Outros inibidores

<p>β-Catenin-IN-6 is an inhibitor of the canonical Wnt/β-catenin signaling pathway, effectively impeding the proliferation of human colorectal cancer cells and</p>

<p>OSBP-IN-1 (compound 12), an analogue of Schweinfurthins, selectively targets oxysterol-binding protein (OSBP) and exhibits antitumor activity [1].</p>

<p>MDL-74156 is an active metabolite of dolasetron and a 5-hydroxy-tryptamine3 (5-HT3) antagonist.</p>

<p>1-Lauroyl-2-stearoyl-rac-glycerol, a diacylglycerol, harbors lauric acid and stearic acid at the sn-1 and sn-2 positions, respectively.</p>

<p>9-Keto Fluprostenol Isopropyl Ester, an ester derivative of the FP receptor agonist fluprostenol, undergoes oxidation at carbon 9. This compound serves as a potential prodrug for 9-keto fluprostenol, which may function as an agonist at EP receptors. Additionally, it is considered a possible metabolite of fluprostenol isopropyl ester (travoprost), drawing parallels to the metabolism of latanoprost by 15-hydroxyprostaglandin dehydrogenase observed in monkey cornea. Furthermore, certain F-series prostaglandins, such as 6-keto prostaglandin F1α (PGF1α), undergo conversion to their E-series counterparts in isolated human platelets, highlighting a metabolic pathway of relevance.</p>

<p>L-054,522 is potent, selective agonists of somatostatin receptor.</p>

<p>UK 55444 is a potent calcium antagonist.</p>

<p>PAK1-IN-1: PAK1 inhibitor, IC50 9.8 nM, hinders tumor cell migration and invasion dose-dependently.</p>

<p>Faropenem sodium hemipentahydrate is an orally administered beta-lactam antibiotic within the penem group, exhibiting resistance to certain types of extended-spectrum beta-lactamase (beta-lactamase).</p>

<p>8(R),11(S)-DiHODE, a fungal oxylipin identified in various Aspergillus species, is synthesized through the isomerization of an 8(R)-HpODE intermediate during linoleic acid oxidation.</p>

<p>(Rac)-Neurodegenerative Disorder-Targeting Compound 1 is a calpain inhibitor.</p>

<p>Embramine hydrochloride is a monoethanolamine derivative utilized for its antihistaminic and anticholinergic properties [1].</p>

<p>WAY-660222 is an active molecule.</p>

<p>(S)-Ro 32-0432 is a potent, selective inhibitor of protein kinase C (PKC) and G protein-coupled receptor kinase 5 (GRK5), demonstrating ATP-competitive and oral activity. It presents IC50 values of 9.3 nM for PKCα, 28 nM for PKCβI, 30 nM for PKCβII, 36.5 nM for PKCγ, and 108.3 nM for PKCε, showcasing its effectiveness against multiple PKC isoforms. Additionally, (S)-Ro 32-0432 inhibits T-cell activation, indicating its potential application in the research of chronic inflammatory and autoimmune diseases [1] [2].</p>

<p>AGN 193109 is a potent antagonist of retinoic acid receptors (RARs; Kd= 2, 2, and 3 nM for RARα, β, and γ, respectively), exhibiting selectivity for RARs over retinoid X receptors (RXRs; Kd= &gt;10,000 nM for human RXRα, β, and γ receptors). This compound effectively reverses cellular morphology changes and growth suppression induced by RAR agonists such as all-trans-RA, 13-cis-RA, and 9-cis-RA in ECE16-1 human endometrial ectocervical epithelial cells, particularly when used at a 10-fold molar excess. Furthermore, AGN 193109 downregulates the expression of cytokeratin K5-8, 13, 14, 16, 17, and 19 genes, indicating inhibition of retinoid action, specifically when co-administered with TTNPB but not as a standalone treatment. In vivo studies demonstrate teratogenic effects, including cleft palate, frontonasal dysplasia, and eye malformations in mouse fetuses following a single oral dose of 1 mg/kg.</p>

<p>1-Palmitoyl-2-elaidoyl-3-linoleoyl-rac-glycerol is a triacylglycerol composed of palmitic acid (at the sn-1 position), elaidic acid (at the sn-2 position), and linoleic acid (at the sn-3 position) respectively.</p>

<p>L-869298 is a potent and selective inhibitor of PDE4.</p>

<p>Rohitukine: anticancer, modulates apoptosis, antiadipogenic, antidyslipidemic, gastroprotective, antifertility, antileishmanial.</p>

