Other Inhibitors

<p>SOMG-833 HCl is a selective inhibitor of c-MET. It acts by blocking c-MET dependent neoplastic effects and exerting antitumor activity.</p>

<p>1-Palmitoyl-3-oleoyl-sn-glycero-2-PE is an active molecule that can be used in life science related research. The CAS number of 1-Palmitoyl-3-oleoyl-sn-glycero-2-PE is 884324-34-9.</p>

<p>Rel-HDMP-28 hydrochloride (Compound 2g) is an analogue of methylphenidate, exhibiting selective affinity for the serotonin transporter (SERT) with a binding constant (Ki) of 105 nM [1].</p>

<p>Sure, here is a clearer and more professional version:<br><br>"WAY-637940 is an active molecule."</p>

<p>CJ-15161 (free base), an opioid κ-receptor agonist, is undergoing development with Pfizer as an analgesic agent.</p>

<p>Metabutoxycaine, a local anesthetic [1], serves to numb specific areas of the body.</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>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>Diacylglycerols (DAG) are generated through the hydrolysis of membrane phospholipids and function as lipid second messengers by activating protein kinase C (PKC) and modulating cell growth and apoptosis. Additionally, they act as precursors for DAG kinases in the synthesis of phosphatidic acid, a crucial lipid messenger. The compound 1-NBD-decanoyl-2-decanoyl-sn-glycerol incorporates a nitrobenzoxadiazole (NBD) fluorophore at the ω-end of its terminal decanoyl chain, using the structure of 1,2-didecanoyl-sn-glycerol as a model for diacylglycerol. This molecule is expected to exhibit excitation and emission peaks at roughly 470/541 nm, paralleling those of various NBD-labeled phospholipids. Fluorescently labeled lipids, such as this, are instrumental in exploring their interactions with proteins, their uptake by cells and liposomes, and in developing assays for lipid metabolism research.</p>

<p>3-Hydroxy Nonanoic Acid, a hydroxylated fatty acid, is present in the young peridioles of Pisolithus fungi, LPS of P. aeruginosa, bovine milk, and the methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers synthesized by P. oleovorans [Matreya, LLC. Catalog No. 1725].</p>

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

<p>Lansoprazole N-oxide is a potential impurity in lansoprazole bulk preparations, identified as a degradation product under acidic or basic conditions. This compound is related to lansoprazole, a proton pump inhibitor.</p>

<p>Mk-7725 is an effective selective bombesin receptor subtype 3 agonist for the treatment of obesity.</p>

<p>DC-120: ATP-competitive AKT inhibitor, hinders liver cancer growth, triggers apoptosis, blocks AKT pathway, effective in vivo/vitro with EC50 of 153 nM.</p>

<p>eIF4A3-IN-17, a silvestrol analogue, disrupts eIF4F assembly; EC50: 0.9-15 nM. Used in cancer pathogenesis research.</p>

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

<p>AZ-2 induces ABCA1/apoE, boosts ABCA1, reduces P2X7 activity, and activates LXR signaling without direct LXRα/β agonism.</p>

<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>8(S)-HETE activates mouse keratinocyte PKC (IC50: 100 μM) and PPARα (&gt;0.3 μM); identified by chiral HPLC in murine skin.</p>

<p>Oxycodegol phosphate is a mu-opioid agonist used in the treatment of Moderate to Severe Chronic Low Back Pain</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>BAY-678: Oral selective human neutrophil elastase inhibitor; IC50: 20 nM; SGC-approved chemical probe.</p>

<p>WAY-312491 is an active compound.</p>

<p>CGC 11093: A polyamine analog inhibiting human prostate tumor growth in mice; may help regress choroidal neovascularization.</p>

<p>ASP8497 is a potent DPP-IV inhibitor enhancing GLP-1, used for type 2 diabetes and glucose intolerance.</p>

<p>C24 (2'(R)-hydroxy) dihydro Ceramide (d18:0/24:0) is a lipid molecule that can be used in life science related research. The CAS number of C24 (2'(R)-hydroxy) dihydro Ceramide (d18:0/24:0) is 164989-36-0.</p>

<p>B-Raf IN 5 is a potent inhibitor of the protein kinase B-Raf (IC50: 2.0 nM). B-Raf IN 5 resists rapid metabolism and does not bind to the secondary target PXR.</p>

<p>VU0531245 is a potent inhibitor of the SLACK (Sequence Like A Calcium-activated K+) channel, exhibiting an IC50 of 2.1 μM [1].</p>

JYL-273 is a TRPV1 agonist.

