Other Inhibitors

<p>Advantame, an aspartame analog, serves as a non-caloric artificial sweetener frequently utilized as a food additive [1].</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>MLN-0415 is an IKK2 inhibitor which decreases NF-κB activation and down-regulates the expression of a number of inflammatory proteins.</p>

<p>(R)-FT671 is the R-isomer of FT671. FT671 is a potent, non-covalent and selective inhibitor of USP7 (IC50 of 52 nM)</p>

<p>L-159884 is a radiolabelled, nonpeptide angiotensin II antagonist that is useful for angiotensin II, AT1 receptor imaging</p>

<p>PTK7/β-catenin-IN-1 (compound 01065) is a potent inhibitor targeting PTK7/β-catenin and p53/MDM2, with IC50 values of 8.9 μM and 56.5 μM, respectively. This compound shows promise for cancer research applications [1].</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>PD-1-IN-1 is a programmed cell dealth-1inhibitor. PD-1-IN-1 can be used as an immune modulator.</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>CGP 20309 is a kind of thiocarbonylamide with high anti filamentous activity.</p>

<p>RSV604 R enantiomer is the R-enantiomer of RSV604. RSV604 is a respiratory syncytial virus (RSV) replication inhibitor.</p>

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

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

<p>N-5984 Hydrochloride is a beta3-AR agonist.</p>

<p>UR-144, a synthetic cannabinoid, exhibits high affinity for the peripheral cannabinoid receptor (CB2) with a Ki of 1.8 nM, markedly greater than its affinity for the central cannabinoid receptor (CB1), for which it has a Ki of 150 nM. XLR-11 differs from UR-144 by featuring a fluorine atom on the terminal carbon of the alkyl chain and a methyl group on the C2 carbon of the indole. The specific biological activities of XLR-11 remain uncharacterized. It is designed for forensic and research use only.</p>

<p>p38 MAP kinase inhibitor</p>

<p>Velagliflozin proline hydrate, an oral SGLT2 inhibitor, reduces blood sugar by inhibiting renal glucose reabsorption.</p>

<p>Niceritrol (Cardiolipol) is a niacin ester that reduces cholesterol and triglycerides in total plasma and in the VLD and LD lipoprotein fractions.</p>

<p>Ramipril diketopiperazine acid represents a potential impurity identified within commercial ramipril formulations.</p>

<p>AZD8926, a GSK3β inhibitor, may treat Alzheimer's, schizophrenia, and neurodegenerative diseases.</p>

<p>WAY-299765 is an active molecule.</p>

<p>Monofluoromethylagmatine is an arginine decarboxylase inhibitor.</p>

<p>eIF4A3-IN-18, a silvestrol analogue with EC50s: 0.8/35/2 nM, inhibits eIF4F complex and is cytotoxic (LC50: 0.06 nM) for cancer research.</p>

<p>AS100 is a bioactive chemical.</p>

<p>KH064 is a sPLA2-IIA inhibitor of oral activity.</p>

<p>WAY-313165 is an active molecule.</p>

<p>N-(2-Hydroxyphenyl)picolinamide is an active molecular compound.</p>

<p>O-2545 is a potent water-soluble central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptor agonist with Ki values of 1.5 and 0.32 nM, respectively. Typically, cannabinoid agonists are highly lipophilic and require solubilization through surfactant agents or binding to water miscible substances like albumin, Tween 80, or Emulphor for use. When dissolved in saline, O-2545 has shown high efficacy in mouse behavioral models, administered either intravenously or intracerebroventricularly.</p>

<p>TLR4 agonist-1 (compound 17a) serves as a potent activator of Toll-like Receptor 4 (TLR4) and stimulates the production of MIP-1β in RAW 264.7 and MM6 cells [1</p>

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

<p>SNAP-7941: Selective MCH1 receptor antagonist with potential anxiolytic, antidepressant, and appetite-suppressing qualities.</p>

<p>Enpp-1-IN-4: potent enpp-1 inhibitor with potential in cancer research. See patent WO2019177971A1, compound 1.</p>

