Other Inhibitors

<p>β-Catenin modulator-3 (compound IIa-112), an oxazole and thiazole-based chemical entity, serves as a potent and selective modulator of β-Catenin [1].</p>

<p>RO4927350 is a potent, selective MEK1/2 inhibitor, blocking MAPK pathway in vitro/vivo and showing notable antitumor effects.</p>

<p>FAP Ligand 1 (FL), a high-affinity small molecule targeting fibroblast activation protein (FAP), facilitates the delivery of conjugated therapeutics to FAP-</p>

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

<p>WAY-313318 is an active compound.</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>Fluocortin butyl ester is a topical corticosteroid without systemic effects, effective in treating perennial rhinitis.</p>

<p>ONO-8539 is a prostanoid EP1 receptor antagonist.</p>

<p>Abiraterone sulfate N-oxide, a carboxylic acid and major metabolite of Abiraterone, is utilized in prostate cancer research [1] [2].</p>

<p>2-MT 63: Novel, selective TIE-2 kinase inhibitor with &gt;30-fold specificity over other angiogenesis-related kinases like KDR, PDGFR, EPHB4.</p>

<p>DM-Nitrophen tertasodium acts as a calcium (Ca 2+) cage, releasing Ca 2+ when cleaved by near-ultraviolet light illumination, and is utilized in the study of Ca</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>PDE12-IN-3 is an inhibitor of phosphodiesterase 12 (PDE12) (pXC50 of 7.68),with antiviral activity.</p>

<p>Onchidal is a key lipid-soluble defense compound from Onchidella binneyi's secretion for chemical protection.</p>

<p>CGP-49823 is a non-peptide tachykinin NK1 receptor antagonist.</p>

<p>C6 dihydro Ceramide (d18:0/6:0) is a lipid molecule that can be used in life science related research. The CAS number of C6 dihydro Ceramide (d18:0/6:0) is 171039-13-7.</p>

<p>ICMT-IN-6 (compound 29) serves as an inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an inhibitory concentration 50 (IC50) value of</p>

<p>1-Myristoyl-3-chloropropanediol, a 3-monochloropropanediol (3-MCPD) fatty acid ester, induces nephropathy, tubular hyperplasia, and adenomas through chronic</p>

<p>Tetranor-PGFM, the principal urinary metabolite of PGF2α, is excreted at rates of 7-13 µg per day in healthy females and 11-59 µg per 24 hours in healthy males. During pregnancy, female urinary levels of tetranor-PGFM increase 2 to 5-fold, returning to normal shortly after childbirth.</p>

<p>(2E,9Z)-Octadeca-2,9-dienoic acid, a polyunsaturated fatty acid, is utilized in the study of lipoxygenase-dependent metabolism [1].</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>AH-9700 fumarate, salt of AH-9700, treats frequent urination from cystitis, unlike oxybutynin.</p>

Compound 1: Anti-itch, combats bites, allergens, infections, vermination, dialysis-related itching.

<p>Lalioside is a potent accelerator of neurite outgrowth.</p>

<p>Nurr1 inverse agonist-1 inhibits Nurr1 transcription by over 90%, targeting monomers, dopaminergic neuron regulation and neurodegenerative diseases.</p>

<p>Fmoc-D-Lys(N3)-OH is an azide-containing click chemistry reagent utilized in biochemical research [1].</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>glycogen phosphorylase inhibitor</p>

<p>BML-288 is a phosphodiesterase Type II (PDE2) inhibitor that demonstrates no inhibition of 5-lipoxygenase (5-LO) or cyclooxygenase (COX-1).</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>6,9,12,15-Hexadecatetraenoic acid-ethyl ester, an n-1PUFA, demonstrates oral activity and has been shown to lower plasma triglyceride levels in mice when</p>

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

<p>Methyl 10(Z)-heptadecenoate, a minor fatty acid methyl ester (FAME) component of biodiesel, is the ester derivative of cis-10-heptadecenoic acid.</p>

<p>RE-33 is an analgesic compound with the ability to penetrate the blood-brain barrier [1].</p>