<p>Δ7(Z)-C14-HSL (Compound 12), an immunosuppressive agent, inhibits the proliferation of mouse splenic cells, exhibiting an IC 50 of 17 μM. It holds promise for exploring its role as a molecular mechanism in TNF-R-driven immune diseases, including autoimmune disorders like psoriasis, rheumatoid arthritis, and type 1 diabetes [1].</p>

<p>(R)-Butaprost (free acid) is a prostaglandin E2 (PGE2) analog exhibiting high EP2 receptor subtype selectivity, commonly used to delineate EP receptor</p>

<p>Piribedil N-oxide, a metabolite of the dopamine receptor agonist piribedil, represents a chemical compound involved in the metabolic processing of its parent compound, piribedil.</p>

<p>RB-3, a PRC1 inhibitor, binds to RING1B-BMI1f , with a K d of 2.8 μM.</p>

<p>1,3-Dioleoyl-2-linoleoyl glycerol, a triacylglycerol, features oleic acid at the sn-1 and sn-3 positions and linoleic acid at the sn-2 position. This compound is a prominent species in butterfat and is present in A. trifoliata seed oil (ASO), along with smaller amounts in its physical blends and interesterified products.</p>

<p>RO5068760, a selective MEK1/2 inhibitor, effectively targets a range of tumors, particularly B-RafV600E mutants, with an IC50 of 0.025 μM.</p>

<p>N-Arachidonoyl-L-serine (ARA-S), a recently isolated endocannabinoid with a distinct activity profile that diverges from typical endocannabinoids, does not interact with central cannabinoid (CB1), peripheral cannabinoid (CB2) receptors, or vanilloid receptor 1 (VR1). Unlike other compounds, ARA-S (5 mg/kg) counteracts the lowering of blood pressure induced by a 10 mg/kg intravenous bolus of abnormal cannabidiol (Abn-CBD) in anesthetized rat models. Additionally, akin to Abn-CBD, ARA-S induces relaxation in isolated rat mesenteric arteries and abdominal aorta and promotes phosphorylation of Akt and mitogen-activated protein kinase (MAPK) in human umbilical vein endothelial cells (HUVEC). The mechanisms through which ARA-S and Abn-CBD exert their effects on vascular systems show variations and merit deeper investigation.</p>

<p>SB-682330A is a Raf kinase inhibitor.</p>

<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>3'-Ethoxy spinosyn L, a minor component in the insecticide spinetoram, is utilized in certain formulations for its insecticidal properties. Marketed solely for research and analytical purposes, it is designed for controlled laboratory use with no option for bulk purchase.</p>

<p>D-Carnitine, an orally available isomer of the essential nutrient L-carnitine, facilitates the transport of long-chain fatty acids into the mitochondrial matrix for beta-oxidation. Additionally, D-Carnitine exhibits antiparasitic activity [1] [2] [3].</p>

<p>GLPG-0259 is an inhibitor of mitogen-activated protein kinase-activated protein kinase 5 (MAPKAPK5).</p>

<p>1-Palmitoyl-2-oleoyl-3-linolenoyl-rac-glycerol is a triacylglycerol comprising palmitic acid, oleic acid, and α-linolenic acid esterified at the sn-1, sn-2, and sn-3 positions, respectively.</p>

<p>Spermine (N3BBB), a click chemistry reagent with an azide group, facilitates diverse biochemical studies [1].</p>

<p>BAY-204 is a CSNK1α/δ inhibitor that can be used in the treatment of proliferative diseases.</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>IDN-1965: potent, irreversible caspase inhibitor; blocks Fas-induced apoptosis; varied administration; promising for liver injury treatment.</p>

<p>PU-48 is a potent inhibitor of urea transporters A (UT-A) with an IC50 value of 0.32 μM, exhibiting a significant diuretic effect in mouse models without</p>

BD-AcAc 2 (Ketone Ester) is a ketone monoester and can be used as a source of oral nutritional ketones.

