Otros inhibidores

<p>α-Synuclein inhibitor 9 (Compound 20C) is a molecule that targets and binds to cavities within mature α-synuclein fibrils, diminishing their β-sheet content.</p>

<p>11(Z),14(Z),17(Z)-Eicosatrienoic acid methyl ester is the ester derivative of 11(Z),14(Z),17(Z)-eicosatrienoic acid, identified within lipid-producing microalgae Nannochloropsis, as well as in diesel-contaminated soils and residential wastewater.</p>

<p>DC 015 is a novel potent and selective alpha 1-adrenoceptor antagonist.</p>

<p>WAY-649123 is an active molecule that exhibits (in vitro) antagonistic properties against (alpha-1A adrenergic receptors), with a (pKi) of 8.9.</p>

<p>15-epiProstaglandin A1 (15-epiPGA1) is an R-stereoisomer of PGA1, belonging to the A-series prostaglandins derived from gorgonian soft corals. PGA1 is known for its effects on renal vasodilation, promoting sodium excretion through urine, and reducing arterial pressure in hypertensive individuals. However, the specific biological activities of 15-epiPGA1 have not yet been documented in published reports.</p>

<p>Advantame, an aspartame analog, serves as a non-caloric artificial sweetener frequently utilized as a food additive [1].</p>

<p>N-Desmethyl Regorafenib N-oxide, an active metabolite of the multi-kinase inhibitor regorafenib, originates through the action of the cytochrome P450 (CYP) isoform CYP3A4. This compound demonstrates efficacy in vitro by inhibiting key enzymes such as VEGFR2, Tie2, c-Kit, and B-RAF, and it exhibits tumor growth inhibition in HT-29 and MDA-MB-231 mouse xenograft models at a dosage of 1 mg/kg.</p>

<p>Ro 18-5364 is a potent inhibitor of the gastric (H+ + K+)-ATPase with an apparent Ki of 0.1 μM at pH 6.</p>

<p>DYSP-C34, a potent ultrasound (US)-triggered multifunctional molecular machine, exhibits a favorable lipophilic/hydrophilic balance, enhanced US-induced</p>

<p>ICMT-IN-10 (compound 32) serves as an inhibitor for ICMT, exhibiting potent activity with an IC50 value of 0.184 μM [1].</p>

<p>WAY-639729 is an active compound.</p>

<p>NK3201, a specific chymase inhibitor, suppresses bleomycin-induced pulmonary fibrosis in hamsters.</p>

<p>TMC-649128, a RNA polymerase NS5B inhibitor, is used for the treatment of HCV infection.</p>

<p>ICMT-IN-43 (compound 22) acts as a potent inhibitor of the enzyme ICMT, exhibiting an inhibitory concentration (IC50) value of 0.04 μM [1].</p>

<p>DuP-532, an angiotensin type 1 receptor antagonist, is used potentially for the treatment of hypertension and heart failure.</p>

<p>Corey lactone aldehyde benzoate serves as a versatile, chiral intermediate in the synthesis of prostaglandins and their analogs.</p>

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

<p>CB 168 is a potent selective aminoacylaminoaryl tetrazole inhibitor targeting isoleucine tRNA synthetase (IleRS).</p>

<p>Activated DPG subunit facilitates the synthesis of exon jumping oligomer conjugates targeting specific sites within the human anti-muscular atrophy protein gene</p>

<p>HA-2a inhibits the JAK2/STAT3 pathway by downregulating circDcbld2 expression in RAW264.7 cells [1].</p>

<p>Phosphatidylinositols, comprising about 10% of total cellular phospholipids, are glycerophospholipids featuring a glycerol backbone, two non-polar fatty acid tails (primarily C16:0 and C18:0), and a polar inositol head group. Synthesized from cytidine diphosphate diacylglycerol (CPD-DAG) and myoinositol via phosphoinositol synthase, these compounds play pivotal roles in cellular processes, including calcium regulation, vesicle trafficking, mitogenesis, cell survival, and actin rearrangement. Phosphorylation of their inositol rings produces phosphoinositides, crucial for these cellular functions. [Matreya, LLC. Catalog No. 1048]</p>

