Other Inhibitors

17-Phenyl trinor Prostaglandin F2αdiethyl amide (17-phenyl trinor PGF2αdiethyl amide) is a Prostaglandin F2α(PGF2α) analog characterized by the substitution of the C-1 carboxyl group with an N-diethyl amide. Prostaglandin (PG) esters and N-ethyl amides have demonstrated ocular hypotensive properties, with N-ethyl amides introduced as alternative options for PG hypotensive prodrugs. Studies indicate that both bovine and human corneal tissues can convert N-ethyl amides of various PGs into their free acid forms at a rate of approximately 2.5 µg/g corneal tissue/hr. However, dialkyl amides like 17-phenyl trinor PGF2αdiethyl amide resist conversion by corneal amidase, showing no detectable transformation into free acids. This characteristic suggests their potential as valuable investigative tools for assessing the intrinsic intraocular hypotensive activities of PG amides.

Mdl 27013 is a derivative of methoxysuccinyl-alanyl-alanyl-prolyl-valine.

<p>ICMT-IN-41 (compound 20) serves as a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), demonstrating an IC50 value of 0.069 μM [1].</p>

8-iso-15(R)-Prostaglandin F2α (8-iso-15(R) PGF2α) is a chemically distinct member within a broad group of prostaglandin-like eicosanoids, produced through the free radical peroxidation of arachidonic acid contained in membrane phospholipids. It represents the C-15 epimer of 8-isoPGF2α, distinguished as the sole isoprostane isomer extensively examined across numerous biological systems.

SC 34301 (Enisoprost), a strong oral PGE1 analog, decreases bacterial translocation and increases burned mice survival.

<p>MOTS-c is a mitochondria-derived polypeptide (MDP) that has anti-damage and anti-inflammatory effects by activating the AMPK pathway and inhibiting the MAP</p>

WAY-323756 is a research-active molecule utilized in the study of amyloid diseases and synucleinopathies.

<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>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>

Bicyclophenamine is a pharmaceutical active ingredient.

<p>2-Methoxyestrone is a methoxylated catechol estrogen and the principal metabolite of 2-hydroxyestrone, a nonuterotropic metabolite of estradiol.</p>

Tecarfarin sodium is a novel orally active non-competitive vitamin K epoxide reductase antagonist. Tecarfarin sodium has the antithrombotic activity.

GIV3727, a bitter taste receptor hTAS2R antagonist, inhibits the activation of hTAS2R31 by saccharin and acesulfame potassium, effectively diminishing the

TASP0376377 is a potent antagonist of CRTH2.

<p>CycLuc3 is a type of mutant firefly luciferase variant with enhanced light emission.</p>

<p>LC kinetic stabilizer-1: potent, selective for amyloid light chains, EC50: 140 nM (WIL-FL*), 74.1 nM (WIL-FL*T46L/F49Y).</p>

<p>ZD-8731, an angiotensin type 1 receptor antagonist, is used potentially for the treatment of hypertension and heart failure.</p>

ICMT-IN-22 (compound 62) acts as an ICMT inhibitor with an IC50 value of 0.63 μM [1].

PD-1/PD-L1-IN-22 is a small molecule inhibitor of PD-1/PD-L1 protein-protein interactions that blocks PD-1/PD-L1 interactions (IC50: 0.732 μM).

<p>CC-90005 is a potent, selective oral PKC-θ inhibitor with an IC50 of 8 nM, preferential over PKC-δ, and inhibits T cell activation.</p>

Cannabipiperidiethanone, a synthetic cannabinoid structurally similar to JWH 250 and AM2233, has been detected in prohibited "herbal" blends in Japan. It exhibits affinity for CB1 and CB2 receptors with IC50 values of 591 nM and 968 nM, respectively. Compared to JWH 250, its affinities for CB1 and CB2 receptors are 2.3- and 9.4-fold lower, and 13- and 70-fold lower than (R)-(+)-WIN 55,212-2, respectively. Cannabipiperidiethanone is designated for forensic and research purposes only.

This novel compound is an orally bioavailable antagonist of P2X3/P2X2/3 receptors, exhibiting potent activity with a pIC50 of 8 in both human and rat, and a pIC50 of 7.3 specifically for the human P2X2/3 receptor. It demonstrates high brain penetration, evidenced by a brain to plasma ratio of 6, and effectively blocks agonist-evoked intracellular Ca2+ flux and inward currents within the nanomolar range (10 nM to 1 µM) in cell lines that express human P2X3 and P2X2/3 receptors recombinantly. The compound also shows favorable pharmacokinetic properties, with a half-life (t1/2) of 1.63 hours and a time to reach maximum concentration (Tmax) of 30 minutes.

