Other Inhibitors

<p>Lamellarin E is an antineoplastic.</p>

<p>1-Palmitoyl-2-arachidoyl-3-oleoyl-rac-glycerol, a triacylglycerol, incorporates palmitic acid, arachidic acid, and oleic acid at the sn-1, sn-2, and sn-3 positions, respectively, and is identified in cod liver oil.</p>

<p>Bharangin is a inhibitor of penicillinase enzyme in E coli.</p>

PF-06456384 is a highly potent and selective NaV1.7 inhibitor with IC50 value of 0.01 nM.

<p>FR-181157, a novel prostaglandin (PG) mimetic, shows high potency and agonist efficacy at the IP receptor and has good bioavailability.</p>

<p>Siramesine Fumarate, a sigma receptor agonist, is used potentially for the treatment of generalized anxiety disorder.</p>

<p>DosatiLink-2 is an inhibitor of the Abelson murine leukemia (ABL) enzyme [1].</p>

<p>ICI 200355 is an inhibitor of human neutrophil elastase.</p>

<p>gamma-Kainylglutamic acid is a selective amino acid-induced neuroexcitation antagonist.</p>

<p>NBD-09027 is an inhibitor of HIV-1 entry.</p>

<p>Thioquinapiperifil is a type of phosphodiesterase-5 (PDE-5) inhibitor found in dietary supplements.</p>

<p>16-phenyl tetranor Prostaglandin E2 is an active molecule that can be used in life science related research. The CAS number of 16-phenyl tetranor Prostaglandin E2 is 38315-44-5.</p>

<p>ACT-280778 is a potent L/T calcium channel blocker.</p>

<p>RIOK2-IN-1 (com 4) is a selective RIOK2 inhibitor with a Kd of 150 nM, though it demonstrates low cellular activity with an IC50 of 14,600 nM.</p>

<p>A 69992 is an HIV anti-infective nucleoside.</p>

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

<p>LY 106737 is opioid antagonist in the class of phenylpiperidine.</p>

<p>6-Azidohexanoic acid, a six-carbon saturated fatty acid featuring an ω-terminal azide group, serves as a versatile linker for bioconjugation via copper(I)-catalyzed cycloaddition reactions (click chemistry). This functionality enables its initial acylation to a compound, forming a derivative that can subsequently be conjugated to another compound through click chemistry, facilitating the synthesis of complex molecules.</p>

<p>NVP-ABJ688 is the cysteine protease cathepsin K inhibitor.</p>

<p>ICMT-IN-54 (compound 7c), an adamantyl analogue, serves as an ICMT inhibitor with an IC50 value of 12.4 μM, targeting the methylation process facilitated by</p>

<p>GX-395 is a novel Nav1.7 inhibitor.</p>

<p>L-644,698 is a selective agonist of human prostanoid DP receptor.</p>

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

<p>Bioethanomethrin is a biochemical.</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>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>RR-RJW100: potent LRH-1 &amp; SF-1 agonist; studies metabolic disorders, diabetes, liver disease, IBD.</p>

<p>Ent-Entecavir, an enantiomeric impurity of Entecavir (an oral HBV drug), inhibits HBV replication as a reverse transcriptase inhibitor.</p>

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

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

<p>JTT 130 is an agent of hypolipidemic. It inhibits microsomal triglyceride transfer protein.</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>PPARγ agonist 7 (Compound 3a) is a highly potent and selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ).</p>

<p>CB 168 is a potent selective aminoacylaminoaryl tetrazole inhibitor targeting isoleucine tRNA synthetase (IleRS).</p>

<p>L-739943 is a growth hormone secretagogue.</p>

<p>Compound 17b, an amino alcohol-quinoline, targets Pf3D7 (IC50: 14.9 nM) and PfW2 (IC50: 11 nM) with selectivity index &gt;770.</p>

<p>SSAO/VAP-1 inhibitor 1 regulates glucose transport and may reduce inflammation, potential for diabetes and inflammatory disease research.</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>

5-Methyldihydrofolate is the primary biologically active form of folate used for DNA reproduction, the cysteine cycle, and the regulation of homocysteine.

