki 0.25 nM, is derived from alvimopan by gut microbes and counteracts loperamide effects in rats.</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>ICMT-IN-16 (compound 33) functions as an inhibitor of ICMT, demonstrating inhibitory concentration 50% (IC50) efficacy at 0.131 μM [1].</p>

<p>SB1-F-78 is an USP30 inhibitor.</p>

<p>Sialyllacto-N-tetraose b, a sialylated oligosaccharide, naturally occurs in mammalian milk [1].</p>

<p>H-Gly-Pro-Hyp-OH, a peptide dipeptidyl peptidase 4 (DPP-4) inhibitor with an inhibition concentration (IC50) of 2.51 mM, effectively hinders the activity of the DPP-4 enzyme.</p>

<p>SUCNR1-IN-2 (Statement 35) serves as an inhibitor of both succinate and succinate receptor 1, utilized in research pertaining to neurodegenerative disorders,</p>

<p>L 363851 is a neurokinin B agonist.</p>

<p>B-Raf IN 5 is a potent inhibitor of the protein kinase B-Raf (IC50: 2.0 nM). B-Raf IN 5 resists rapid metabolism and does not bind to the secondary target PXR.</p>

<p>D-Carnitine, an orally available isomer of the essential nutrient L-carnitine, facilitates the transport of long-chain fatty acids into the mitochondrial matrix for beta-oxidation. Additionally, D-Carnitine exhibits antiparasitic activity [1] [2] [3].</p>

<p>Tolterodine Dimer is a derivative of Tolterodine -- a muscarinic receptor antagonist that is used to treat patients with overactive bladder.</p>

<p>DGKζ-IN-1 (compound 9) is a DGKζ inhibitor with potential applications in cancer research, particularly for studying immunocyte activation and resistance to</p>

<p>Brevicompanine B: fungal metabolite, regulates plant growth/circadian rhythm, inhibits Arabidopsis roots, affects gene transcription, anti-P. falciparum.</p>

<p>1,3-Dieicosenoyl glycerol is a diacylglycerol featuring 11(Z)-eicosenoic acid at both the sn-1 and sn-3 positions.</p>

<p>1-Stearoyl-2-eicosapentaenoyl-sn-glycero-3-PC is a phospholipid comprising stearic acid and eicosapentaenoic acid at the sn-1 and sn-2 positions, respectively, identified in human red blood cells (RBCs).</p>

<p>C6 urea ceramide blocks neutral ceramidase, boosts ceramide levels, halts HT-29 cancer cell growth, and shrinks HT-29 tumors in mice when dosed.</p>

<p>Neurodegenerative Disorder-Targeting Compound 1 is an inhibitor of calpain [1].</p>

<p>DI-1859: selective, potent DCN1 covalent inhibitor, blocks cullin 3 neddylation, raises NRF2 in mice, prevents acetaminophen liver damage.</p>

<p>Glycine, N-[(1,1-dimethylethoxy)carbonyl]thio-L-phenylalanyl-, methyl ester (compound 3b) is a sulfamide-containing polypeptide that can be utilized in the</p>

<p>BMS-496 is a dual DGKα/ζ lipid kinase inhibitor exhibiting IC50 values of 0.09 μM (DGKα) and 0.006 μM (DGKζ) [1].</p>

<p>CRM-51005 is a new phospholipase C inhibitor produced by unidentified fungal strain MT51005</p>

<p>3'-Ethoxy spinosyn L, a minor component in the insecticide spinetoram, is utilized in certain formulations for its insecticidal properties. Marketed solely for research and analytical purposes, it is designed for controlled laboratory use with no option for bulk purchase.</p>

<p>AKR1C3-IN-6: Strong AKR1C3 inhibitor (IC50: 0.31 μM); weak on AKR1C2 (IC50: 73.23 μM); shows antitumor effects.</p>

<p>MNI-caged-L-glutamate, a derivative of glutamate conjugated with a 4-methoxy-7-nitroindolinyl (MNI) photoprotective group, remains pharmacologically inactive at neuronal glutamate receptors at concentrations up to mM. Upon light exposure (300 - 380 nm excitation), it rapidly releases L-glutamate by cleaving the MNI group within submicroseconds. This characteristic enables the investigation of fast synaptic glutamate receptor mechanisms in situ.</p>

<p>Dihydroquinoline-pyrazoline DQP-997-74 (compound 2i) is a selective N-methyl-d-aspartate receptor (NMDAR) inhibitor that preferentially targets GluN2C/D</p>

<p>AtPCO4-IN-1 is a selective AtPCO4 inhibitor, exhibiting an IC50 value of 264.4 μM [1].</p>

<p>Dual photoCORM 1 (compound 5), a metal-free, photoactive, dual carbon monoxide releasing molecule (CORM), demonstrates efficient cellular uptake and enables</p>

<p>1,2-Diheptadecanoyl-rac-glycerol is a diacylglycerol featuring heptadecanoic acid at both the sn-1 and sn-2 positions.</p>

<p>Ciprostene, a stable prostacyclin analog, lowers blood pressure, increases heart rate, and inhibits platelets; tested in vascular disease patients.</p>