Other Inhibitors

<p>AH13205 is an agonist of EP2 prostanoid receptor.</p>

<p>MK-8245 analog is an analog of MK-8245 which is a liver-targeted Inhibitor of Stearoyl-CoA Desaturase (SCD).</p>

<p>AEG40730: A potent, selective IAP inhibitor, induces cIAP1/2 degradation, reduces RIP1 ubiquitination, and depletes XIAP, c-IAP1.</p>

KCA-1490 is an inhibitor of dual PDE3/4.

<p>Z-LVG, an irreversible cysteine protease inhibitor and a tripeptide derivative of cystatin C, serves as an inhibitor of viral replication and is utilized in</p>

<p>(±)9(10)-DiHOME, the diol derivative of (±)9(10)-EpOME—a cytochrome P450-derived epoxide of linoleic acid also known as leukotoxin—is formed through the action of soluble epoxide hydrolase (sEH) in neutrophils. It exhibits toxicity towards Sf21 cells expressing sEH as well as tolacZ-expressing control cells, differing from leukotoxin which only harms sEH-containing cells. Furthermore, combined exposure to 9(10)- and 12(13)-DiHOME leads to cell death in rabbit renal proximal tubule cells by disrupting mitochondrial respiration, and causes lung injury, respiratory distress, and mortality in mice, highlighting its role as a toxic lipid mediator. Specifically, 9(10)-DiHOME has been associated with acute respiratory distress syndrome (ARDS), a severe and often deadly complication in patients with major burns. Elevated levels of this compound have been detected in the bronchoalveolar lavage fluid (BALF) of women, but not men, with chronic obstructive pulmonary disease (COPD), and its levels are also increased in patients with allergic asthma, indicating its significance in respiratory conditions.</p>

<p>WAY-215718 is an active molecule.</p>

<p>FPL-65447 HCl is a D1 agonist for renal/cardiac failures and sepsis treatment.</p>

BPI-9016M, an oral c-Met/AXL inhibitor, curbs growth and spread of lung cancer.

<p>A 56234 is a high-ceiling diuretic.</p>

<p>Zaldaride (free base) is a calmodulin antagonist.</p>

<p>(R)-4-Amino-3-hydroxybutyric acid, also known as (R)-GABOB, acts as a modulator of GABA receptors, specifically binding to both GABAA and GABAB receptors and blocking GABA reuptake in rat brain synaptosomes. Additionally, it serves as a GABAC receptor agonist, triggering currents in patch-clamp assays with Xenopus oocytes that express the human receptor. In vivo studies reveal its capability to suppress electrical discharges in the amygdala in cats undergoing N-amidinobenzamide-triggered seizures, indicating its potential therapeutic application in managing seizure disorders.</p>

<p>C12((±)-2'-hydroxy) dihydro Ceramide (d18:0/12:0) is a lipid molecule that can be used in life science related research. The CAS number of C12((±)-2'-hydroxy) dihydro Ceramide (d18:0/12:0) is 2377379-54-7.</p>

<p>UNC1666 is a dual ATP-competitive small molecule tyrosine kinase inhibitor, which potently diminishes Mer and Flt3 phosphorylation in AML.</p>

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

<p>N,N-dihexyl Sphingosine (d18:1/6:0/6:0) is a lipid molecule that can be used in life science related research. The CAS number of N,N-dihexyl Sphingosine (d18:1/6:0/6:0) is 2377379-53-6.</p>

<p>SAD-448 is a cannabinoid receptor type 1 (CB1) agonist. SAD-448 controls spasticity via action on the peripheral nerve CB1 receptor.</p>

<p>Compound 107 (Compd 11jc) exhibits potent antitumor activity and serves as an effective anticancer agent in the investigation of pulmonary metastatic melanoma [</p>

<p>AZD2716 is an effective selective phospholipase A2 inhibitor for the treatment of coronary artery and cardiovascular disease.</p>

<p>K-8986 is a novel h1-receptor antagonist</p>

<p>BIM 23056 TFA, a potent linear octapeptide antagonist of sst3 and sst5 somatostatin receptors, exhibits inhibition constants (K_i) of 10.8 for sst3 and 5.7 for</p>

