Other Inhibitors

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

<p>(±)-Pregabalin-13C3 serves as an internal standard for the quantification of pregabalin via GC- or LC-MS. Pregabalin, classified as an anticonvulsant and analgesic, presents a potential for abuse and misuse. In the United States, (±)-Pregabalin-13C3 is regulated as a Schedule V compound, indicating restricted use mainly for research and forensic purposes.</p>

<p>2-Thiophenecarboxamide, N-(5-(p-aminophenoxy)pentyl)- is a bioactive chemical.</p>

<p>Dityrosine, an oxidation product of protein formed through the intermolecular cross-linking of tyrosyl radicals from the reactive oxygen species (ROS) and tyrosine interaction, is associated with decreased hippocampal expression of NMDA receptor subunits Nr1, Nr2a, and Nr2b when administered intragastrically at 320 µg/kg per day, leading to memory impairments in mice as evidenced by their performance in a novel object recognition test. Additionally, it raises fasting blood glucose levels while reducing plasma insulin levels and the pancreatic expression of insulin synthesis-related genes Ins2, Pdx1, and MafA. Increased dityrosine levels have been positively linked to a range of diseases, including autism spectrum disorder, cataracts, Alzheimer's disease, Parkinson's disease, atherosclerosis, and cystic fibrosis.</p>

<p>1dinor-12-oxo-Phytodienoic acid (dinor-OPDA) serves as an intermediate in the biosynthesis of jasmonic acid from hexadecatrienoic acid, playing a crucial role in the jasmonate pathway in plants. This pathway oxygenates and modifies certain unsaturated fatty acids to produce plant hormones critical for processes such as senescence, flower development, mechanotransduction, and response to herbivory. Additionally, dinor-OPDA can be incorporated into glycerolipids and galactolipids, including specific arabidopsides.</p>

<p>Luminespib (AUY-922) is a 3rd-gen Hsp90 inhibitor, disrupting tumor cell proliferation &amp; oncogenic proteins, raising Hsp72 levels.</p>

<p>12-oxo-9(Z)-Dodecenoic acid, an ω-oxoacid metabolite derived from the ω-6 PUFA linoleic acid and the ω-3 PUFA α-linolenic acid, is synthesized in plants through</p>

<p>Difethialone is an anticoagulant rodenticide and a vitamin K antagonist.</p>

<p>WAY-660222 is an active molecule.</p>

<p>AC-4 is a blocker of photoswitchable TRPV1 channel.</p>

<p>ent-Abacavir, enantiomer of an anti-HIV carbocyclic nucleoside RT inhibitor, is metabolized in the liver, forms active CBV-TP.</p>

<p>N-Formyl-L-histidine demonstrates a binding affinity for histidyl-tRNA synthetase, featuring a K i value of 4.6 μM.</p>

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

<p>13(S)-HOTrE, the 15-lipoxygenase (15-LO) metabolite of linolenic acid, is present in cell membranes and as a cholesteryl ester in atherosclerotic lesions, as well as in the biomembranes of soybeans subjected to 15-LO.</p>

<p>Difluorocyclooctyne-CH2-COOH is a DIFO analogue for live-cell glycan imaging, reacting swiftly with azides sans copper catalysts.</p>

<p>OXA-06 hydrochloride, an ATP-competitive ROCK inhibitor, impedes anchorage-dependent growth and invasion in non-small cell lung cancer cell lines. It effectively inhibits cofilin phosphorylation without inducing apoptosis [1].</p>

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

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

<p>Prostaglandin F2α serinol amide, a serinolamide G protein-coupled receptor, elevates calcium levels in human non-small cell lung cancer cells. Additionally, Prostaglandin F2α functions as a luteinizing hormone in sheep and potentially serves as a nociceptive mediator in the spinal cord [1] [2] [3].</p>