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

<p>T-0201 (TA 0201): Potent, long-acting, oral selective ETA antagonist; blocks ET-1-induced contraction in rabbit arteries.</p>

<p>Eltrombopag (LGD-4665, GSK2285921, SB559448) is an oral TPO receptor agonist for thrombocytopenia treatment.</p>

<p>PARP7-probe-1: biotinylated, chemiluminescent PARP7 active site probe for research use.</p>

<p>Cis-indatraline hydrochloride (cis-Lu 19-005) is an active compound utilized in the research of neurodegenerative diseases [1].</p>

<p>1-Palmitoyl-3-linolenoyl-rac-glycerol, a diacylglycerol with palmitic acid and α-linolenic acid at the sn-1 and sn-3 positions respectively, is present in both the peel and pulp of unripe Dwarf Cavendish bananas.</p>

<p>PCSK9-IN-20 (Compound 3i) is a PCSK9 inhibitor exhibiting an IC50 value of 3.96 µM, shown to reduce PCSK9 and enhance LDLR protein levels in vitro [1].</p>

<p>DC 015 is a novel potent and selective alpha 1-adrenoceptor antagonist.</p>

<p>ZH8659 is a Gq agonist targeting the trace amine-associated receptor 1 (TAAR1) and has potential applications in schizophrenia research [1].</p>

<p>18-Carboxy dinor Leukotriene B4 (18-carboxy dinor LTB4) represents a β-oxidation metabolite of Leukotriene B4 (LTB4). Initially, LTB4 is metabolized in the liver to 20-carboxy LTB4, which subsequently undergoes β-oxidation to form 18-carboxy dinor LTB4.</p>

<p>3-Hydroxy Undecanoic Acid Methyl Ester, a hydroxylated fatty acid methyl ester, is present in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers synthesized by P. oleovorans, P. putida, and D. tsuruhatensis [Matreya, LLC. Catalog No. 1730].</p>

<p>(R)-BDP9066 blocks MRCK to curb cancer cell spread, aiding research on diseases like cancer.</p>

<p>11(Z)-Docosenoic acid, a 22-carbon monounsaturated fatty acid, is identified in fish oil.</p>

<p>5-Oxo Leukotriene B4 (5-oxo LTB4) serves as an intermediate metabolite in the production of 12-oxo LTB4.</p>

<p>CYT296 is a chromatin de-condensation agent that enhances the efficiency of induced pluripotent stem cell (iPSC) generation mediated by defined factors (OSKM)</p>

<p>1,2,3-Trimyristoleoyl glycerol, a triacylglycerol featuring myristoleic acid at the sn-1, sn-2, and sn-3 positions, is detected in Idiazabal cheese.</p>

<p>Urocortin II, a neuropeptide hormone within the corticotropin-releasing factor (CRF) family—which comprises mammalian CRF, urocortin I, urocortin III, frog sauvagine, and piscine urotensin I—displays 34, 43, and 37-40% sequence homology with rat and human CRF, human urocortin I, and human urocortin III, respectively. This compound enhances rabbit ventricular myocyte shortening and relaxation in both a time- and concentration-dependent manner. In vivo studies reveal that urocortin II lowers arterial blood pressure in both normotensive and spontaneously hypertensive rats through peripheral CRF2 receptor agonism, inducing dose-dependent tachycardia and hypotension at doses of 3 and 30 pmol/kg. Additionally, it mitigates the visceral pain response to colorectal distension at 10 and 20 μg/kg in conscious rats and delays gastric emptying in mice.</p>

<p>1-Arachidoyl-2-palmitoyl-3-oleoyl-rac-glycerol, a triacylglycerol, incorporates arachidic, palmitic, and oleic acids at the sn-1, sn-2, and sn-3 positions, respectively. It is present in butterfat and exhibits elevated liver levels in Plin5-overexpressing mice subjected to a high-fat diet.</p>

<p>Indomethacin acyl glucuronide, a metabolite of the COX inhibitor indomethacin (1), embodies an essential byproduct formed during the metabolic processing of indomethacin.</p>

<p>ICMT-IN-8 (compound 30) serves as an inhibitor of ICMT, exhibiting an IC50 value of 0.652 μM [1].</p>

