Otros inhibidores

<p>TA-606 is an angiotensin type 1 receptor antagonist with antihypertensive activity.</p>

<p>Amedalin is a biochemical.</p>

<p>CBM-301940 is a oral MCD (Malonyl-CoA Decarboxylase) inhibitorthat improves cardiac efficiency and function with cardioprotective properties.</p>

<p>CYP11A1-IN-1 (compound 30) is a selective inhibitor of the enzyme CYP11A1, displaying an IC50 ranging from 201-2000 nM.</p>

<p>WAY-327131 is an active molecule.</p>

<p>Val-Cit-PAB-OSBT is a degradable ADC (Antibody-Drug Conjugate) linker composed of the polypeptide Val-Cit-PAB and the OSBT groups [1].</p>

<p>GSK-256066 is a PDE4 inhibitor.</p>

<p>Apaxifylline is a selective Adenosine A1 antagonist.</p>

<p>Activated EG3 Tail facilitates the synthesis of exon-skipping oligomer conjugates that target specific sites within the human anti-muscular atrophy protein gene</p>

<p>Compound 15, 2-Quinizarincarboxylic acid, functions as a glucose uptake inhibitor, demonstrating a 24.9% inhibition rate at a concentration of 50 μM [1].</p>

<p>DW10075, a novel potent and highly selective inhibitor of VEGFR, exhibits antitumor activities both in vitro and in vivo.</p>

<p>CGP 57813 is a lipophilic compound, which can be used as an inhibitor of HIV-1 protease.</p>

<p>SARS-CoV-2/MERS Mpro-IN-1 is a potent inhibitor of the main proteases in SARS-CoV-2 and MERS, exhibiting IC50 values of 0.10 and 0.06 µM, respectively.</p>

<p>AZD6126 (ANG-453), a water-soluble prodrug converted to N-acetylcolchinol in vivo, potentially treats solid tumors by inhibiting angiogenesis and tubulin.</p>

<p>ATIC-IN-1 (compound 14) serves as an inhibitor specifically aimed at the dimerization of Aminoimidazole carboxamide ribonucleotide transformylase/inosine</p>

<p>Cisd2 agonist 2 (compound 6), with an EC50 of 191 nM, is an orally active activator of Cisd2, a protein whose levels are associated with nonalcoholic fatty</p>

<p>Fluprostenol isopropyl ester, a potent agonist of the F-series prostaglandin receptor, serves as a prodrug utilized clinically as an ocular hypotensive agent for glaucoma treatment. An impurity, 13(R),14(R)-epoxy fluprostenol isopropyl ester, arises during its production, existing as a chiral enantiomer of the epoxide. The pharmacological properties of this specific enantiomer have yet to be thoroughly investigated.</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>Vamagloxistat is a glycolate oxidase inhibitor utilized to mitigate hyperoxaluria and reduce the formation of kidney stones [1].</p>

<p>Ebopiprant (OBE-022) is an oral, selective PGF2α antagonist for preterm labor, safer than indomethacin.</p>

Vedaclidine tartrate is a muscarinic analgesic.

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

<p>Makaluvamine A comes from the fruiting bodies of Didymium bahiense that act as active anti-cancer agents and DNA topo II inhibitors.</p>

<p>PD 117302: nonpeptide, kappa-opioid agonist, anti-arrhythmic, anticonvulsant, impacts locomotion, diuresis.</p>

<p>Droxinavir Free Base is an experimental protease inhibitor researched by Pharmacia as a treatment for HIV infection.</p>

<p>Cytidine 3'-monophosphate, a ribonucleotide, results from the hydrolysis of cytidine 2',3'-cyclic monophosphate via RNase—a process that cytidine 3'-monophosphate itself inhibits. Additionally, it can be dephosphorylated to cytidine by 3'-nucleotidase.</p>

<p>LY 154045 is a selective antagonist of N-methylaspartate.</p>

<p>Spectramide is a dopamine D-2 receptor antagonist.</p>

<p>Axl-IN-12 inhibits AXL, useful in studying various diseases including cancer and autoimmune disorders.</p>