<p>CU06-1004 (Sac-1004) is an orally active compound that acts as an endothelial dysfunction blocker.</p>

<p>(E)-5-Octadecene ((E)-Octadec-5-ene) serves as a sex pheromone or a chemically related compound, disrupting the sexual attraction of female Chilo suppressalis</p>

<p>WAY-612453 is an active compound utilized in researching amyloid diseases and synucleinopathies.</p>

<p>Prostaglandin G2 (PGG2) serves as the initial stable intermediate in the COX pathway, identifiable and characterizable due to its stability. This compound is identified as the C-15 hydroperoxide derivative of PGH2. Typically, PGG2 undergoes rapid metabolism via the inherent peroxidase activity of both COX-1 and COX-2 enzymes, resulting in the production of PGH2. PGH2 is crucial as it is the primary precursor for the generation of 2-series prostaglandins and thromboxanes.</p>

<p>Gemcitabine-ibandronate (GEM–IB), a conjugate of gemcitabine (GEM)-5'-phosphate with ibandronate (IB), exhibits efficacy both as a monotherapy and</p>

<p>A1AT Modulator 1 potently inhibits Z α1-antitrypsin (A1AT) polymerization, exhibiting a pIC50 of 8.3 [1].</p>

<p>2C07 is a Novel switch-II binder. 2C07 alters nucleotide preference and inhibits SOS binding and catalyzed nucleotide exchange.</p>

<p>MSN8C, a mansonone E analog, acts as a novel catalytic inhibitor of human DNA topoisomerase II, inducing apoptosis in cancer cells and exhibiting considerable</p>

<p>BDW568, a prodrug of BDW-OH, serves as a stimulator of interferon genes (STING) agonist.</p>

<p>Orexin Receptor Modulator-1 is a compound utilized in the study of various conditions including substance addiction, panic disorder, anxiety, post-traumatic</p>

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

<p>1-Palmitoyl-2-Linoleoyl-sn-glycero-3-phosphatidylcholine (PC) is a phospholipid characterized by the incorporation of palmitic (16:0) and linoleic (18:2) acids at the sn-1 and sn-2 positions, respectively. It is utilized in the creation of micelles, liposomes, and various artificial membranes, playing a significant role in research on lipid peroxidation.</p>

<p>O-1057 hydrochloride is a water-soluble cannabinoid receptor agonist with antinociceptive properties. RESEARCH USE ONLY.</p>

<p>Prostaglandin E2 Serinol Amide acts as a weak inhibitor against the hydrolysis of [3H]2-oleoylglycerol, but it is non-hydrolyzable and cannot produce PGE2. Consequently, it is unable to inhibit leukotriene B4 biosynthesis, superoxide production, migration, and the release of antimicrobial peptides [1].</p>

<p>Jak2-IN-7j is a selective Jak2 inhibitor which demonstrates a time-dependent knock-down of pSTAT5, which is a downstream target of Jak2.</p>

<p>1-Stearoyl-2-palmitoyl-3-oleoyl-rac-glycerol is a triacylglycerol comprising stearic acid (at the sn-1 position), palmitic acid (at the sn-2 position), and oleic acid (at the sn-3 position), identified in bovine milk.</p>

<p>Hydroxy lenalidomide, a metabolite of the thalidomide analog and anticancer agent lenalidomide, is a derivative substance involved in the metabolic process of its parent compound.</p>

58-G3 is an agonist of methuselah (Mth)-specific that acts by inducing dose-dependent calcium elevation and membrane translocation of β-arrestin2.

<p>(-)-15-Deoxyspergualin trihydrochloride exhibits potent antitumor properties and demonstrates significant inhibition activity against mouse leukemia L-1210 [1].</p>

<p>Cis-10-Nonadecenoic acid methyl ester, a fatty acid methyl ester, serves as a chromatography standard for the quantification of cis-nonadecenoic acid.</p>

<p>BIM-46068 is a potent inhibitor of human farnesyltransferase with a unique anti-proliferative profile.</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>

<p>Cotosudil 2HCl is the salt form of Cotosudil Free Base, a Rho-associated (ROCK) kinase inhibitor.</p>

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

<p>Indacaterol xinafoate is an ultra-long-acting beta-adrenoceptor agonist.</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>MDL-19744A is an alpha 1-adrenergic receptor antagonist and renal vasodilator.</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>BO-1158 is an antibacteria agent.</p>

<p>5-Azacytidine 5′-triphosphate (5-aza-CMP), a cytidine analog, selectively inhibits the incorporation of [^3H]CTP into RNA during the DNA-dependent RNA</p>