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

<p>U 66985 is a Platelet-activating factor (PAF) receptor antagonist that inhibit the electrophysiological effects of PAF.</p>

<p>WIN site inhibitor 1 TFA is a WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5) inhibitor (Kd: 0.1 nM).</p>

<p>VUAA1, an insect odorant co-receptor (Orco) agonist, activates heteromeric and homomeric Orco-containing channels and can disrupt the behaviors of nuisance</p>

<p>DXR inhibitor 11a, with an IC50 of 0.11 µM, effectively inhibits P.</p>

<p>TOP1362: a kinase inhibitor for dry eye and ocular inflammation; targets p38α, Syk, Src, Lck; reduces cytokines and cell infiltration.</p>

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

<p>MK-8666, a partial GPCR agonist targeting GPR40, may treat type 2 diabetes by enhancing insulin secretion and lowering glucose safely.</p>

<p>glycogen phosphorylase inhibitor</p>

<p>N-3-hydroxyoctanoyl-L-Homoserine lactone, a small diffusible signaling molecule secreted by various bacteria, plays a critical role in quorum sensing—a regulatory system used by bacteria to control gene expression according to cell density changes. This compound is generated via lactonolysis from 3-oxooctanoyl-homoserine lactone and can either activate or suppress gene expression and biofilm formation. Its production and function vary within the bacterial population growth phases, consequently mediating distinct cellular effects through alterations in gene expression, hence contributing to either quorum sensing or quenching.</p>

<p>MK-8153: Selective, potent ROMK inhibitor, orally active, IC50: ROMK EP 5 μM, hERG EP 34 μM; potential diuretic.</p>

<p>C16 Ceramide-1-phosphate (d18:1/16:0) ammonium salt (C16 C1P ammonium salt) is an ester product used in synthesizing nanobiomaterials.</p>

<p>Amotosalen is a Dermatologic Agent.</p>

<p>AG28262 is a VEFG-2 inhibitor that increases serum ALT, due in part to both gene up-regulation.</p>

<p>CycLuc2, a cyclic luciferin for firefly luciferase, outshines aminoluciferin and D-luciferin by 4.7x and 2.6x, respectively.</p>

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

<p>"(S)-3'-amino Blebbistatin, retaining the active stereochemistry of the less stable and more phototoxic (–)-blebbistatin, serves as a refined selective cell-permeable inhibitor of non-muscle myosin II ATPases. This compound efficaciously inhibits the Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB across several species with IC50s ranging from 0.5-5 µM, and exhibits minimal inhibition against smooth muscle myosin (IC50= 80 µM). Its primary functions include obstructing apoptosis-related bleb formation, directed cell migration, and cytokinesis in vertebrate cells. (S)-3'-amino Blebbistatin overcomes (–)-blebbistatin's limitation of rapid degradation under blue light (450-490 nm) exposure, which generates cytotoxic intermediates, thus posing a challenge for fluorescent live cell imaging applications. The introduction of a 3'-amino group to its structure notably reduces fluorescence while maintaining (–)-blebbistatin's activity, making it a superior alternative for research purposes."</p>

<p>1-1(Z)-Hexadecenyl-2-palmitoyl-sn-glycero-3-PC, a plasmalogen, appears in various rat tissues including the liver, heart, kidney, and both gluteus and soleus muscles, as well as visceral and subcutaneous adipose tissues. It serves in lipid bilayer synthesis to investigate how amphiphilic compounds, like lysophosphatidylcholine (1-palmitoyl-2-hydroxy-sn-glycero-3-PC) and lysoplasmenylcholine, influence membrane dynamics.</p>

<p>1-Palmitoyl-sn-glycerol 3-phosphate (1-P-GPA), an endogenous metabolite, is utilized in the research of non-alcoholic fatty liver disease [1].</p>