SQ 32970 is a potent Endothia aspartic proteinase inhibitor.

MDL-104168 is a macrocyclic HIV-protease inhibitor.

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

15(R)-Prostaglandin D2 functions as a DP(2) receptor (Prostaglandin Receptor) agonist with potential roles in prostatic hormone signaling and exhibits anti-inflammatory properties. It enhances actin polymerization in human eosinophils and elevates cAMP levels in platelets [1].

SLU-10482, an antiparasitic agent, effectively reduces C.

<p>Indinavir lactone is a protease inhibitor used as a component of highly active antiretroviral therapy to treat HIV/AIDS.</p>

DBCO-PEG2-DBCO is a click chemistry reagent comprised of a polyethylene glycol (PEG) linker flanked by two terminal dibenzocyclooctyne (DBCO) groups. These DBCO units are utilized for copper-free Click Chemistry reactions, leveraging their strain-promoted high energy to facilitate bonding. The inclusion of a hydrophilic PEG chain enhances water solubility, making it ideal for diverse research applications. This reagent is of research-grade quality [1].

<p>Sphingosine-1-phosphate (S1P), a bioactive lipid crucial in numerous signaling pathways, undergoes irreversible degradation by membrane-bound S1P lyase, producing (E)-2-Hexadecenal, a derivative of sphingolipid breakdown. This compound can be oxidized to (2E)-hexadecenoic acid by long-chain fatty aldehyde dehydrogenase before being activated through linkage to coenzyme A. Notably, (E)-2-Hexadecenal induces cytoskeletal reorganization, leading to cell rounding, detachment, activation of JNK pathway targets, and ultimate apoptosis in a variety of cell types. Furthermore, it readily forms aldehyde-derived DNA adducts through reactions with deoxyguanosine and DNA.</p>

ICMT-IN-4 (compound 28) serves as an inhibitor of ICMT, exhibiting an IC50 value of 0.27 μM [1].

DGKζ-IN-4 is a DGK-zeta inhibitor employed as an active ingredient in pharmaceutical formulations designed to treat cancers linked to immune cell activation or

2-Hydroxy arachidic acid is a hydroxylated fatty acid identified in various sources, including pasture grass (S. sphacelata), soil from abandoned pastures in Ecuador, wool wax, and as the N-acyl chain of galactosylceramides in mouse brain. [Matreya, LLC. Catalog No. 1709]

3-Azidopropanol, a click chemistry reagent featuring an azide group, holds significant potential for facilitating bindings among nucleic acids, lipids, proteins, and various molecules. Its application across numerous research domains stems from advantageous traits like high yield, specificity, and simplicity [1].

Piperidione is a cough-suppressing agent [1].

BN 52256 helps reduce arrhythmias.

3-O-Acetylbufotalin is a derivate of bufadienolide with anti-cancer activity.

1,2,3-Tri-13(E)-docosenoyl glycerol, a triacylglycerol featuring 13(E)-docosenoic acid at the \(sn-1\), \(sn-2\), and \(sn-3\) positions, transiently elevates heart triglyceride levels in weanling rats when administered as 15% of a calcium-deficient diet, with levels returning to baseline after 28 days.

<p>Amesergide is a serotonin antagonist.</p>

Nabitan hydrochloride: synthetic antiemetic and analgesic, binds CB1/CB2 receptors, lowers eye pressure, may treat glaucoma.

<p>BMS-538158 is a bio-active chemical.</p>

<p>Smo antagonist, IC50=5 nM; reduces AML cell leukemia potential and self-renewal in mice.</p>

<p>1,1'-Ethylidene-bis-(L-tryptophan) is a potential impurity in L-tryptophan commercial products, promoting EoL-3 eosinophilic leukemia cell proliferation, enhancing eosinophil cationic protein release from human peripheral blood eosinophils, and boosting IL-5 production in human T cells. At 40 µg/kg, it triggers fascia thickening, mast cell infiltration, inflammation, and fibrosis in mouse superficial adipose and panniculus carnosus tissues, serving as an eosinophilia-myalgia syndrome research model.</p>

Bibw 22 is a bifunctional modulator of P-glycoprotein and nucleoside transport.

<p>Chenodeoxycholic acid 3-glucuronide (CDCA-3G), a metabolite of Chenodeoxycholic acid (CDCA), is synthesized in human liver microsomes.</p>

FR-217840: Potential anti-rheumatic drug; inhibits matrix metalloproteinases, halts joint damage.