<p>N3-TEMPO, a click chemistry reagent featuring an azide group, exhibits significant potential in facilitating connections among nucleic acids, lipids, proteins, and various molecules. Its application across numerous research domains is attributed to advantageous traits such as high yield, high specificity, and simplicity [1].</p>

<p>Compound CMC23, an FPR2 agonist, mitigates lactate dehydrogenase release in LPS-stimulated cultures and reduces pro-inflammatory IL-1β and IL-6 levels.</p>

<p>17-Hydroxyheptadecanoic acid, a hydroxylated fatty acid identified in aeolian particles from the Frioul Islands and the outer bark of E. globulus, serves in the synthesis of diverse macrocyclic lactones. [Matreya, LLC. Catalog No. 1760]</p>

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

<p>Chloramine-T serves as a versatile reagent in numerous synthetic procedures, including aminohydroxylation, allylic amination, as a nitrogen source in aziridination reactions of alkenes and olefins, and for the deprotection of thio groups in sulfur-containing molecules. Additionally, it plays a role in the synthesis of Factor Xa inhibitors. At a concentration of 0.2% w/v, Chloramine-T acts as an effective antiseptic agent with bactericidal properties against S. epidermidis, S. aureus, E. faecalis, E. coli, P. mirabilis, and E. cloacae.</p>

<p>Palmitoleic acid alkyne, an ω-terminal alkyne derivative of palmitoleic acid, facilitates click chemistry applications. This compound has played a crucial role in examining protein palmitoylation processes. Specifically, the cis form of palmitoleic acid alkyne selectively tags wild-type Wnt3a protein within mouse fibroblast L-cells expressing Wnt3a and its secretion in conditioned media, distinguishing itself from the trans form and proving ineffective against the S209A mutant Wnt3a.</p>

<p>Hydroxy darunavir, a metabolite of the HIV-1 protease inhibitor darunavir, is generated through isobutyl aliphatic hydroxylation of darunavir.</p>

<p>15(R)-Prostaglandin E2, the C-15 epimer of the more physiologically abundant 15(S)-PGE2 (sc-201225) isomer, is produced mainly from arachidonic acid (sc-200770) via the action of COX and PGES enzymes. Present in nearly all cell types, PGE2 interacts with four distinct receptors, EP1 to EP4, leading to a wide range of biological effects. However, 15(R)-Prostaglandin E2 exhibits significantly lower efficacy in most biological assays compared to its 15(S) counterpart. Notably, acid catalyzed epimerization can transform 15(R)-Prostaglandin E2 into the more active 15(S)-Prostaglandin E2 form.</p>

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

<p>PPO-IN-2 is a protoporphyrinogen IX oxidase inhibitor, exhibiting a Ki value of 16 nM [1].</p>

<p>Bidisomide (SC40230) is an agent of class I antiarrhythmic.</p>

<p>RXFP1 receptor agonist-6 (Example 7) serves as an agonist for the RXFP1 receptor and effectively suppresses cAMP production in HEK293 cells that stably express</p>

<p>JTT 551: Selective PTP1B inhibitor for type 2 diabetes research; Ki=0.22μM for PTP1B, 9.3μM for TCPTP.</p>

<p>14-Pentadecenoic acid, a 15-carbon long-chain fatty acid with an alkene functional group on the terminal carbon of its aliphatic tail, has been observed to undergo oxidation due to the growth of M. cerificans at the expense of the parent alkene. This compound is utilized in the creation of fibrous scaffold biomaterials for tissue engineering purposes and in constructing metallomesogenic side-chain polymers for coating capillary columns in gas chromatography applications.</p>

<p>7-Keto-25-hydroxy Cholesterol, an oxysterol and proposed metabolite of 7-keto cholesterol and 7-dehydro cholesterol, binds to and activates Smoothened (Smo) at the conserved extracellular cysteine-rich domain (CRD) in a reporter assay. Additionally, it enhances the number of EGF high affinity binding sites in normal rat kidney (NRK) cells.</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>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>DIOA acts as a potent antagonist of acid-sensitive outwardly rectifying (ASOR) anion channels [1].</p>