<p>20-Ethyl Prostaglandin E2 (20-ethyl PGE2) is an analog of Prostaglandin E2 (PGE2) characterized by an extended ω-chain due to two additional methylene carbon atoms. Compared to unoprostone, a clinically approved glaucoma medication and the only extensively studied prostaglandin analog sharing this structural modification, 20-ethyl PGE2 maintains the natural 15(S) allylic hydroxyl in its lower side chain, potentially enhancing its effectiveness. Unoprostone, despite being an F-series prostaglandin, exhibits reduced affinity for FP receptors because of its lower side chain modifications (13,14-dihydro-15-keto), which diminishes its medicinal potency. Notably, 20-ethyl PGE2's efficacy relative to unoprostone and its interaction with EP or other prostanoid receptors remains unconfirmed due to the lack of published ligand binding assays. E-type prostaglandins, including 20-ethyl PGE2, are broadly acknowledged for their inflammatory, cytoprotective, and diverse biological activities.</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>Bicuculline methobromide: GABAA antagonist, IC50=3μM, induces convulsions, used in epilepsy research.</p>

WAY-616296 has potential anticholesterol activity and can be used in the study of diabetes, hypertension, psoriasis and obesity.

<p>WAY-639299 is an investigational compound targeting amyloid disorders and synucleinopathies for research purposes.</p>

<p>AMD-3329 hydrobromide: strong, selective anti-HIV agent, blocks virus replication by targeting CXCR4 co-receptor.</p>

<p>9(E),11(E)-9-nitro Conjugated Linoleic Acid (9E,11E-9-nitro CLA) is a nitrated fatty acid produced from 9Z,11E-CLA through exposure to acidified nitrite, peroxynitrite, gaseous nitrogen dioxide, or the combined action of myeloperoxidase, hydrogen peroxide, and nitrite. Additionally, it forms in LPS-stimulated RAW 264.7 macrophages, a process that can be inhibited by the nitric oxide synthase (NOS) inhibitor L-NAME. This compound has also been detected in human plasma.</p>

<p>Aptazapine (CGS 7525A) is a TECA that blocks α2-adrenergic, 5-HT2 receptors, and reverses H1; it inhibits serotonin and norepinephrine reuptake.</p>

<p>(3S,4S)-Tivantinib, a potent and highly selective inhibitor of the receptor tyrosine kinase c-MET, targets GSK3α and GSK3β—two novel enzymes implicated in the</p>

Racemetirosine is a Tyrosine 3-monooxygenase inhibitor, and inhibits the synthesis of catecholamines consequently.

<p>R1487 Hydrochloride is an inhibitor of mitogen-activated protein kinase (p38α) and is used in the study of metabolic diseases.</p>

<p>NC1 is a potent allosteric inhibitor of lymphoid-specific PTPN22, a protein tyrosine phosphatase.</p>

<p>A 53693 is a rigid catecholamine and a selective adrenergic agonist. A 53693 has affinity to certain alpha receptor subtypes in rat alpha-2 receptors.</p>

<p>TIE-2/VEGFR-2 kinase-IN-3, a benzimidazole derivative, serves as a potent inhibitor of the tyrosine kinase receptors TIE-2 and VEGFR-2, exhibiting IC50 values</p>

<p>C2 Sphingomyelin (d18:1/2:0) is a lipid molecule that can be used in life science related research. The CAS number of C2 Sphingomyelin (d18:1/2:0) is 74713-54-5.</p>

<p>AC-099 (compound 3) serves as a selective full agonist at NPFF2R (EC50 = 1189 nM) and a partial agonist at NPFF1R (EC50 = 2370 nM).</p>

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

<p>Cgs 18102A (HCl) has 5-HT(1) agonist &amp; 5-HT(2) antagonist properties.</p>

<p>Setipafant is an antagonist of the platelet-activating factor.</p>

<p>GT-2394 is a histamine H3 receptor agonist.</p>

<p>3,3,9-Trimethyl-3,4-dihydroacridin-1(2H)-one is an active molecule.</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>Onchidal is a key lipid-soluble defense compound from Onchidella binneyi's secretion for chemical protection.</p>

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

<p>7'-Hydroxy ABA (7'-OH ABA), a metabolite of Abscisic acid (ABA), arises from the hydroxylation at the 7'-carbon of ABA.</p>

<p>2-Deoxy-D-galactose is a glucose analog and glucose antagonist that inhibits the maintenance of hippocampal LTP.</p>