<p>10-SAHSA, an endogenous lipid recently discovered, is part of the FAHFAs, a group of branched fatty acid esters of hydroxy fatty acids. It specifically consists of stearic acid esterified to 10-hydroxy stearic acid. Notably, PAHSAs, closely related to 10-SAHSA, are significantly present in the adipose tissue of AG4OX mice that are glucose tolerant due to the overexpression of the Glut4 glucose transporter in their adipose tissue. Similar to other FAHFAs, which are known to improve glucose tolerance, promote insulin secretion, and possess anti-inflammatory properties, 10-SAHSA is considered a potential bioactive lipid with implications for metabolic syndrome and inflammation management.</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>ICMT-IN-31 (compound 68) serves as an ICMT inhibitor, demonstrating significant potency with an IC50 value of 0.0038 μM [1].</p>

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

<p>6-Methoxypurine arabinoside (Ara-m), a potent inhibitor of the varicella-zoster virus (VZV), exhibits 50% inhibitory concentrations (IC50) between 0.5 and 3</p>

<p>PF3845yne is an alkyne analogue of PF-3845 maintaining high potency for FAAH.</p>

<p>Isoacitretin is an oral retinoid effective and can be used to treat psoriasis.</p>

<p>TMV-IN-4, a TMV inhibitor, enhances plant defense and TMV resilience by interacting with helicase, increasing peroxidase and SOD activity.</p>

<p>SARS-CoV-2/MERS Mpro-IN-1 is a potent inhibitor of the main proteases in SARS-CoV-2 and MERS, exhibiting IC50 values of 0.10 and 0.06 µM, respectively.</p>

<p>Limocrocin is an inhibitor of reverse transcriptase.</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>NEU-730, a novel inhibitor of TbrPDEB1, shows modest inhibition of T. brucei proliferation.</p>

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

<p>Des-4-fluorobenzyl Mosapride, the main metabolite of mosapride, acts as a gastroprokinetic agent improving upper gastrointestinal (GI) motility by stimulating the serotonin receptor 4 (5-HT4; EC50= 74.2 nM, in guinea pig ileal longitudinal muscle myenteric plexus). It has been shown to increase colonic motility in dogs, horses, and guinea pigs in vivo. Mosapride, including this metabolite, is utilized in human and veterinary medicine to mitigate post-surgical and Parkinson's-induced constipation.</p>

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

<p>CHI-000-667 can be used in studies about Ras.</p>

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

<p>S-(N-Methylsulfinylbutylthiocarbamoyl)-L-cysteine (SFN-Cys) is an isothiocyanate derivative, functioning as an active metabolite of sulforaphane, a class I and</p>

<p>Maropitant citrate anhydrous is a neurokinin (NK1) receptor antagonist.</p>

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

FTI-276 is an inhibitor of protein farnesyltransferase (PFT) (IC50s: 0.9 and 0.5 nM for Plasmodium falciparum and human).

<p>(R)-FT709 is an active compound utilized in cancer research [1].</p>

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

<p>R-1663 inhibits factor Xa, prolongs clotting, reduces thrombin without affecting bleed time; more effective on peak than ETP.</p>

<p>Dual photoCORM 1 (compound 5), a metal-free, photoactive, dual carbon monoxide releasing molecule (CORM), demonstrates efficient cellular uptake and enables</p>

<p>AtPCO4-IN-1 is a selective AtPCO4 inhibitor, exhibiting an IC50 value of 264.4 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>NEPP-11 is a selective JNK signaling pathway inhibitor.</p>

<p>PSD-506, a muscarinic M2/M3 antagonist, is used potentially for the treatment of overactive bladder, and urinary incontinence.</p>

<p>MET kinase-IN-2, a selective and potent MET kinase inhibitor, demonstrates oral bioavailability and exhibits an IC50 value of 7.4 nM.</p>

<p>NMS-P515 is an effective, orally active, and stereospecific PARP-1 inhibitor (Kd: 16 nM and an IC50: 27 nM (in Hela cells)). It has anti-tumor activity.</p>

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

<p>MNI-caged-L-glutamate, a derivative of glutamate conjugated with a 4-methoxy-7-nitroindolinyl (MNI) photoprotective group, remains pharmacologically inactive at neuronal glutamate receptors at concentrations up to mM. Upon light exposure (300 - 380 nm excitation), it rapidly releases L-glutamate by cleaving the MNI group within submicroseconds. This characteristic enables the investigation of fast synaptic glutamate receptor mechanisms in situ.</p>