<p>T2AA, a proliferating cell nuclear antigen (PCNA) inhibitor, disrupts protein-protein interactions between PCNA and both a PIP-box-containing peptide (IC50= 1 μM) and full-length p21, reducing cellular colocalization of PCNA with DNA polymerase δ. This compound effectively inhibits DNA replication and cell proliferation in U2OS and HeLa cells in a concentration-dependent manner, additionally inducing S phase cell cycle arrest at a 20 μM concentration. Furthermore, T2AA enhances DNA double strand break formation alongside cisplatin in a neutral comet assay and augments cisplatin-induced reductions in clonogenic survival in HeLa and U2OS cells.</p>

<p>WAY-359473 is an active compound.</p>

<p>"(15R)-Bimatoprost (15(R)-17-phenyl trinor PGF2α ethyl amide), an isomer of Bimatoprost characterized by an inverted (β) hydroxyl group on C-15 [1], is a prostaglandin analog employed in the treatment of glaucoma and ocular hypertension."</p>

<p>STING agonist D61 is a compound that activates the stimulator of interferon genes (STING), leading to the induction of IFN3-inducible secreted alkaline</p>

<p>Activated C Subunit is utilized in synthesizing exon jumping oligomer conjugates that complement specific target sites within the human anti-muscular atrophy</p>

<p>Tenalisib R Enantiomer is an R enantiomer of Tenalisib .</p>

<p>Deoxyharringtonine, an alkaloid extracted from the Cephalotaxus genus, exhibits significant anti-leukemic properties [1].</p>

<p>Hexacyclen is an analogue of 18-crown-6, antagonistic and blocking effects on the extracellular calcium-sensing receptor.</p>

<p>BRCA1-IN-2 is a cell membrane-crossing BRCA1 protein-protein interaction (PPI) inhibitor with antitumor activity that acts by disrupting the interaction of BRCA1 (BRCT)2 with proteins.</p>

<p>Heneicosapentaenoic Acid (HPA), a 21:5 ω-3 fatty acid, is found in minute quantities in green algae and fish oils, resembling eicosapentaenoic acid (EPA) but with an added carbon on the carboxyl end, positioning the initial double bond at the Δ6 location. HPA serves as a tool for examining the impact of double bond positions within n-3 fatty acids, as it is incorporated into phospholipids and triacylglycerol in vivo as efficiently as EPA and docosahexaenoic acid (DHA), while significantly inhibiting the synthesis of arachidonic acid from linoleic acid. Moreover, the ethyl ester variant of heneicosapentaenoic acid offers a more lipophilic and stable alternative to the free acid form.</p>

<p>"YM543 is an effective, oral SGLT2 inhibitor that lowers blood glucose, useful for diabetes research."</p>

<p>PDD00031705 is a benzimidazolone core cell-inactive Poly (ADP-ribose) glycohydrolase (PARG) inhibitor.</p>

<p>inhibitor of phosphodiesterase type 5 (PDE5)</p>

<p>1-Palmitoyl-3-arachidoyl-rac-glycerol is a diacylglycerol featuring palmitic acid at the sn-1 position and arachidic acid at the sn-3 position.</p>

<p>GJH-166 is an analog of dopamine that has been shown to inhibit adrenergic transmission in canines.</p>

<p>BRP-201: selective mPGES-1 inhibitor (IC50: 0.42 μM), potential next-gen anti-inflammatory drug.</p>

<p>MMV009085 is a potent inhibitor of the Plasmodium falciparum hexose transporter (Pf HT1), with potential as an anti-malarial agent.</p>

<p>PF-05241328 is an effective and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (IC50: 31 nM).</p>