<p>DBCO-PEG4-GGFG-Dxd is a conjugate used in antibody-drug conjugates (ADCs) exhibiting potent antitumor activity. It incorporates Dxd, a DNA topoisomerase I inhibitor, connected through the cleavable linker DBCO-PEG4-GGFG [1]. This compound functions as a click chemistry reagent, featuring a DBCO group capable of strain-promoted alkyne-azide cycloaddition (SPAAC) with azide-containing molecules.</p>

<p>SB1578/ONX-0805: an oral JAK2 inhibitor, also targets FLT3/c-Fms; blocks kinase signaling; effective in rodent arthritis models.</p>

<p>(±)-Pregabalin-13C3 serves as an internal standard for the quantification of pregabalin via GC- or LC-MS. Pregabalin, classified as an anticonvulsant and analgesic, presents a potential for abuse and misuse. In the United States, (±)-Pregabalin-13C3 is regulated as a Schedule V compound, indicating restricted use mainly for research and forensic purposes.</p>

<p>Kv3 modulator 3 is a selective modulator of Kv3.1 and/or Kv3.2 and/or Kv3.3 channels .has analgesic activity for use in the prophylaxis o or treatment of pain.</p>

<p>CU06-1004 (Sac-1004) is an orally active compound that acts as an endothelial dysfunction blocker.</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>THR-β Modulator-1 (Compound 1a) is a potent modulator of the thyroid hormone receptor β, utilized in the study of thyroid hormone receptor-associated disorders</p>

<p>2,3-Diphospho-D-glyceric acid pentasodium salt is a highly anionic polyphosphorus compound located within the concave center of red blood cells, where it</p>

<p>PR825 is a β5c inhibitor with IC50 = 20 nM</p>

<p>Compound 166, also referred to as compound 3, exhibits potent anticancer properties, demonstrating significant inhibitory activity against Caco-2 cells with an</p>

<p>meplazumab is a humanized anti-CD147 antibody, as add-on therapy in patients with COVID-19 pneumonia.</p>

<p>BMS-317180 is a potent, orally active GHS with a great safety profile in preclinical studies, now in clinical development.</p>

<p>1-Arachidoyl-2-palmitoyl-3-oleoyl-rac-glycerol, a triacylglycerol, incorporates arachidic, palmitic, and oleic acids at the sn-1, sn-2, and sn-3 positions, respectively. It is present in butterfat and exhibits elevated liver levels in Plin5-overexpressing mice subjected to a high-fat diet.</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>(E)-5-Octadecene ((E)-Octadec-5-ene) serves as a sex pheromone or a chemically related compound, disrupting the sexual attraction of female Chilo suppressalis</p>

<p>2-Thiophenecarboxamide, N-(5-(p-aminophenoxy)pentyl)- is a bioactive chemical.</p>

<p>ICMT-IN-34 (compound 39) serves as an effective inhibitor of ICMT, exhibiting an IC50 value of 0.17 μM [1].</p>

<p>Veldoreotide (DG3173) TFA, a somatostatin analogue, effectively binds to and activates somatostatin receptors (SSTR) 2, 4, and 5. This compound demonstrates a higher efficacy in inhibiting growth hormone (GH) secretion in adenomas than Octreotide, showcasing its potential as a pain modulating agent [1].</p>

<p>1,3-Dipalmitoyl-2-oleoyl glycerol, a triacylglycerol, incorporates palmitic acid in the sn-1 and sn-3 positions and oleic acid in the sn-2 position. This compound is present in cocoa butter, Chinese tallow butter, and the palm stearin fraction of palm oil.</p>

UDM-001651: oral PAR4 antagonist, IC50=4 nM, Kd=1.4 nM, antiplatelet IC50=25 nM in γ-thrombin assay.

<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>DGKζ-IN-3 is an inhibitor of diacylglycerol kinase zeta (DGK-ζ), employed in the treatment of both liquid and solid cancers, as well as other diseases regulated</p>

AG-28262 besylate is a VEGFR-2 Inhibitorwhich may affect alanine aminotransferase gene expression and enzymatic activity in the liver.