<p>Cis-9,10-Methyleneoctadecanoic acid methyl ester, a cyclopropane fatty acid methyl ester, stimulates DNA synthesis in rat hepatocytes and serves as a standard for quantifying cis-9,10-methyleneoctadecanoic acid in bacterial membranes through co-chromatography. [Matreya, LLC. Catalog No. 1823]</p>

<p>Potent α7L-GlyR &amp; PSAM4-5-HT3 agonist (EC50: 0.3/0.5 nM). Reduces cortical neuron activity; induces contralateral rotation in mice (LED 0.1 mg/kg).</p>

MK-8141 is a renin inhibitor. It displays some antihypertensive efficacy in hypertensive patients.

<p>FWM-4 is a potent inhibitor of SARS-COV-2 NSP13 decapping enzyme.</p>

<p>F-amidine is a selective inhibitor of protein arginine deiminases (PADs), specifically targeting PAD1 and PAD4 with in vitro IC50 values of 29.5, 350, and 21.6 µM for PAD1, PAD3, and PAD4, respectively. It irreversibly inactivates all four PAD subtypes by covalently modifying an active site cysteine crucial for enzymatic activity, with kinact/KI values of 2,800, 380, 170, and 3,000 M^-1min^-1. Additionally, F-amidine demonstrates cytotoxicity against HL-60, MCF-7, and HT-29 cancer cell lines, with IC50s of 0.5, 0.5, and 1 μM, respectively.</p>

<p>H-(Gly)3-Lys(N3)-OH (hydrochloride) is a click chemistry reagent renowned for its high yield, specificity, and simplicity, making it an ideal choice for creating bindings among nucleic acids, lipids, proteins, and other molecules across various research domains.</p>

<p>WAY-232897 is an active compound utilized in the investigation of amyloid diseases and synucleinopathies.</p>

<p>Tegolimod fumarate is an immunomodulator [1].</p>

Benzoadenosine suppresses kinase activity slightly less than does adenosine.

Microtubule inhibitor 185322 is an inhibitor of microtubule assembly, inducung mitotic arrest and apoptosis of MM cells.

CGP-49823 is a non-peptide tachykinin NK1 receptor antagonist.

PDE5-IN-42 is a selective inhibitor of second-generation phosphodiesterase type 5 (PDE5).

JWH 387, a potent analgesic cannabimimetic belonging to the naphthoylindole family, serves as a strong cannabinoid (CB) agonist targeting both central CB1 and peripheral CB2 receptors with Ki values of 1.2 and 1.1 nM, respectively. This compound is designed for research and forensic applications.

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

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

<p>AP-C3 is a potent inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), exhibiting a pIC50 value of 6.3 and</p>

Ovothiol C confers NAD(P)H-O2 oxidoreductase activity on ovoperoxidase.

<p>NCQ-469 is a metabolite of remoxipride and a dopamine D2 receptor antagonist.</p>

<p>1-Myristoyl-2-linoleoyl-3-palmitoyl-rac-glycerol, a triacylglycerol comprising myristic, linoleic, and palmitic acids at the sn-1, sn-2, and sn-3 positions respectively, is present in palm and vegetable oils.</p>

<p>1,3-Distearoyl-2-palmitoyl glycerol, a triacylglycerol, comprises stearic acid at the sn-1 and sn-3 positions, and palmitic acid at the sn-2 position. This compound is present in bovine milk fat.</p>

<p>Oxeglitazar, a peroxisome proliferator-activated receptor (PPAR) agonist, is used potentially for the treatment of gout and type two diabetes.</p>

<p>SB 203580 sulfone, an analog of the p38 MAP kinase inhibitor SB 203580, inhibits IL-1 production in monocytes and binds competitively with CSAID binding proteins (CSBP), inhibiting stress response signaling. It exhibits an IC50 of 0.2 μM for IL-1 inhibition and 0.03 μM for CSBP-mediated signaling inhibition [1].</p>

CS-526 is a reversible proton pump inhibitor targeting the K+ site on H+,K+-ATPase, reducing gastric acid secretion and preventing mucosal lesions.

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

Naamidine A is a marine alkaloid with a selective ability to inhibit epidermal growth factor receptor (EGFR)-dependent cellular proliferation.

WAY-639872 is an active molecule exhibiting (in vivo) efficacy.

Cardanol diene: phenol in cashew shells; anti-tyrosinase (IC50=52.5μM); used to make anti-E. coli biofilm complexes.