<p>2-Hydroxy Myristic Acid Methyl Ester, a rare hydroxylated fatty acid methyl ester isolated from aquatic microbial sources, experiences a decrease in levels to &lt;1% within these communities following Atradex pesticide exposure at 245 mg/L concentration. [Matreya, LLC. Catalog No. 1704]</p>

<p>SGC agonist 1 is a potent soluble guanylate cyclase (SGC) agonist. SGC agonist 1 is able to increase solubility and has high cell permeability.</p>

<p>Human enteropeptidase-IN-3 is an inhibitor of enteropeptidase activity, characterized by extended duration of inhibition.</p>

<p>SPD 502 is a potential selective AMPA antagonist for epilepsy.</p>

<p>UK 55444 is a potent calcium antagonist.</p>

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

<p>Mdl 27013 is a derivative of methoxysuccinyl-alanyl-alanyl-prolyl-valine.</p>

<p>Rosuvastatin zinc salt (Rosuvastatin zinc), a zinc-infused variant of Rosuvastatin, functions as an HMG-CoA reductase inhibitor, utilized primarily in</p>

<p>PARPYnD: Photoaffinity PARP probe; inhibits PARP2, PARP1, PARP6 (IC50: 6, 38, 230 nM); tags PARP1/2 with N3 fluorescent probe.</p>

<p>3'-O-Methylguanosine-5'-O-triphosphate (3'-O-methyl GTP), a methylated derivative of GTP, serves as a chain termination reagent in synthesizing early RNA</p>

<p>GNE-3476 is an NMDA PAM with low GluN2A efficacy, AMPAR activity, and weak at GluN2B receptors.</p>

<p>(±)5-HETE, a monohydroxy fatty acid, emerges from the non-enzymatic oxidation of arachidonic acid and is one of six such derivatives. Its methyl ester variant exhibits no unique biological activity and serves as a provided standard. This methyl ester can also be present in oxidatively degraded polyunsaturated fatty acid (PUFA) methyl esters.</p>

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

<p>XR9051 Hydrochloride, a potent modulator of P-glycoprotein-mediated multidrug resistance (MDR), inhibits the binding of cytotoxics to P-glycoprotein.</p>

<p>Nε-(1-Carboxymethyl)-L-lysine (CML), an advanced glycation end product (AGE), is formed through the oxidative modification of glycated proteins under conditions of oxidative stress.1,2,3 Its levels escalate with age, diabetes, cancer, vascular diseases, and various pathologies associated with oxidative stress.1,4,5 CML interacts with the membrane-bound receptor for AGEs (RAGE), initiating signaling via MAPKs and NF-κB pathways. Conversely, a truncated version of RAGE generates a soluble protein that sequesters CML, thereby diminishing this signaling.6,7</p>

<p>KST012174 is a HIF-1α inhibitor. KST012174 involves in the HIF-1α/p300 protein−protein interaction.</p>

<p>TRPC3/6-IN-2 is a potent inhibitor of TRPC3 and TRPC6, exhibiting IC50 values of 16 nM for TRPC3 and 29.8 nM for TRPC6, respectively [1].</p>

<p>Photosensitizer-2 (compound 1), an organic D-π-A sensitizer, exhibits antitumor properties and potent phototoxicity due to an acrylic acid moiety.</p>

<p>VPC 32183 (S) is an LPA1/LPA3 antagonist with no agonist effect on human/mammal LPA receptors.</p>

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

<p>Kdo Azide is a metabolic labeling reagent and a click chemistry reagent that contains an azide group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkyne-containing molecules. Additionally, it can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.</p>

<p>Sirt2-IN-5 is a potent inhibitor of SIRT2.</p>

<p>5-Demethylnobiletin (2-(3,4-dimethoxyphenyl)-6,7,8-trimethoxychromen-4-one), a distinctive flavonoid present in citrus fruits, shows potential as a chemopreventive agent against human cancers.</p>