<p>17(S)-HDoTE, a metabolite of adrenic acid, is synthesized through the action of 15-lipoxygenase (15-LO) via a 17-HpDoTE intermediate.</p>

<p>Himbacine is a muscarine receptor antagonist.</p>

<p>SEN461 is a wnt inhibitor.</p>

<p>SOCLAC, a derivative of the acid ceramidase inhibitor SABRAC, functions as an irreversible inhibitor of acid ceramidase with an inhibition constant (Ki) of 40.2 nM.</p>

<p>Ardisin is a Topoisomerase I and II enzyme inhibitor. Ardisin may have antioxidant effects.</p>

<p>1,2-Dilinoleoyl-3-stearoyl-rac-glycerol, a triacylglycerol, comprises linoleic acid at the sn-1 and sn-2 positions and stearic acid at the sn-3 position. It is present in various plant oils such as soybean, poppy seed, maize, evening primrose, and blackcurrant.</p>

<p>Astiron is a self-expanding bare-metal nitinol stent.</p>

<p>5(S)-HpEPE, derived from EPA by 5-LO, forms LTA5 for leukotrienes or is reduced to 5(S)-HEPE by peroxidases.</p>

<p>TFIIH Modulator-19 induces the dimerization of trichothiodystrophy group A protein to modulate TFIIH transcriptional activity.</p>

<p>L-163491: partial agonist at angiotensin II receptor type 1, less so at type 2, used in research, may treat viral lung inflammation.</p>

<p>XR3054 is a farnesyl protein transferase inhibitor that blocks proliferation in certain cancer cells, not dependent on ras mutation status.</p>

<p>KH-4-43, an inhibitor of the E3 CRL4 ligase complex, demonstrates anticancer activity by targeting the core of the E3 CRL4. It exhibits a binding affinity (Kd) of 83 nM to the E3 ROC1-CUL4A CTD and 9.4 μM to the closely related ROC1-CUL1 CTD [1].</p>

<p>MEN-10612 is a cyclic pseudopeptide and potent tachykinin NK-2 receptor antagonist.</p>

<p>AP-C7 is a selective inhibitor of cGMP-dependent protein kinase II (cGKII) with a pIC50 value of 5.0, demonstrating only weak inhibition of cGKII-dependent</p>

<p>1,3-Didocosanoyl-2-oleoyl glycerol, a triacylglycerol, incorporates docosanoic acid at the sn-1 and sn-3 positions and oleic acid at the sn-2 position. Present in cocoa butter, its use as a seed material in dark chocolate enhances solidification rates and inhibits fat bloom formation.</p>

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

<p>L 702958 is one kind of spirobenzopyran piperidine.</p>

<p>1-Stearoyl-2-oleoyl-3-linoleoyl-rac-glycerol is a triacylglycerol consisting of stearic acid, oleic acid, and linoleic acid esterified at the sn-1, sn-2, and sn-3 positions, respectively. This compound is present in peanut and soybean oils as well as in ostrich and emu oils. Additionally, it serves as a substrate for soybean lipoxygenase in cell-free assays.</p>

<p>Perfluoro(2-methyl-3-oxahexanoic) acid (HFPO-DA) is a PFECA that induces apoptosis and increases reactive oxygen species ROS levels.</p>

<p>Compound 10w, a substituted pyrazolo[1,5-a]pyrimidinamide compound, is a ZSTK474 analog that shows anticancer activity against HeLa cells.</p>

<p>HBED-CC-tris(tert-butyl ester) is a monovalent variant of HBED-CC that can be used for tumor imaging.</p>

<p>RO5263397: TAAR1 agonist, orally active, studied as antidepressant, COX-2 inhibitor.</p>

<p>Phos-tag Acrylamide AAL-107 is a polyacrylamide-conjugated phosphate-binding tag,visualizing phosphorylated proteins. High-Quality, Low-Cost!</p>

<p>Holomycin, a dithiopyrrolidone antibiotic, promotes S2753 biofilm formation and has broad-spectrum antibacterial and antitumor properties.</p>

<p>WAY-639228-A has potential antithrombotic and anticoagulant activity for the study of cerebral thrombosis.</p>

<p>gamma-Glu-Tyr (gamma-Glutamyltyrosine) is a kokumi peptide against dipeptidyl peptidase-IV (DPP-IV) and is used in the study of diabetes mellitus.</p>

<p>Melengestrol acetate is a derivative of progesterone and acts as a corticosteroid hormone.</p>

Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex. Toxoflavin also acts as an inhibitor of KDM4A.

<p>STM2120 is a potent METTL3 inhibitor (IC50: 64.5 μM) with inhibitory effect on METTL14.</p>

<p>Xinidamine: antitumor agent for prostate hyperplasia, macular degeneration; inhibits PWR-1E cell growth, IC50=4μM.</p>

<p>TCMDC-135051: Selective PfCLK3 inhibitor, low toxicity, halts parasite growth &amp; transmission; EC50=320 nM.</p>

<p>DL-Borneol ((endo)-Borneol) is a small molecule extracted from traditional Chinese medicine (TCM). It is an orally bioadjuvant that improves drug delivery to the brain and is commonly used as an adjuvant ingredient in TCM for the treatment of cardio-cerebral vascular diseases.</p>

<p>CINPA1 selectively inhibits CAR with IC50 of 70 nM, useful in CAR function studies.</p>

hRIO2 kinase ligand-1 is a potent ligand for hRIO2 kinase (Kd: 520 nM).