<p>KNI 174 is a new type of anti‐AIDS drug used as an HIV‐1 protease inhibitor</p>

<p>Nepaprazole (TY-11345) is a potent proton pump inhibitor; IC50: 5.8µM at pH 6.0, 9.9µM at pH 7.4. Better inhibition in weak acid.</p>

<p>AKI-001: Strong Aurora kinase inhibitor, blocks Aurora A/B under 100 nM IC50,oral, halts tumor growth in mice at 5 mg/kg QD.</p>

<p>WAY-358981 is an active molecule.</p>

<p>Flovagatran sodium, a thrombin inhibitor, is used potentially for the treatment of thrombosis.</p>

<p>ICMT-IN-1 (compound 75) is a potent ICMT inhibitor with an IC50 value of 0.0013 μM.</p>

<p>Lanceolatin A exhibits adulticidal activity against Sitophilus oryzae, Rhyzopertha dominica, and Tribolium castaneum.</p>

<p>Trypanothione, a bis-glutathionyl derivative present in trypanosomatids, offers protection against oxidative stress [1] [2] [3].</p>

<p>ICI-M247496 is a non-polyglutamated analog of CB3717 and quinazoline-based inhibitor of thymidylate synthase.</p>

<p>GABA-IN-2 (Compound 5), a GABA inhibitor, exhibits both larvicidal and insecticidal properties, achieving an 87% mortality rate at a concentration of 50 mg/L [1</p>

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

<p>Metesind, a thymidylate synthase inhibitor, is used potentially for the treatment of brain cancer and solid tumours.</p>

<p>(3R,5R)-Rosuvastatin, a potential impurity detected in bulk rosuvastatin formulations, arises as a degradation product through various stresses including acid or base hydrolysis, thermal, photolytic, hydrolytic, oxidative stress, or during storage. This compound is associated with the HMG-CoA reductase inhibitor class to which rosuvastatin belongs.</p>

<p>Manoalide: sesterpenoid, PLA2/PLC inhibitor, anti-inflammatory, antibacterial.</p>

<p>Haloxyfop-P-methyl, an aryloxyphenoxypropionate herbicide, is absorbed through both foliage and roots, where it inhibits lipogenesis and induces oxidative</p>

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

PDE1-IN-2 is an PDE1 inhibitor(PDE1C, PDE1B and PDE1A with IC50 values of 6, 140 and 164 nM, respectvely).

<p>WAY-271999 is an active molecule.</p>

<p>Hydroxydione, a neuroactive steroid with general anesthetic properties, is utilized in anesthesia-related research [1] [2].</p>

<p>1R-cis-Permethrin, an insecticide and neurotoxin, acts on neuron membranes by extending the activation of sodium channels [1].</p>

<p>SLP7111228 is a potent, selective SPHK1 inhibitor with Ki values of 0.048 μM for SPHK1 and &gt;10 μM for SPH2K, showing a concentration-dependent reduction of sphingosine-1-phosphate (S1P) in U937 cells without affecting sphingosine levels. In vivo, it dose-dependently lowers S1P blood levels in rats.</p>

<p>EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM. EMD638683 S-Form is the S-form of EMD638683.</p>

<p>MDK-5432, also known as AMPA stabilizer (R,R)-2a, is the most potent AMPA stabilizer.</p>

<p>Lilopristone is an antagonist of progesterone.</p>

<p>Luminespib (AUY-922) is a 3rd-gen Hsp90 inhibitor, disrupting tumor cell proliferation &amp; oncogenic proteins, raising Hsp72 levels.</p>

<p>DC271, a retinoid and RAR agonist, mimics the cellular effects of the endogenous ATRA and the synthetic EC23, by binding to retinoid protein machinery such as CRABPII to facilitate the translocation of ATRA into the nucleus [1].</p>