<p>9-Keto Fluprostenol Isopropyl Ester, an ester derivative of the FP receptor agonist fluprostenol, undergoes oxidation at carbon 9. This compound serves as a potential prodrug for 9-keto fluprostenol, which may function as an agonist at EP receptors. Additionally, it is considered a possible metabolite of fluprostenol isopropyl ester (travoprost), drawing parallels to the metabolism of latanoprost by 15-hydroxyprostaglandin dehydrogenase observed in monkey cornea. Furthermore, certain F-series prostaglandins, such as 6-keto prostaglandin F1α (PGF1α), undergo conversion to their E-series counterparts in isolated human platelets, highlighting a metabolic pathway of relevance.</p>

<p>CGP 6809: a methylnitrosoureido-sugar derivative active against various mice/rat tumors; promising for bowel/lung cancer trials.</p>

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

<p>ICMT-IN-23 (compound 36) serves as an inhibitor of ICMT, exhibiting a half-maximal inhibitory concentration (IC50) of 0.123 μM [1].</p>

<p>PI5P4Ks-IN-3 (compound 30) is a covalent inhibitor of PI5P4K, exhibiting inhibition constants (IC50s) of 1.34 μM for PI5P4Kα and 9.9 μM for PI5P4Kβ.</p>

<p>OSBP-IN-1 (compound 12), an analogue of Schweinfurthins, selectively targets oxysterol-binding protein (OSBP) and exhibits antitumor activity [1].</p>

<p>1,1'-(Azodicarbonyl)dipiperidine (ADDP) serves as a widely employed reagent in the Mitsunobu reaction, facilitating the condensation between an alcohol and an acidic compound. Moreover, ADDP has found application in synthesizing agonists for the G protein-coupled receptor 120 (GPR120) with potential antidiabetic effects as well as in the creation of triple agonists for peroxisome proliferator-activated receptor α (PPARα), PPARγ, and PPARδ.</p>

<p>L 363851 is a neurokinin B agonist.</p>

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

<p>E7974, a hemiasterlin analog, targets the Vinca domain on tubulin, disrupts microtubules, and inhibits cell division and proliferation.</p>

<p>SARS-CoV-2/MERS Mpro-IN-2 is a potent inhibitor of the main proteases of SARS-CoV-2 and MERS, demonstrating IC50 values of 0.21 and 0.07 µM, respectively.</p>

<p>Necrostatin-1 (Nec-1) (inactive control), an inactive analog of Necrostatin-1, functions as a potent inhibitor of necroptosis [1].</p>

<p>BMS-433771 dihydrochloride hydrate is a potent oral RSV inhibitor, affects groups A &amp; B, with a 20 nM EC50, used in respiratory disease research.</p>

<p>Sunepitron Free Base, a 5-HT1A agonist/α₂-antagonist, halted in Phase III for depression/anxiety.</p>

<p>"1-O-Hexadecyl-2-eicosapentaenoyl-sn-glycero-3-PC is a compound that results from the incorporation of eicosapentaenoic acid (EPA) into lyso-PAF C-16, a process demonstrated in neutrophils from monkeys and humans consuming a diet rich in fish oils. Furthermore, it functions as a precursor for PAF C-16 synthesis via the remodeling pathway."</p>

<p>Spirotetramat is an insecticide that demonstrates efficacy against C. pyrinymphs in vitro (LC50= 6.51-12.53 mg AI/L) and achieves a 99.2% mortality rate in C. pyrinymphs within European pear (P. communis) fields 15 days post-application at a dosage of 27 g/hectare. Additionally, it reduces embryonic viability and nymph survival in O. insidiosus. Spirotetramat exhibits aquatic toxicity by altering protein levels in organisms, specifically by increasing glutathione peroxidase (GPX) and superoxide dismutase (SOD) levels, decreasing malondialdehyde (MDA) levels, and causing lethality in Chinese toad (B. gargarizans) tadpoles (LC50= 6.98 mg/L). Its formulations are utilized in agricultural insect control. Spirotetramat is marketed exclusively for research and analytical applications, formulated for controlled laboratory settings without the availability of bulk sizes.</p>