<p>L 681176 is an inhibitor of the angiotensin-converting enzyme.</p>

<p>Eicosapentaenoic acid (EPA) is metabolized into epoxyeicosatetraenoic acids (EpETE) by multiple cytochrome P450 isoforms. The predominant compound of this epoxygenase pathway, (±)17(18)-EpETE, induces relaxation in vascular and airway smooth muscles through its action on large conductance Ca2+-activated K+ (BKCa) channels, specifically by binding to the BKα channel subunits. Another notable epoxygenase pathway derivative, (±)11(12)-EpETE, also generated from EPA via CYP450 activity in both in vitro and in vivo studies, has biological and physiological roles that are yet to be fully elucidated.</p>

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

<p>Activated A Subunit is instrumental in synthesizing exon skipping oligomer conjugates, which are designed to specifically pair with chosen sequences within the</p>

<p>MNG-14a, an amphiphilic compound, facilitates the isolation and determination of both function and structure of membrane proteins [1].</p>

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

<p>Therapeutic Agent-1, a heteroaryl compound, serves as an enzyme replacement therapy to enhance glucocerebrosidase activity in the treatment of Gaucher disease [</p>

<p>Mal-GGG-Bal-NHS ester, an ADC linker, facilitates the synthesis of antibody-drug conjugates (ADCs) [1].</p>

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

<p>Neurodegenerative Disorder-Targeting Compound 1 is an inhibitor of calpain [1].</p>

<p>Bicuculline methobromide: GABAA antagonist, IC50=3μM, induces convulsions, used in epilepsy research.</p>

<p>Potassium Channel Activator 1 aids treatment of ADHD, schizophrenia, and mood disorders by targeting the dopaminergic system.</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>C.I. Vat Black 27 is a black dye.</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>TRPV2-selective blocker 1 (compound IV2-1) is a selective inhibitor of the TRPV2 channel, exhibiting an IC50 value of 6.3 μM.</p>

<p>hDDAH-1-IN-2 is an orally active human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1) inhibitor.</p>

<p>7-Hydroxy Etodolac, an inactive metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor etodolac, serves no active function in the drug's pharmacological effects.</p>

<p>METTL3-IN-5 (Compound 13) serves as an inhibitor of METTL3 and demonstrates efficacy in suppressing MOLM-13 cell growth with an IC50 of less than 2 μM.</p>

<p>Eprinomectin B1a, composing over 90% of the antiparasitic agent eprinomectin, is a primary component alongside eprinomectin B1b, which constitutes less than 10%. This compound is part of the avermectin family, used as insecticides and anthelmintics.</p>

<p>Sterculic acid methyl ester, an ester derivative of sterculic acid known for inhibiting Δ9 desaturase, has been found to adversely affect and exhibit toxicity towards R. opacus bacteria at a concentration of 0.75 mM. It not only hampers bacterial growth but also modifies fatty acid composition by reducing stearate and oleate levels, increasing the palmitate ratio, and decreasing overall fatty acid content at 0.25 or 0.5 mM concentrations. Additionally, at 50 ppm, Sterculic acid methyl ester enhances the tumor growth-promoting effects of aflatoxin Q1 in rainbow trout, indicating a synergistic interaction between the two compounds. [Matreya, LLC. Catalog No. 1236]</p>

<p>Vadaclidine is an orally acting antinociceptive muscarinic agonist.</p>

<p>PDE7-IN-3 (Example 2) serves as an inhibitor of phosphodiesterase PDE7 and exhibits potential analgesic properties.</p>

<p>(±)-N-desmethyl Venlafaxine, a minor active metabolite of venlafaxine, serves as a selective norepinephrine and serotonin reuptake inhibitor (SNRI). Generated through the metabolization by the cytochrome P450 (CYP) isoform CYP3A4, it exhibits reuptake inhibition of norepinephrine and serotonin in rat synaptosome preparations, demonstrated by IC50 values of 4.7 and 1.6 µM, respectively. Clinically, it has been shown to counteract reserpine-induced hypothermia in mice, displaying efficacy at a minimum effective dose (MED) of 10 mg/kg.</p>

<p>Y-27152 is a prodrug of the KATP (Kir6) channel opener Y-26763 and is a long-acting K+ channel opener.</p>

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

<p>OfChi-h-IN-1 is a potent inhibitor of OfChi-h, exhibiting a K i value of 0.33 μM.</p>