Other Inhibitors

<p>Alpertine HCl is a small molecule compound with anti-neuropathic properties.</p>

<p>PI5P4Kα-IN-1 (Compound 13) is a phosphatidylinositol 5-phosphate 4-kinase (PI5P4K) inhibitor, displaying IC50 values of 2 μM for PI5P4Kα and 9.4 μM for PI5P4Kβ</p>

<p>PBR28, a TSPO modulator, holds potential for preventative research in Pulmonary Arterial Hypertension (PAH) and is instrumental in brain positron emission</p>

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

<p>Dimethylamiloride is a specific inhibitor of antiporters [1].</p>

<p>Hydroxy celecoxib, an inactive metabolite of celecoxib, is synthesized through the metabolism of celecoxib by cytochrome P450 (CYP) isoforms CYP2C9, CYP3A4, and CYP2D6 in human liver microsomes.</p>

<p>RS-93427-007 is an orally active stable mimetic agent of prostacyclin for the study of mechanisms of atherogenesis.</p>

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

<p>GGTI-2133: potent GGTase I inhibitor, IC50=38 nM; blocks inflammatory cell invasion in mice asthma.</p>

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

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

<p>1-Palmitoyl-3-lauroyl-rac-glycerol, a diacylglycerol, features palmitic acid and lauric acid at the sn-1 and sn-3 positions, respectively.</p>

<p>FK-352 is a pyrazolopyridine derivative and adenosine-1 receptor antagonist.</p>

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

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

<p>Dibutylephrine is a sympathomimetic agent.</p>

<p>U 19052 is a Leukotriene D4 antagonist.</p>

<p>BMS-561392 formate, the formate derivative of BMS-561392, functions as a TNF alpha-converting enzyme (TACE) inhibitor and an ADAM17 blocker. It is utilized in the research of inflammatory bowel disease [1] [2].</p>

<p>DGKζ-IN-3 is an inhibitor of diacylglycerol kinase zeta (DGK-ζ), employed in the treatment of both liquid and solid cancers, as well as other diseases regulated</p>

<p>17β-Hydroxywortmannin is an orally active phosphatidylinositol-3-kinase (PI-3-kinase) inhibitor, exhibiting an IC50 of 0.5 nM and notably suppresses osteoclast resorption at an IC50 of 10 nM. Additionally, it demonstrates antitumor activity.</p>

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

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

<p>HQ005, a potent CCNK degrader, exhibits an impressive DC50 value of 0.041 µM and functions as a molecular-glue degrader.</p>

<p>Phenylephrine glucuronide, a metabolite of phenylephrine (an α1A-adrenergic receptor agonist), is produced through metabolic processes.</p>

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

<p>ddATP is a dideoxynucleotide, used as a chain extension inhibitor for DNA polymerase, and used for DNA sequencing by the Sanger method.</p>

<p>Sontigidomide (Compound 5) is an antineoplastic agent that demonstrates over 80% inhibition of MOLM-13 cell proliferation at a concentration of 1 μM after 3</p>

<p>9(Z),11(Z)-Conjugated Linoleic Acid Methyl Ester serves as a standard in the quantification of conjugated linoleic acid methyl esters via GC-MS, according to Matreya, LLC. Catalog No. 1256.</p>

<p>WAY-608106 is an active molecule.</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>Pecavaptan is a vasopressin receptor antagonist.</p>

<p>ICMT-IN-14 (compound 50) serves as an inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting potent activity with an IC50 of 0.025 μM [1].</p>

<p>ONO-8539 is a prostanoid EP1 receptor antagonist.</p>

<p>ZM 260384 is a potassium channel opener.</p>

<p>GTPγS tetralithium (Guanosine 5'-[γ-thio]triphosphate tetralithium) is a G-protein activator and a non-hydrolyzable GTP analog.</p>

<p>ICMT-IN-52 (compound 44) serves as an ICMT inhibitor with an IC50 value of 0.052 μM [1].</p>

<p>PDE12-IN-3 is an inhibitor of phosphodiesterase 12 (PDE12) (pXC50 of 7.68),with antiviral activity.</p>

<p>Valyl-glycyl-arginine-4-nitroanilide is a tissue plasminogen activator.</p>

<p>STING agonist D61 is a compound that activates the stimulator of interferon genes (STING), leading to the induction of IFN3-inducible secreted alkaline</p>

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

<p>PTC258 is a specific, orally active modulator of the splicing of the Elongator complex protein 1 gene (ELP1), enhancing its expression both in vitro and in vivo</p>

<p>GPR3 agonist-2 (compound 32) is a potent full agonist of the G protein-coupled receptor 3 (GPR3), exhibiting an IC50 value of 260 nM [1].</p>

<p>BMS-538203 is a novel HIV integrase inhibitor.</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>"(1R,4R)-N-desmethyl Sertraline, a metabolite of the selective serotonin reuptake inhibitor (SSRI) sertraline, plays a key role in its pharmacological effects."</p>