<p>1-(2-fluorophenyl)-3-[5-(2-methoxyphenyl)-1,3,4-thiadiazol-2-yl]urea is a chemical compound.</p>

<p>5(R)-HETE, a chemotactic for neutrophils, is a potent rare arachidonic acid derivative confirmed in S. solidissima oocytes.</p>

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

<p>AY 31906: High ceiling diuretic, boosts sodium/chloride excretion without affecting potassium, GFR, or renal flow in dogs.</p>

<p>Ro 23-0364 an imidazobenzodiazepine with mixed benzodiazepine agonist/antagonist properties.</p>

<p>6-Methoxypurine arabinoside (Ara-m), a potent inhibitor of the varicella-zoster virus (VZV), exhibits 50% inhibitory concentrations (IC50) between 0.5 and 3</p>

<p>mDPR-Val-Cit-PAB-MMAE TFA is a drug-linker conjugate for antibody-drug conjugates (ADC), comprising the tubulin polymerization inhibitor MMAE coupled with an ADC-specific peptide linker (Val-Cit-PAB) [1].</p>

<p>Pin1 modulator 1 (compound IIb-219) is a specific β-Catenin targeting agent that inhibits the Wnt pathway and is applicable in researching Wnt-mediated diseases, including cancer [1].</p>

<p>ICMT-IN-25 (compound 37) serves as a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an IC50 value of 0.025 μM [1].</p>

<p>SRX246: potent CNS-penetrant V1a antagonist (Ki=0.3 nM), inactive at V1b/V2, negligible binding at 64 other receptor classes.</p>

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

<p>WAY-658494 is an (active) compound.</p>

<p>CR6086: potent EP4 antagonist with DMARD effects, low Ki (16.6 nM), and specific anti-inflammatory action.</p>

<p>OM-1700 inhibits tankyrase 1 (IC50=127 nM) and 2 (IC50=14 nM); hinders colon cancer cell growth, COLO 320DM (GI50=650 nM).</p>

<p>10-Nitrolinoleate, a nitration product of linoleate, modulates PPARγ, enhancing glucose uptake, and aids in muscle relaxation via NO/cGMP pathway.</p>

<p>SCH79797 dihydrochloride is a PAR1 antagonist with IC50 70 nM, Ki 35 nM, antiproliferative, and pro-apoptotic properties.</p>

<p>HCAR2 agonist 1 (Compound 9n), a G i protein-biased allosteric modulator of HCAR2, activates the G i protein signaling pathway and exhibits anti-inflammatory</p>

<p>ICMT-IN-17 (compound 52) serves as an ICMT inhibitor, exhibiting an IC50 value of 0.38 μM [1].</p>

<p>Bisthianostat (CF367) is an oral HDAC inhibitor that blocks histone deacetylation, potentially disrupting cancer cell growth and inducing apoptosis.</p>

<p>Anticancer agent 61, an oral drug, inhibits HepG2, Bel-7402, MCF-7 cell growth; IC50: 1.12, 1.97, 1.08 μM respectively. Stops tumor growth.</p>

<p>11alpha-Hydroxyprogesterone, an inactive analogue of 11beta-Hydroxyprogesterone, serves as an experimental control. Meanwhile, 11beta-Hydroxyprogesterone functions as a potent inhibitor of 11β-Hydroxysteroid dehydrogenase and activates the human mineralocorticoid receptor in COS-7 cells, with an effective dose (ED)50 of 10 nM.</p>

<p>Antiarrhythmic agent-1 (example I), functioning as an antiarrhythmic agent and an IKr potassium channel blocker (IC 50 &lt;1 μM), effectively inhibits cardiac</p>

<p>Montelukast alcohol is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies.</p>

<p>VU661, a redox-active phenazine carboxamide, modulates circadian rhythms by inducing period lengthening.</p>

<p>C12 1-Deoxyceramide (m18:1/12:0) is a lipid molecule that can be used in life science related research. The CAS number of C12 1-Deoxyceramide (m18:1/12:0) is 1246298-54-3.</p>

<p>OBBA is a phospholipase A2 antagonist.</p>

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