<p>1,3-Dilinoleoyl glycerol, a diacylglycerol, incorporates linoelaidic acid at both the sn-1 and sn-3 positions. This compound emerges from the collision-induced decomposition of synthetic linoleic ammoniated triglycerides.</p>

<p>Oxamniquine is an effective compound for the treatment of schistosomiasis.</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>L-Biotin, or simply biotin, is a water-soluble vitamin crucial for carboxylation reactions in various enzymes.</p>

<p>Flesinoxan HCl is the salt form of Flesinoxan, which is a selective 5-HT1A receptor agonist.</p>

<p>N1-Azido-spermine trihydrochloride (Spermine[HHHN3]) is a click chemistry agent featuring an azide group.</p>

<p>GCC-4401C free base is a factor Xa inhibitor similar to rivaroxaban that is currently under development for venous thromboembolic disease (VTE).</p>

<p>LG 83-6-05 is a novel kind of sodium channel blocking agent.</p>

<p>NVP-BHS345 is a dual inhibitor of TORC1 and TORC2.</p>

<p>ICI-185282 is a potent thromboxane receptor antagonist.</p>

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

E2072 is a potent and selective thiol-based Glutamate Carboxypeptidase II (GCP-II) inhibitor.

<p>3-Keto Sphinganine (d12:0) is a short-chain analog of 3-keto sphinganine (d18:0), which typically possesses a C18 chain length. The latter is a lyso-sphingolipid synthesized through the condensation of L-serine and palmitoyl-CoA mediated by the enzyme serine palmitoyl transferase (SPT). A deficiency in Vitamin K deactivates SPT, leading to a reduced synthesis of 3-keto sphinganine among other sphingolipids. [Matreya, LLC. Catalog No. 1893]</p>

<p>KUNG94 selectively inhibits Grp94 at 8 nM IC50, a 90 kDa Hsp90 variant in the endoplasmic reticulum.</p>

<p>ICMT-IN-25 (compound 37) serves as a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an IC50 value of 0.025 μM [1].</p>

<p>I-BET469 is a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose.</p>

<p>PAN12314 (Compound 5a) is a 5-HT4R partial agonist with cognition-enhancing effects in animals, lacking a formal name.</p>

<p>T-705RTP is a selective and GTP-competitive of influenza virus RNA polymerase(IC50 of 0.14 μM and a Ki of 1.52 μM), has potent anti-influenza virus activity.</p>

<p>mDPR-Val-Cit-PAB-MMAE TFA is a drug-linker conjugate for antibody-drug conjugates (ADC), comprising the tubulin polymerization inhibitor MMAE coupled with an ADC-specific peptide linker (Val-Cit-PAB) [1].</p>

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

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

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

<p>CH-5137291 is a pure AR antagonist with AR nuclear translocation inhibition activity. It suppresses castration and prevents the growth of prostate cancer cells.</p>

<p>(R)-FTY-720 Vinylphosphonate is a sphingosine 1-phosphate type 1 (S1P1) receptor agonist and lacks anti-apoptotic activity.</p>

<p>FAUC-179 is a selective dopamine D4 receptor partial agonist.</p>

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

<p>Kadsurenin L is a neolignan originally isolated from Piper kadsura. It has a role as a platelet-activating factor receptor antagonist and a plant metabolite.</p>

<p>ASP-4000 HCl is an inhibitor of dipeptidyl peptidase 4 (DPP) with anti-hyperglycemic activity.</p>

<p>WIN site inhibitor 1 TFA is a WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5) inhibitor (Kd: 0.1 nM).</p>

<p>p-SCN-Bn-HOPO: superior (89)Zr ImmunoPET chelator, low background, high tumor contrast, minimal bone uptake in BT474 breast cancer scans.</p>

<p>MEN-10612 is a cyclic pseudopeptide and potent tachykinin NK-2 receptor antagonist.</p>

<p>Compound 17b, a TLR7 agonist also known as TLR7 agonist 14, exhibits high potency with an EC50 of 18 nM.</p>