<p>16,16-Dimethyl PGF2β, a metabolically stable analog of PGF2β, mitigates bronchospasm in asthma patients, albeit with lower potency compared to PGE2.</p>

<p>WAY-620445 is an active molecule.</p>

<p>Clentiazem (free base) is a calcium channel blocker. It is a chlorine derivative of diltiazem.</p>

<p>L 708286 is an agent of peptide-based phenethylcarbamoyldifluoromethylene. It is a slow-binding inhibitor of human leucocyte elastase (HLE).</p>

<p>Piridoxilate, a glyoxylate derivative, functions as an anti-anoxic agent and serves research purposes, particularly in the study of vascular diseases and</p>

<p>1-Myristoyl-3-elaidoyl-rac-glycerol is a diacylglycerol comprising myristic acid and elaidic acid at the sn-1 and sn-3 positions, respectively.</p>

<p>AC-4 is a blocker of photoswitchable TRPV1 channel.</p>

<p>WAY-322454 is an active molecule.</p>

<p>TM2 TEAD inhibitor, a robust and reversible inhibitor of the TEA domain transcription factor, presents dual inhibitory concentrations (IC50) of 38 nM for TEAD4</p>

<p>S07-1066, an aldo-keto reductase 1C3 (AKR1C3) inhibitor, enhances doxorubicin (DOX) cytotoxicity by selectively inhibiting AKR1C3-mediated reduction of DOX and</p>

<p>Antitumor agent-38 inhibits cancer cell growth, causing cell cycle arrest at the S/G2/M phase without affecting microtubules or cell shape.</p>

<p>E235, an activator of the transcription factor 4 (ATF4), enhances the integrated stress response (ISR) and DNA damage response, thereby reducing cell viability</p>

<p>Serine Hydrolase Inhibitor-21 (compound 8), a pyridine-based serine hydrolase inhibitor, exhibits a K i of 429 nM against BuChE, and shows promise for Alzheimer</p>

<p>Windaus ketone functions as a vitamin D (VD) synthesis inhibitor.</p>

<p>N-Formyl-L-histidine demonstrates a binding affinity for histidyl-tRNA synthetase, featuring a K i value of 4.6 μM.</p>

<p>STAT6-IN-1: STAT6 inhibitor, IC50=0.028 µM, targets SH2 domain, for allergy and cancer research.</p>

<p>4-Hydroxyphenylglyoxylic acid, an active metabolite of the prodrug oxfenicine, functions as an inhibitor of carnitine palmitoyltransferase 1 (CPT1).</p>

<p>ICMT-IN-44 (compound 23) serves as an ICMT inhibitor with an IC50 value of 0.167 μM [1].</p>

<p>Sodium zirconium cyclosilicate (UXSi-9) is a cation exchanger and a K+ binder used in the treatment of hyperkalemia.</p>

<p>11β-Prostaglandin F2αethanolamide (11β-PGF2α-EA), posited as the hepatic metabolite derived from PGD2-EA during COX-2 metabolism of AEA—an endogenous cannabinoid present in brain, liver, and various mammalian tissues—is synthesized directly from AEA via COX-2 and specific prostaglandin synthase, leading to ethanolamide versions of classical prostaglandins. Additionally, PGD2-EA formation occurs in activated RAW 264.7 cells upon AEA treatment.</p>

<p>1,3-Distearoyl glycerol, a diacylglycerol with stearic acid at the sn-1 and sn-3 positions, is present in wheat bran extract. It is utilized in creating prodrug versions of NSAIDs (ibuprofen, naproxen, and diclofenac) with decreased ulcerogenicity.</p>

<p>SRI 6409-94, a teratogenic analogue of Ro 13-6298, is orally active and utilized as a molecular tool to investigate the impact of retinol's three-dimensional</p>

<p>1,2-Dipalmitoyl-3-linoleoyl-rac-glycerol, a triacylglycerol, features palmitic acid at the sn-1 and sn-2 positions and linoleic acid at the sn-3 position. This compound is present in ostrich and emu oils as well as in bovine milk fat.</p>