<p>Tyropeptin A-4 is used as a proteasome inhibitor.</p>

<p>2-Aminotetralin acts as a neuromodulatory agent by inhibiting serotonin (5-HT) and norepinephrine reuptake in the rat brain at a dose of 39.4 mg/kg. It triggers hypothermia in rats through intracisternal or intraperitoneal injection, while the implantation of crystals in the hypothalamus' medial preoptic area leads to hyperthermia. Additionally, it mimics (+)-amphetamine in a two-lever drug discrimination test among rats in a dose-dependent manner.</p>

<p>NIBR-1282 is a CCR5 antagonist.</p>

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

FTI-276 is an inhibitor of protein farnesyltransferase (PFT) (IC50s: 0.9 and 0.5 nM for Plasmodium falciparum and human).

<p>NMS-P953: JAK2 inhibitor, reduces tumor growth in SET-2 model, confirmed in vivo action, good pharmacokinetics and safety.</p>

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

<p>Bexicaserin (Compound 3), a 5-HT2C receptor agonist, has potential applications in research pertaining to obesity and psychiatric disorders [1].</p>

<p>Trimethylcolchicinic acid methyl ether (HAN 76504), an antimitotic agent, blocks microtubule assembly by attaching to tubulin and inhibiting its polymerization. It enhances tubulin's intrinsic GTPase activity, induces apoptosis across various normal and tumor cell lines, and activates the JNK/SAPK pathway. Currently unnamed, it is referred to by a provisional code name in line with MedKoo Chemical Nomenclature (<a href="https://www.medkoo.com/page/naming)" target="_blank" rel="noreferrer noopener">https://www.medkoo.com/page/naming)</a> for ease of communication.</p>

<p>E197 is an anti-osteoporotic compound, a Dock5 inhibitor, which can be used in the study of osteoporosis.</p>

<p>WAY-119918 is an active molecule.</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>JNJ-42259152 is a phosphodiesterase 10A PET tracer.</p>

<p>HR68, a derivative of the peroxisome proliferator-activated receptor (PPAR) agonist fenofibric acid, serves as an anticancer agent.</p>

<p>WAY-621924 is an active molecule.</p>

<p>RORγt agonist 3 is a potent agonist of RORγt.</p>

<p>PLK1-IN-4: strong PLK1 blocker (&lt;0.508 nM IC50), inhibits cancer cell growth, triggers G2/M arrest and apoptosis.</p>

<p>Ovothiol C confers NAD(P)H-O2 oxidoreductase activity on ovoperoxidase.</p>

<p>Atiprimod: an oral azaspirane inhibiting STAT3, blocking IL-6/VEGF pathways, and promoting apoptosis by downregulating Bcl-2 and Mcl-1.</p>

<p>O-Demethyl apixaban sulfate, a metabolite of the factor Xa inhibitor Apixaban, is in development for treating thrombotic diseases.</p>

<p>PCSK9-IN-3 is a next-generation tricyclic peptide inhibitor of PCSK9, characterized by its novel structure, high potency, and oral bioavailability.</p>

<p>Trk-IN-11 inhibits TRK: IC50 of 1.4 nM for TrkA, 1.8 nM for TrkA G595R; potential in cancer research.</p>

<p>PPO-IN-2 is a protoporphyrinogen IX oxidase inhibitor, exhibiting a Ki value of 16 nM [1].</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>XR9051, a synthetic derivative of a natural compound, potently reverses P-glycoprotein MDR (EC50 = 1.4 nM) by inhibiting cytotoxic binding.</p>

<p>GR-92549 is an HMG-CoA reductase inhibitor.</p>

<p>CBB1007 trihydrochloride inhibits hLSD1 selectively (IC50=5.27μM), blocks demethylation of H3K4Me2/Me, and activates certain genes.</p>

<p>Prenalterol HCl: beta 1-specific agonist; treats acute cardiac failure, shock, low-output post-MI, Shy-Drager syndrome.</p>

<p>PI5P4K-β-IN-1 (compound vs1) is a potent PI5P4K-β inhibitor with an IC50 of 0.80 μM [1].</p>

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

<p>M5N36: selective Cdc25C inhibitor, IC50: 0.15µM A, 0.19µM B, 0.06µM C; halts cell growth, boosts p-CDK1/2.</p>