<p>MCHB-1, a potent agonist of the human cannabinoid 2 (CB2) receptor (EC50= 0.52 nM), demonstrates high selectivity for CB2 over CB1 (Kis = 3.7 and 110 nM, respectively), distinguishing itself from similar benzimidazole compounds that significantly alleviate peripheral pain while minimizing central nervous system side effects in mice.</p>

<p>eIF4A i28, an inhibitor of the eukaryotic initiation factor-4A (eIF4A) with an IC50 of 8.60 μM in an eIF4A ATPase assay, effectively reduces the viability of</p>

<p>Azilsartan mopivabil is the potent antagonist of angiotensin II receptor .</p>

<p>H 142-08 is a partial beta 1-agonist with adrenoreceptor stimulatory effects.</p>

BMS-538203 is a novel HIV integrase inhibitor.

<p>Compound B18 (RyRs activator 4) is an insect ryanodine receptor activator that exhibits larvicidal activity against Mythimna separata with an LC50 value of 1.32</p>

Adrixetinib is an inhibitor of protein tyrosine kinase with antineoplastic activity .

ACT-335827: oral, brain-penetrant OXR1 selective antagonist; IC50: 6 nM (OXR1), 417 nM (OXR2); for neurological research.

<p>Capnoidine: a potential anti-inflammatory lead for diseases with limited treatments and major side effects.</p>

<p>GGTI 2133, a peptidomimetic inhibitor of geranylgeranyl transferase type I (GGTase I; IC50= 38 nM), exhibits 140-fold selectivity towards GGTase I compared to farnesyltransferase (IC50= 5,400 nM). The compound effectively inhibits the geranylgeranylation of RAP1A (IC50= 10 µM) without affecting the farnesylation of H-Ras (IC50= &gt;30 µM). Moreover, GGTI 2133 reduces the growth, migration, and invasion of oral squamous cell carcinoma (OSSC) cells to 75, 45, and 27% of control levels, respectively. When administered intraperitoneally at 5 mg/kg per day, it prevents eosinophil infiltration into the airways in a mouse model of allergic bronchial asthma, although it does not reduce chemokine levels. Additionally, GGTI 2133 thwarts naloxone-induced contraction of ileum in rats experiencing morphine withdrawal syndrome and mitigates the severity of withdrawal symptoms in vivo (ED50= 0.076 mg/kg).</p>

<p>CGP 20376: Benzothiazole anthelmintic, modulates eosinophil burst, antifibrillatory, dose-dependent effects.</p>

<p>BMS-986122: IRAK4 inhibitor, reduces symptoms in mouse lupus models, may benefit human lupus therapy.</p>

D-threo-PDMP inhibits glucoceramide synthase, cutting cell surface glycosphingolipids and hindering neurite growth.

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

<p>ICMT-IN-9 (compound 47) is a potent ICMT inhibitor with an IC50 value of 0.16 μM [1].</p>

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

Dexlofexidine HCl, a less potent isomer of lofexidine, is an alpha 2-adrenoceptor agonist.

Flovagatran sodium, a thrombin inhibitor, is used potentially for the treatment of thrombosis.

<p>Benzyl DC-81 (Compound 6a), an anticancer agent, exhibits antiproliferative activity against A375 and MCF-7 cells [1].</p>

<p>FPL-63012AR is a D1-receptor agonist.</p>

HDAC-IN-6 is an HDAC inhibitor, targeting HDAC2, HDAC3, HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9.

<p>1,3-Dielaidoyl-2-oleoyl glycerol is a triacylglycerol consisting of elaidic acid at the sn-1 and sn-3 positions and oleic acid at the sn-2 position.</p>

<p>PF-06748962 is a potent and selective lactam-based prostaglandin EP3 receptor antagonist.</p>

GW-813893: potent, selective oral factor Xa inhibitor; Ki 4.0 nM (FXa), 9.7 nM (prothrombinase).

<p>DG046 is a potent ERAP1 inhibitor, a phosphinic pseudopeptide with unique π-stacking stabilization in the active site.</p>

VU6019650: potent M5 mAChR antagonist, IC50=36nM. May help with OUD, crosses blood-brain barrier, affects VTA dopamine neurons.

<p>Linoleoyl ethanolamide phosphate is an intermediate in the biosynthesis of linoleoyl ethanolamide, generated through phospholipase C-mediated hydrolysis of N-acylphosphatidylethanolamine. Linoleoyl ethanolamide phosphate, along with other endogenous N-acylethanolamines, is thought to regulate food intake by selectively prolonging feeding latency and post-meal interval [Linoleoyl Ethanolamide Phosphate].</p>

MDL 101146 is an orally active neutrophil elastase inhibitor.

<p>Ferroportin-IN-1 is an inhibitor of the iron transport protein Ferroportin, which regulates cellular iron efflux and metabolism, used in metabolism studies.</p>

Brivudine monophosphate, a phosphate ester, inhibits DNA repair, induces apoptosis, and may downregulate STAT3 and chemoresistance genes.

KUNG38 is a purine-based inhibitor of Grp94.