<p>Nivocasan (GS-9450/LB-84451), a caspase-inhibitor, reduces ALT in NASH, shows hepatoprotective effects in fibrosis models.</p>

<p>DDR1/2 Inhibitor-2 (Example 31) serves as an inhibitor of DDR1/DDR2, exhibiting IC50 values below 100 nM.</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>C8 Ceramine (d18:1/8:0) is a lipid molecule that can be used in life science related research. The CAS number of C8 Ceramine (d18:1/8:0) is 170926-06-4.</p>

<p>(+)-Leucocyanidin, an isoform of leucocyanidin and potent anti-ulcerogenic agent, has been extracted from Litchi chinensis.</p>

<p>Methotrexate-alpha glutamate: treats cancer, autoimmune disorders, ectopic pregnancy, medical abortions; chemotherapy, immunosuppressant.</p>

<p>XR3054 is a farnesyl protein transferase inhibitor that blocks proliferation in certain cancer cells, not dependent on ras mutation status.</p>

<p>4-Oxo-2-nonanal (4-ONE) is a lipid peroxidation product that actively modifies histidine and lysine residues in proteins, leading to protein cross-linking, and alters 2'-deoxyguanosine, indicating its role in mutagenesis and carcinogenesis. 4-ONE alkyne, an alkyne-tagged electrophile, serves as a probe for isolating and identifying lipid peroxidation reaction products through click chemistry.</p>

<p>RPR203494 is a pyrimidine analogue of the p38 inhibitor RPR200765A with an improved in vitro potency.</p>

<p>YUN90389 (CAS#1673590-38-9) is the first pparα/δ dual antagonist, as reported in 2019.</p>

<p>Activated DPG subunit facilitates the synthesis of exon jumping oligomer conjugates targeting specific sites within the human anti-muscular atrophy protein gene</p>

<p>AM-156 is a bio-active chemical.</p>

<p>DI-591: High-affinity DCN1-UBC12 inhibitor; permeates cells; Ki: DCN1 - 12 nM, DCN2 - 10.4 nM; doesn't bind DCN3-5.</p>

<p>Metabutoxycaine, a local anesthetic [1], serves to numb specific areas of the body.</p>

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

<p>Sphingomyelin (chicken egg) (SMs (chicken egg)) is a sphingolipid from eggs and is a major component of the plasma membrane.</p>

<p>RXFP1 receptor agonist-3 (Example 223) is an agonist of the RXFP1 receptor that inhibits cyclic AMP (cAMP) production in HEK293 cells stably expressing human</p>

<p>Fazamorexant (YZJ-1139) is a powerful orexin receptor antagonist effective for insomnia research.</p>

<p>Flovagatran sodium, a thrombin inhibitor, is used potentially for the treatment of thrombosis.</p>

<p>Spexin-2 (53-70), human, mouse, rat (NPQ 53-70), is a biologically active, non-amidated peptide derived from the prohormone proNPQ, conserved across mammalian</p>

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

<p>PF-06807656 remains effective against ROMK with N171D mutation, unlike other inhibitors; it has an IC50 of 160 nM for Tl+ flux.</p>

<p>Wieland-Gumlich aldehyde is an indoline derived by chemical degradation from strychnine.</p>

<p>Cyclic HPMPC: Potent antiviral, raises O2 in mice with lethal vaccinia, lowers guinea pig CMV replication.</p>

<p>VGD020 inhibits CD4/sortilin, reduces sortilin &amp; hinders breast cancer stem cell growth.</p>

<p>S 16020-2 is an olivacine derivative, and DNA topoisomerase II inhibitor endowed with a remarkable antitumor activity against various experimental tumors.</p>

<p>3-Hydroxy Stearic acid methyl ester, a hydroxylated fatty acid methyl ester, occurs in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers synthesized by Streptomyces sp. JM3 and is present in trace amounts in M. bijuga fruit. Additionally, it is identified as a chemical scent constituent in the feces of adult wild Iberian wolves (C. lupus signatus). [Matreya, LLC. Catalog No. 1744]</p>

<p>JAK2 inhibitor; IC50=397 nM; hampers STAT3/5 phosphorylation; curbs growth and triggers apoptosis in JAK2V617F+ cells.</p>

<p>8(R),11(S)-DiHODE, a fungal oxylipin identified in various Aspergillus species, is synthesized through the isomerization of an 8(R)-HpODE intermediate during linoleic acid oxidation.</p>

<p>FR-226928 is a potent antagonist of human neuropeptide Y Y5 receptors.</p>

<p>Nurr1 inverse agonist-1 inhibits Nurr1 transcription by over 90%, targeting monomers, dopaminergic neuron regulation and neurodegenerative diseases.</p>

<p>Cintirorgon (LYC-55716) is an oral RORgamma agonist with immunomodulatory and anticancer effects.</p>