<p>MFN2 agonist-1 (B-A/l) effectively induces mitochondrial fusion in cells deficient in mitofusin 2 (MFN2).</p>

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

<p>WAY-606376 具有潜在的抗肿瘤活性，可用于研究免疫疾病。</p>

<p>10(Z)-Pentadecenoic acid methyl ester is the methyl ester derivative of the fatty acid known as 10(Z)-pentadecenoic acid. This compound serves as a standard for quantifying pentadecenoic acid in vernix caseosa, as indicated by Matreya, LLC. Catalog No. 1210.</p>

<p>2-C-Methylene-myo-inositol oxide (NSC 45109), an inositol derivative, promotes pseudohyphal growth in Saccharomyces species [1].</p>

<p>Rohitukine: anticancer, modulates apoptosis, antiadipogenic, antidyslipidemic, gastroprotective, antifertility, antileishmanial.</p>

<p>α-HNJNAc is a potent, competitive hexosaminidases inhibitor that does not interfer with other glycosidases [1].</p>

<p>BODIPY-Palmitate, a fluorescent derivative of palmitic acid, exhibits excitation and emission maxima at 488 nm and 508 nm, respectively. It is employed in the monitoring of fatty acid uptake and metabolism within cultured cells.</p>

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

<p>KH-4-43, an inhibitor of the E3 CRL4 ligase complex, demonstrates anticancer activity by targeting the core of the E3 CRL4. It exhibits a binding affinity (Kd) of 83 nM to the E3 ROC1-CUL4A CTD and 9.4 μM to the closely related ROC1-CUL1 CTD [1].</p>

<p>KVI-020: oral Kv1.5 blocker (IC50: 480nM), hERG inhibitor (IC50: 15100nM), potent antiarrhythmic for AF studies.</p>

<p>CP-432 (CP-734432) is an EP4 prostaglandin agonist for the treatment of glaucoma and ocular hypertension.</p>

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

<p>11-Keto Fluprostenol, a potent analog of prostaglandin F2α (PGF2α), primarily interacts with the FP receptor. It is a structurally modified derivative of prostaglandin D2 (PGD2) designed to enhance its potency and extend its half-life. The compound is produced by oxidizing fluprostenol at the C-11 position, which results in 11-keto fluprostenol. This modification allows 11-keto Fluprostenol to exhibit moderate affinity for the CRTH2/DP2 receptor, though it shows negligible activity at the DP1 receptor, distinguishing its action from that of PGD2.</p>

<p>Dim16, a dual inhibitor of PCSK9/HMG-CoAR, demonstrates potent activity with an IC50 of 19 nM against PCSK9 and significantly impedes PCSK9-LDLR interaction</p>

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

<p>TRK-IN-17 is a potent TRK inhibitor with potential for cancer research, targeting neurotrophic factor-activated kinases. See WO2021148807A1 for details.</p>

<p>1-O-Hexadecyl-2-arachidonoyl-sn-glycero-3-PC undergoes acylation through the action of CoA-independent transacylase, transforming lyso-PAF C-16 into this compound. It serves as the predominant precursor in the biosynthesis of PAF C-16 via the remodeling pathway.</p>

<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>

<p>Atherospermidine is a smooth muscle relaxant aporphines from Artabotrys maingayi.</p>

<p>S-Octylglutathione is a competitive inhibitor of glutathione S-transferase (GST) [1].</p>

<p>20-HETE Inhibitor-1 (Comp 83) serves as an inhibitor of 20-HETE formation [1].</p>

<p>ICMT-IN-46 (compound 25) is a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an IC50 value of 0.556 μM [1].</p>