<p>ATI-22-107 is a positive cardiac inotropic agent which may affect myocyte calcium cycling and contractility.</p>

<p>AZD4619 is a potent, selective and reversible orally bioavailable agonist of PPARα receptor.</p>

<p>AGN-191129 (PGF2α-OMe) is a PGF2α analog with C-1 carboxyl replaced by O-methyl; it lowers eye pressure, but its receptors are unclear.</p>

<p>AMOR is unique to plant cell walls and enhances plant fertilization efficiency and capacity</p>

<p>A-794278 is a bioactive chemical.</p>

<p>DCLK1-IN-2 (Compound I-5) is a potent inhibitor of DCLK1, exhibiting an IC50 of 171.3 nM, and demonstrates significant antiproliferative effects on SW1990 cell</p>

<p>1-Stearoyl-2-lauroyl-rac-glycerol, a diacylglycerol, features stearic acid at the sn-1 position and lauric acid at the sn-2 position. It serves as a substrate for the rat diacylglycerol lipase DDHD2.1.</p>

<p>WAY-354436 is an active molecule.</p>

<p>Agavoside A is a biochemical.</p>

<p>ZM 260384 is a potassium channel opener.</p>

<p>17-Phenyl trinor Prostaglandin F2α isopropyl amide is a derivative of 17-phenyl trinor prostaglandin F2α ethyl amide.</p>

<p>Japonilure is an agent of insecticide and pheromone.</p>

L 640035 inhibits human platelet aggregation which is induced by arachidonic acid, collagen, and the prostaglandin-endoperoxide analog of U44069.

<p>Furodysinin is an agonist of human leukotriene B4 receptor.</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>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>

FR-193879 is an efficacious cephem derivative, it has extremely potent therapeutic efficacy against H. pylori.

<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>NEU-730, a novel inhibitor of TbrPDEB1, shows modest inhibition of T. brucei proliferation.</p>

<p>Limocrocin is an inhibitor of reverse transcriptase.</p>

<p>RO4583298 is a highly potent dual NK1/NK3 receptor antagonist with in vivo activity.</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>MDL-25637 is a glucosidase inhibitor.</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>PF 00277343, a thyroid receptor agonist, is used for the treatment of androgenetic alopecia.</p>

<p>SRX 251, a vasopressin V1a receptor antagonist, is used potentially for the treatment of primary dysmenorrhea.</p>

<p>CL-329167, a angiotensin type 1 receptor antagonist, is used potentially for the treatment of hypertension.</p>

<p>MK-0736 hydrochloride is a potent and selective 11β-HSD-1 inhibitor.</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>AGN-201904Z is a slow-release, acid-resistant pro-PPI that turns into omeprazole, offering extended acid suppression.</p>

<p>TSR011-isomer, a TrKA/ALK inhibitor, is used potentially for the treatment of solid tumours and lymphoma.</p>

<p>B 581 is an inhibitor that specifically blocks farnesylated.</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>ZINC08792229 is a novel inhibitor of SIRT1.</p>

<p>JYL-1511 is the TRPV1 channel partial agonist.</p>

<p>Oxilorphan is a μ-opioid blocker and a weak κ-opioid activator; similar to naloxone in strength; can cause hallucinations and dysphoria.</p>

<p>NEU-1923 is a potent inhibitor of T. brucei proliferation (EC50= 0.37 μM).</p>

<p>BMS-189664 is an inhibitor of thrombin.</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>GSK1360707 is a selective triple reuptake inhibitor (TRI).</p>

<p>14S(15R)-EET methyl ester, an oxylipin derived from arachidonic acid through cytochrome P450 metabolism, demonstrates specific biological activities. It exhibits affinity for isolated guinea pig monocytes, evidenced by a competitive binding assay with a Ki value of 612.5 nM using [3H]14(15)-EET. This compound notably enhances the dilation of precontracted isolated canine epicardial arterioles (EC50= 4 pM) and denuded porcine subepicardial arterioles (EC50= 3 pM), indicating potent vasodilatory effects. Unlike its isomer 14R(15S)-EET, 14S(15R)-EET methyl ester does not inhibit COX activity in enzyme assays or affect isolated platelets, highlighting its distinct functional profile.</p>