<p>DAO-IN-1 (compound 10) is a potent DAO (D -amino acid oxidase) inhibitor that ameliorates schizophrenia by increasing D -serine levels in the brain.</p>

<p>L 662025 is a PAF receptor antagonist.</p>

<p>(2,4-Dichloro-3,5-dimethoxyphenyl) methyl 6-O-β-D-glucopyranosyl-β-D-glucopyranoside, an anticancer agent, inhibits A549 lung cancer cell proliferation with an</p>

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

<p>13(S)-HOTrE, the 15-lipoxygenase (15-LO) metabolite of linolenic acid, is present in cell membranes and as a cholesteryl ester in atherosclerotic lesions, as well as in the biomembranes of soybeans subjected to 15-LO.</p>

<p>Acifluorfen-methyl, a photobleaching herbicide [1], functions as an inhibitor of the enzyme protoporphyrinogen oxidase (Protox), which is crucial for heme and</p>

<p>OXA-06 hydrochloride, an ATP-competitive ROCK inhibitor, impedes anchorage-dependent growth and invasion in non-small cell lung cancer cell lines. It effectively inhibits cofilin phosphorylation without inducing apoptosis [1].</p>

<p>(rel)-Tivantinib is a potent, highly selective inhibitor of the receptor tyrosine kinase c-MET and has additional novel targets, GSK3α and GSK3β, that are</p>

<p>Cy-FBP/SBPase-IN-1 (compound S5) serves as an inhibitor of the key regulatory enzyme Cy-FBP/SBPase in cyanobacterial photosynthesis, impeding the Calvin cycle</p>

<p>STING agonist-3: non-nucleotide, selective, anti-tumor with pEC50=7.5, pIC50=9.5, could enhance cancer therapy.</p>

<p>Lanabecestat (AZD3293/LY3314814) is a potent oral BACE1 inhibitor that crosses the BBB and reduces Aβ levels.</p>

<p>SOBRAC, a derivative of the acid ceramidase inhibitor SABRAC, acts as an irreversible inhibitor of acid ceramidase (Ki= 29.7 nM).</p>

<p>SIC5-6 is a potent inhibitor of Separase, a substantial cysteine protease implicated in critical cellular processes such as chromosome segregation during</p>

<p>TRβ agonist 3 (Compound 3) is a potent TRβ agonist that is a new potential TRβ-selective thyromimetics.</p>

<p>Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are a class of endogenous lipids whose levels are modulated by fasting and high-fat diets, and they play a role in insulin sensitivity. These compounds consist of a fatty acid—either a C-16 or C-18, such as palmitoleic, palmitic, oleic, or stearic acid—esterified to a hydroxylated C-16 or C-18 lipid. One notable FAHFA, 9-PAHSA, features an ester linkage between palmitic acid and 9-hydroxy stearic acid. PAHSAs, with 9-PAHSA being the most prevalent isomer, are significantly found in the serum and both white and brown adipose tissues of glucose-tolerant AG4OX mice, which express the Glut4 gene in adipose tissue, enhancing insulin sensitivity. Additionally, 9-PAHSA is abundant in wild type and AG4OX mice and present in humans, though at reduced levels in those with insulin resistance. 9-PAHSA is associated with improved glucose tolerance, enhanced insulin secretion, and anti-inflammatory effects in mice. The compound 19-PAHSA^13C4 represents an isotopically enriched form of this polyunsaturated fatty acid.</p>

<p>Prostaglandin F2α serinol amide, a serinolamide G protein-coupled receptor, elevates calcium levels in human non-small cell lung cancer cells. Additionally, Prostaglandin F2α functions as a luteinizing hormone in sheep and potentially serves as a nociceptive mediator in the spinal cord [1] [2] [3].</p>