<p>1-Aminodecylidenebis-phosphonic acid, with its potent inhibitory effect on acid sphingomyelinase (IC50= 20 nM), shows selectivity by being less effective against neutral sphingomyelinase (IC50= &gt;100 μM). Additionally, it entirely prevents dexamethasone-induced apoptosis in HepG2 cells.</p>

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

<p>1-Stearoyl-3-arachidoyl-rac-glycerol is a diacylglycerol with stearic acid at the sn-1 position and arachidic acid at the sn-3 position.</p>

<p>ARRY-403 (AMG-151) is an oral glucokinase activator for type 2 diabetes with an EC50 of 79 nM and favorable drug properties.</p>

<p>Adapiprazine is prochlorperazine that works as an anesthetic drug.</p>

<p>Thymidine-5’-O-(α,β-methylene)diphosphate (TMP-CP), a hydrolytically stable derivative of TDP, functions as an inhibitor of thymidine kinase (Ki = 23 µM).</p>

<p>E1R is a positive sigma-1 receptor (Sig1R PAM) allosteric modulator. It has a cognition-enhancing activity.</p>

<p>WAY-309236 is an active compound utilized in researching amyloid diseases and synucleinopathies.</p>

<p>PD-321852, a Chk1 inhibitor, boosts gemcitabine's effect in pancreatic cancer cells, varying from minimal in Panc1 to &gt;30-fold in MiaPaCa2.</p>

<p>Cy5.5 DBCO, a click chemistry reagent, features a cycloalkyne group and serves as a linker for the Cyanine5.5 fluorophore. Its DBCO group facilitates copper-free, biocompatible click chemistry, characterized by rapid reaction kinetics and high stability [1].</p>

<p>Pterostilbene-isothiocyanate (PTER-ITC) demonstrates strong anticancer properties in vitro, particularly disrupting the interaction between β-catenin and TCF-4</p>

<p>C16 (2'(S)-hydroxy) Ceramide (d18:1/16:0) is a lipid molecule that can be used in life science related research. The CAS number of C16 (2'(S)-hydroxy) Ceramide (d18:1/16:0) is 890041-50-6.</p>

<p>17(R)-Resolvin D1 (17(R)-RvD1) is an aspirin-triggered epimer of RvD1 that equivalently inhibits human polymorphonuclear leukocyte migration across the endothelium (EC50= ~30 nM), a precursor to acute inflammation. Unlike RvD1, it resists rapid degradation by eicosanoid oxidoreductases. In a mouse peritonitis model, 17(R)-RvD1 dose-dependently reduces leukocyte infiltration, achieving up to a 35% decrease with a 100 ng dose. Additionally, its methyl ester derivative, designed to enhance its pharmacokinetic and distribution properties as a more lipophilic prodrug, can be converted back into the active acid form by intracellular esterases.</p>

<p>Clazuril, a phenylacetonitrile derivative, treats coccidiosis in poultry by killing Eimeria species.</p>

<p>MK-3901 is a P2X3 antagonist.</p>

<p>NEU-1923 is a potent inhibitor of T. brucei proliferation (EC50= 0.37 μM).</p>

<p>Tridecafluorohexane-1-sulfonic acid potassium salt is a perfluorinated anionic surfactant used in electroplating as a chromium fog inhibitor, a humidifier, and an additive to fluoroprotein foam fire extinguishing agents.</p>

<p>Flucythrinate is an insecticide.</p>

<p>GSK256471 is a selective NK3 antagonist with high affinity for human (PK(I) 8.9) and guinea pig (PK(I) 8.4) receptors, potential schizophrenia treatment.</p>

<p>Oleoyl-L-alpha-lysophosphatidic acid sodium salt is an essential cell membrane biosynthetic metabolite that mediates signal transduction by interacting with G</p>

<p>ASGPR ligand-1 is a compound that targets the asialoglycoprotein receptor (ASGPR) and is utilized in various disease research contexts [1].</p>

<p>Antitumor agent-120 (compound 1), a flavonoid derived from Kudzu root, exhibits negligible inhibitory effects on LNCaP and PC3 cancer cells, with IC50 values</p>

<p>Bimatoprost Serinol Amide (Bima SA), a prostaglandin analog, shows research potential for glaucoma [1].</p>

<p>TBC-3486 is a novel potent inhibitor of integrin α4, being 200-fold more potent in inhibiting α4β1 than α4β7.</p>

<p>PBT434 methanesulfonate is an oral α-synuclein aggregation inhibitor, crosses the blood-brain barrier, and may help treat Parkinson's.</p>

<p>ICMT-IN-12 (compound 78) serves as an ICMT inhibitor, demonstrating an IC50 value of 0.42 μM [1].</p>

<p>AZD-9819 is an inhibitor of human neutrophil elastase for potential treatment of chronic obstructive pulmonary disease (COPD).</p>