<p>Jarin-1: JAR1 inhibitor, blocks bioactive JA production in plants, IC50 3.8 μM.</p>

<p>α-(difluoromethyl)-DL-Arginine (RMI 71897) is an enzyma-activated, irreversible inhibitor of arginine decarboxylase for E.</p>

<p>SynuClean-D prevents α-synuclein clumps, breaks fibrils &amp; protects neurons in Parkinson’s models.</p>

STC-15 is an orally active and potent METTL3 inhibitor with anticancer activity that inhibits cancer growth and induces anticancer immunity.

<p>Antiproliferative agent-36 is a broad-spectrum anticancer benzothiazolylhydrazone-derived compound that inhibits cell proliferation.</p>

<p>PCLX-001, an oral NMT inhibitor, targets NMT1/NMT2 (IC50: 5/8 nM), shows anti-tumor properties, and hampers BCR signaling.</p>

<p>GCN2-IN-7 is an inhibitor of the environmental sensing protein GCN2 with antitumor activity for the study of melanoma.</p>

<p>Terbufibrol reduces the levels of serum total cholesterol in normal and hypercholesterolemic male rats.</p>

CMP-Sialic acid, a sodium salt, inhibits UDP-GlcNAc 2-epimerase allosterically and serves as a sialyltransferase substrate.

<p>CGS 15435: potent TxA2 synthase inhibitor, IC50=1 nM; less selective for PGI2 synthase, COX, and liposynthase.</p>

<p>CAY10781 inhibits NRP-1/VEGF-A binding by 43% at 12.5μM and blocks VEGFR2 phosphorylation in CAD cells.</p>

<p>Anti-TSWV agent 1 is a highly effective inactivator (EC50:144 μg/mL) of tomato spotted wilt virus (TSWV).</p>

Pelagiomicin C exhibits activity against both Gram-positive and Gram-negative bacteria.

<p>Cilobamine mesylate is a drug which acts as a norepinephrine-dopamine reuptake inhibitor (NDRI) and has stimulant and antidepressant effects.</p>

<p>MK-7128 is a CB1 receptor inverse agonist.</p>

<p>Cyclic-di-IMP (C-di-IMP), a STING agonist, serves as a research tool in tumor studies.</p>

<p>Emerin is an antibiotic found in the Aspergillus nidulans strain.</p>

<p>MB725 is a strong and selective inducer of viability reduction in several cancer cell lines containing the oncogenic p53-Y220C mutation.</p>

<p>Azirinomycin exhibits activity against both Gram-positive and Gram-negative bacteria.</p>

<p>(-)-Adenophorine is a moderate alpha-l-fucosidase inhibitor.</p>

BW A868C is a potent, selective PGD2 antagonist and a BW245C analogue, inert to other prostaglandin receptors.

<p>Leucomycin A9 is a macrolide antibiotic known for its potent activity against Gram-positive bacteria. It is also effective against spirochetes, rickettsiae, and chlamydiae.</p>

<p>SAR107375 is a potent, orally active dual inhibitor of thrombin and factor Xa, with K_i values of 1 nM and 8 nM for factor Xa and thrombin, respectively [1].</p>

<p>Salfredin C1 is an inhibitor of aldose reductase.</p>

<p>NA 0362 is a derivative of SF 2370 that inhibits smooth muscle contraction.</p>

<p>Piceid 6″-O-azelaic acid ester exhibited strong intracellular tyrosinase inhibition and decolorization activity.</p>

<p>5-Hydroxy-3,4,7-triphenyl-2,6-benzofurandione is an inhibitor of xanthine oxidase (XO) found in the fungus Peniophora sanguinea.</p>

<p>Chitinase-IN-5 (8i) blocks OfChi-h (IC50: 0.051 μM), has insecticidal qualities, useful for eco-friendly pest control.</p>

<p>Griseolic acid C (Dihydrodeoxygriseolic acid) is an antibiotic found in the Streptomyces griseoaurantiacus SANK43894 strain. This compound is a potent inhibitor of cyclic adenosine monophosphate (cAMP) phosphodiesterase [EC 3.1.4.17], with an IC50 of 0.12 μM (enzyme sourced from rat brain tissue).</p>