<p>12-Bromododecanoic acid, a halogenated derivative of lauric acid, serves in the synthesis of clickable myristic acid derivatives and functions as a model fatty acid ligand for elucidating the X-ray crystal structure of bovine β-lactoglobulin-ligand complexes. This compound, at a concentration of 10 µg/ml, has been shown to diminish virion DNA in the culture supernatant of primary hepatocytes from a duckling model of hepatitis B virus (HBV) infection and exhibits inhibitory activity against HIV replication in CEM-SS T cells with an EC50 value of 38 µM.</p>

<p>A 69992 is an HIV anti-infective nucleoside.</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>LY 106737 is opioid antagonist in the class of phenylpiperidine.</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>NVP-ABJ688 is the cysteine protease cathepsin K inhibitor.</p>

<p>HDM-201 succinate is an orally bioavailable human double minute 2 homolog (HDM2) inhibitor with potential antineoplastic activity.</p>

<p>GX-395 is a novel Nav1.7 inhibitor.</p>

<p>L-644,698 is a selective agonist of human prostanoid DP receptor.</p>

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

<p>FK-352 is a pyrazolopyridine derivative and adenosine-1 receptor antagonist.</p>

<p>TNFalpha-IN-S10 is an inhibitor of TNF-α.</p>

<p>TA-1887: Selective SGLT2 inhibitor, treats type 2 diabetes, lowers glucose in high-fat diet mice, boosts UGE, has good pharmacokinetics.</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>E197 is an anti-osteoporotic compound, a Dock5 inhibitor, which can be used in the study of osteoporosis.</p>

<p>PA-082: PPARγ partial agonist, boosts coactivator-1α, reduces triglycerides, enhances insulin signaling.</p>

<p>Aganepag isopropyl can be used to treat Glaucoma.</p>

<p>ML 10, a [18F] PET radiotracer, detects apoptosis-specific alterations in atherosclerotic plaques.</p>

<p>Difelikefalin: KOR agonist, EC50 of 0.16 nM in humans, inhibits cAMP (EC50=0.048 nM), selective over MOR, reduces pain and itching in mice.</p>

<p>MDL-72392 is a monoamine oxidase inhibitor.</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>

<p>Cyclotheonellazole A inhibits elastase (IC50=0.034nM) &amp; chymotrypsin (IC50=0.62nM), a natural macrocyclic peptide.</p>

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

<p>Adaprolol is a beta-adrenergic antagonist. Enantiomers of Adaprolol may be used in the treatment of Glaucoma or other ailments of the eye.</p>

<p>TLR9-IN-18 is a potent and selective TLR9 antagonist. TLR9-IN-18 suppresses the production of the proinflammatory cytokine IL-6 in a CpG-induced mouse model.</p>

<p>Clazuril, a phenylacetonitrile derivative, treats coccidiosis in poultry by killing Eimeria species.</p>

<p>CBB3001 is a selective lysine-specific histone demethylase LSD1 inhibitor.</p>

<p>BX-320, a PDK1 inhibitor (IC50=30nM), selectively blocks Akt/p70S6K1 phosphorylation, induces apoptosis, and inhibits cancer cell growth.</p>

<p>Solimastat: oral MMPI, &gt;10x active than marimastat, inhibits cell-bound TNF-alpha processing.</p>

<p>PARP7-probe-1: biotinylated, chemiluminescent PARP7 active site probe for research use.</p>

<p>Sjc 13 is an azaindolidine derivative that is a cell adhesion molecule inhibitor.</p>

<p>Deleobuvir sodium (BI207127), a hepatitis C NS5B inhibitor, showed promise in some trials but was discontinued in 2013 due to insufficient efficacy.</p>

<p>WH-10417-099 is a degrader capable of inducing the degradation of an extensive array of unique kinases, exceeding 125 in total [1].</p>

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