<p>Cyclic Phosphatidic Acids (cPAs) are naturally occurring lysophosphatidic acid (LPA) analogs, characterized by a 5-membered ring formed between the sn-2 hydroxy group and the sn-3 phosphate. Carba-derivatives of cPA (ccPA) modify the sn-2 (2-ccPA) or sn-3 (3-ccPA) linkage, hindering the conversion of cPA into LPA. Oleoyl 3-Carbacyclic Phosphatidic Acid (3-ccPA 18:1) incorporates the 18:1 fatty acid oleate at the sn-1 position on the glycerol backbone, acting as a cyclic LPA analog. This compound, at a concentration of 25 μM, blocks MM1 cells' transcellular migration through mesothelial cell monolayers induced by fetal bovine serum (by 90.1%) or LPA (by 99.9%), without impeding cell proliferation. Additionally, 3-ccPA 18:1, in the 0.1-1.0 μM range, notably suppresses autotaxin, which plays a vital role in various cancer cell behaviors including survival, growth, migration, invasion, and metastasis.</p>

<p>Pecavaptan is a vasopressin receptor antagonist.</p>

<p>RTI-371 is a potent and selective dopamine reuptake inhibitor in vitro.</p>

<p>XL-418 is an oral inhibitor of AKT and p70S6K, aiming to induce cancer cell apoptosis and block protein synthesis.</p>

<p>15(S)-Fluprostenol isopropyl ester, an isomer of the prostaglandin F2α analog, fluprostenol isopropyl ester, serves as a possible prodrug to 15(S)-fluprostenol. It has the potential to act as an agonist at FP receptors, albeit with lower potency compared to the 15(R) epimer and the FP receptor agonist, fluprostenol. Additionally, it may be present as a potential impurity in commercial formulations of fluprostenol isopropyl ester.</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>KRM-II-81 is a GABAA receptor ligand with enhanced anxiolytic effects in mice and rats.</p>

<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>

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

<p>L-Biotin, or simply biotin, is a water-soluble vitamin crucial for carboxylation reactions in various enzymes.</p>

<p>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]</p>

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

<p>All-cis-4,7,10,13,16-Docosapentaenoic acid (all-cis-4,7,10,13,16-DPA) methyl ester, also known as Osbond acid, is an isomer of DPA and a more lipid-soluble variant of the free acid, primarily found in fish oils as an ω-3, 22-carbon fatty acid. Despite being an ω-6 fatty acid synthesized through the elongation and desaturation of arachidonic acid, its levels can decrease due to fatty acid desaturase syndrome, potentially impacting development. Additionally, increased expression of hepatic elongation of very long fatty acids protein 6 and elevated levels of very long-chain fatty acids, including all-cis-4,7,10,13,16-DPA, are indicative of nonalcoholic steatohepatitis, a condition that precedes hepatocellular carcinoma.</p>

<p>EZH2-IN-8 inhibits EZH2, potentially useful in cancer research, as per patent WO2021129629A1.</p>

<p>IM-491 is a TNF-alpha converting enzyme inhibitor.</p>

<p>Riboxin (IDP), an orally administered purine derivative known as hypoxanthine riboside, exhibits antihypoxic and antihyperthermic effects.</p>

<p>BO-1158 is an antibacteria agent.</p>

<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>

<p>CS640 is a selective calmodulin-dependent kinase inhibitor, targeting multiple isoforms, namely CaMK1D, CaMK1B, CaMK1A, CaMK1G, PIP5K1C, MEK5, RIPK4, and MLK3,</p>

<p>L-826141 is an inhibitor of phosphodiesterase 4.</p>

<p>C6 Biotin Glucosylceramide (d18:1/6:0) is a lipid molecule that can be used in life science related research. The CAS number of C6 Biotin Glucosylceramide (d18:1/6:0) is 2692623-22-4.</p>

<p>L 699333 is an effective inhibitor of 5-lipoxygenase.</p>

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