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

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

<p>12:0 N-Biotinyl fatty acid, a biotinylated derivative of lauric acid, serves as an intermediate for synthesizing N-biotinylated phenylarsonous acids.</p>

<p>SHP2-IN-18 (compound 183) is a potent SHP2 inhibitor, exhibiting an IC50 of 3 nM and applicable to glioblastoma research [1].</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>

<p>2-O-methyl PAF C-16 is a synthetic analog of platelet-activating factor (PAF) featuring a methyl group attached via an ether linkage at the sn-2 position. While the specific biological activities of 2-O-methyl PAF C-16 remain undercharacterized, studies with its C-18 counterpart have demonstrated its ability to modulate various biological processes. These processes include reducing plasma membrane fluidity and hindering the invasiveness of tumor cells in embryonic chick hearts. Furthermore, in rat astrocytes, the C-18 analog prompts the release of significant amounts of nitric oxide (NO) through a mechanism that involves the activation of nitric oxide synthase (NOS).</p>

<p>HV-723 fumarate is an alpha-1 adrenoceptor antagonist.</p>

<p>U-51605, a stable analog of the endoperoxide prostaglandin H2 (PGH2), functions as an inhibitor with greater selectivity towards prostacyclin (PGI) synthase over thromboxane (TX) synthase. It also acts as a partial agonist at TP receptors. Studies show that at a concentration of 2.8 µM, U-51605 effectively inhibits PGI synthase in human foreskin fibroblasts, while a concentration of 5.6 µM is required to inhibit human platelet TX synthase. Furthermore, U-51605, at up to 1 µM, decreases the release of prostacyclin in SHR aorta triggered by the calcium ionophore A-23187 without impacting TXA2 production, and notably enhances the release of PGE2 and PGF2α.</p>

<p>Bexotegrast (PLN-74809) inhibits αVβ1/αVβ6 integrins, preventing TGF-β1 activation to treat IPF and PSC.</p>

<p>GAT100 is a potent dual-action modulator for CB1R, both covalent NAM and enhancing orthosteric agonist CP55,940 binding.</p>

<p>Hydroxyphenyllactic acid is an antifungal metabolite, fungi such as Lactobacillus sp. SK007.</p>

<p>SOS1-IN-13 inhibits SOS1 (IC50: 6.5 nM) and pERK (327 nM); potential in cancer research.</p>

<p>(–)-G-lactone, a bicyclic γ-lactone, serves as a chiral synthon for prostaglandin and a building block. It is formed through an asymmetric Baeyer-Villiger oxidation reaction. Additionally, (–)-G-lactone has been utilized in the synthesis of HIV-1 protease inhibitors.</p>

<p>Antitumor agent-66 (Compound 4) is a derivative of (-)-cleistenolide, showcasing potential as a research tool for cancer diseases [1].</p>

<p>Onchidal is a key lipid-soluble defense compound from Onchidella binneyi's secretion for chemical protection.</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>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>M4K2163 dihydrochloride, a potent and selective activin receptor-like kinase-2 (ALK2) inhibitor that is permeable to the blood-brain barrier (BBB), has an IC50 of 19 nM. This compound is useful in diffuse intrinsic pontine glioma (DIPG) research [1] [2].</p>

<p>ICMT-IN-50 (compound 3) serves as an inhibitor of ICMT with an IC50 value of 0.31 µM [1].</p>

<p>RO 23-6152, a new calcium antagonist, can inhibit platelet aggregation in vitro associated with occlusive coronary thrombus formation.</p>

<p>Compound 6k, also known as Anti-hepatic fibrosis agent 2, is an orally active inhibitor of the COL1A1 enzyme and exerts anti-fibrogenic effects by targeting the</p>

<p>Antiproliferative Agent-41 (Compound 14), classified as indanorine [1], functions as an antiproliferative compound.</p>

<p>N-Linolenoylethanolamine (18:3 NAE), an endocannabinoid, functions as a vanillin receptor (TRPV1) agonist [1].</p>

<p>"1-Lauroyl-2-palmitoyl-rac-glycerol is a diacylglycerol featuring lauric acid (at the sn-1 position) and palmitic acid (at the sn-2 position)."</p>

<p>1-Myristoyl-3-palmitoyl-rac-glycerol, a diacylglycerol, features myristic acid at the \(sn\)-1 position and palmitic acid at the \(sn\)-3 position.</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>