<p>WAY-649123 is an active molecule that exhibits (in vitro) antagonistic properties against (alpha-1A adrenergic receptors), with a (pKi) of 8.9.</p>

<p>TLR8 Agonist 5, exhibiting potent efficacy as a TLR8 agonist, demonstrates an EC50 of 20 nM in HEK-Blue hTLR8, effectively activating the immune response.</p>

<p>Proteasome-IN-4, a potent non-covalent inhibitor (IC50=8.39nM), halts cancer cell growth, useful for oncology studies.</p>

<p>KW-7158, a potassium channel activator, is used potentially for the treatment of urinary urgency and frequency.</p>

<p>AKR1C3-IN-6: Strong AKR1C3 inhibitor (IC50: 0.31 μM); weak on AKR1C2 (IC50: 73.23 μM); shows antitumor effects.</p>

<p>BCN-endo-PEG4-NHS is an ADC linker comprising 4 polyethylene glycol (PEG) units and features the lyophilic bidentate macrocyclic ligand, endo-BCN. This structure enables the synthesis of macrocyclic complexes and allows endo-BCN to engage in click chemistry reactions with azide-group-containing molecules to form stable triazoles without the need for catalysts.</p>

<p>1-Palmitoyl-sn-glycerol 3-phosphate (1-P-GPA), an endogenous metabolite, is utilized in the research of non-alcoholic fatty liver disease [1].</p>

<p>SEN461 is a wnt inhibitor.</p>

<p>1-1(Z)-Hexadecenyl-2-palmitoyl-sn-glycero-3-PC, a plasmalogen, appears in various rat tissues including the liver, heart, kidney, and both gluteus and soleus muscles, as well as visceral and subcutaneous adipose tissues. It serves in lipid bilayer synthesis to investigate how amphiphilic compounds, like lysophosphatidylcholine (1-palmitoyl-2-hydroxy-sn-glycero-3-PC) and lysoplasmenylcholine, influence membrane dynamics.</p>

<p>Indimilast blocks PDE4, reducing lung inflammation and bronchiectasis, possibly treating COPD.</p>

<p>SIM010603, an oral RTK inhibitor, targets Kit, VEGFR-2, PDGFR-β, RET, FLT3 (IC50: 5.0-68.1 nmol/l), inhibits cell proliferation and angiogenesis.</p>

<p>MMP-9-IN-8 (Compound 3), an MMP-9 inhibitor, exhibits inhibitory activities of 42.16% at 10 μM and 58.28% at 50 μM.</p>

<p>"(S)-3'-amino Blebbistatin, retaining the active stereochemistry of the less stable and more phototoxic (–)-blebbistatin, serves as a refined selective cell-permeable inhibitor of non-muscle myosin II ATPases. This compound efficaciously inhibits the Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB across several species with IC50s ranging from 0.5-5 µM, and exhibits minimal inhibition against smooth muscle myosin (IC50= 80 µM). Its primary functions include obstructing apoptosis-related bleb formation, directed cell migration, and cytokinesis in vertebrate cells. (S)-3'-amino Blebbistatin overcomes (–)-blebbistatin's limitation of rapid degradation under blue light (450-490 nm) exposure, which generates cytotoxic intermediates, thus posing a challenge for fluorescent live cell imaging applications. The introduction of a 3'-amino group to its structure notably reduces fluorescence while maintaining (–)-blebbistatin's activity, making it a superior alternative for research purposes."</p>

<p>Trithiozine is used in peptic ulcer and hypersecretory disorder research for its antiulcer and antisecretory properties.</p>

<p>CP-664511 is an alpha4beta1/ vascular cell adhesion molecule-1 (VCAM-1) inhibitor with therapeutic potential for allergic airway disease.</p>

<p>β-Catenin Modulator-2 (Compound IIa-130), which is an oxazole-thiazole derivative, serves as a potent and selective modulator of β-Catenin [1].</p>

<p>VU 0546110, a selective inhibitor of the sperm-specific potassium channel SLO3 (IC50= 64 μM), demonstrates 40-fold selectivity over SLO1.</p>

<p>6-N-Phthalimidoy hexanoic acid (compound FH) is a hapten featuring a carboxyl group at its spacer arm terminus, facilitating reaction with proteins' free amine groups. This compound is capable of conjugation with carrier proteins for use in antigen design [1].</p>