<p>WAY-324572 is an active compound.</p>

<p>Adomeglivant (LY2409021) is a potent glucagon receptor blocker, reducing blood glucose in type 2 diabetes with minimal side effects.</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>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>Tianagliflozin, a sodium/glucose cotransporter 2 (SGLT-2) inhibitor, is used potentially for the treatment of type 2 diabetes.</p>

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

<p>ICMT-IN-33 (compound 73) functions as an ICMT inhibitor with an IC50 value of 0.46 μM [1].</p>

<p>11(S)-HEDE, obtained through the chromatographic separation of (±)11-HEDE, lacks any documented biological activity in scientific literature.</p>

<p>LB-80380 maleate salt, a novel phosphonate nucleoside, is for the potential treatment of HBV infection.</p>

<p>Bactobolamine, an immunosuppressant, suppresses IL-2 production in CTLL cells at a concentration of 200 µg/ml and extends heart allograft survival in both MHC-</p>

<p>Antitumor Agent-40 serves as a research chemical for investigating cancer [1].</p>

<p>Sunepitron is a combined α2-adrenergic receptor antagonist and 5-HT1A receptor agonist.</p>

<p>Anticancer Agent 93, a 4-Hydroxycoumarin derivative, inhibits the invasion and migration of lung cancer cells through modulation of epithelial-mesenchymal</p>

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

<p>2-Thio-UTP tetrasodium, a potent agonist for P2Y2, P2Y4, and P2Y6 receptors, serves as a crucial compound in cancer research [1].</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>rTRD01 is a TDP-43 ligand that selectively binds to the RRM1 and RRM2 domains of TDP-43, exhibiting a dissociation constant (Kd) of 89 µM for TDP-43 102–269.</p>

<p>Phenoxan is isolated from Polyangium; inhibits electron transport at NADH-ubiquinone oxidoreductase.</p>

<p>Epelsiban Besylate is an oral drug that is a highly selective anamol oxytocin receptor antagonist.</p>

<p>SUN49199, "NaV1.7 Blocker-13," selectively inhibits NaV1.7, not NaV 1.2/1.3/1.6, stronger in humans. No official name yet.</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>Nabazenil is a synthetic cannabinoid receptor agonist which has anticonvulsant properties.</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>1,2-Dipalmitoleoyl-3-palmitoyl-rac-glycerol, a triacylglycerol, features palmitoleic acid at the sn-1 and sn-2 positions and palmitic acid at the sn-3 position. It is identified in the fat body of male B. lapidarius bumblebees.</p>

<p>ICMT-IN-13 (compound 49) functions as an inhibitor of ICMT, exhibiting an IC50 value of 0.47 μM [1].</p>

<p>MγLnFP, an analog of methyl arachidonyl fluozophosphonate (MAFP), holds significance in pharmacological research due to its potential as an inhibitor of phospholipases, FAAH, and its role as a CB receptor ligand. However, the properties and effects of the γ-linolenyl variant of MAFP remain to be fully explored.</p>

<p>(S)-FTY-720 Vinylphosphonate blocks sphingosine kinase 1 and aids its breakdown in various human cancer cells.</p>

<p>GSK598809, a D3 receptor antagonist in Phase I trials, may lessen drug cravings by reducing reward cues.</p>

(2R,3S)-E1R, an enantiomer of E1R, is a sigma-1 receptor modulator for treating cognitive disorders.

<p>NK007 is a novel anti-SARS-CoV-2 agent with an EC 50 value of 30 nM.</p>

<p>FK-352 is a pyrazolopyridine derivative and adenosine-1 receptor antagonist.</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>AtPCO4-IN-1 is a selective AtPCO4 inhibitor, exhibiting an IC50 value of 264.4 μM [1].</p>

<p>NEU-1923 is a potent inhibitor of T. brucei proliferation (EC50= 0.37 μM).</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>MK-0736 hydrochloride is a potent and selective 11β-HSD-1 inhibitor.</p>

<p>ICMT-IN-31 (compound 68) serves as an ICMT inhibitor, demonstrating significant potency with an IC50 value of 0.0038 μM [1].</p>

<p>AGN-190121 is an RAR agonist that can synergize with RXR ligands to induce hypertriglyceridemia.</p>