Organometallic Ligands

<p>Casein kinase (CK1ε and CK1Ύ) inhibitor</p>

<p>Dopamine reuptake inhibitor</p>

<p>Diacerein is a slow-onset anthraquinone IL-1 inhibitor that is used in the treatment of joint diseases such as osteoarthritis. This drug is also being studied for the treatment of insulin resistance and diabetes mellitus. Diacerein works to decrease inflammation and cartilage destruction by reducing the level of interleukin-1.</p>

<p>Dapagliflozin is a sodium-glucose cotransporter subtype 2 (SGLT2) inhibitor that can be used in the treatment of diabetes mellitus type 2. It inhibits glucose reabsorption in the proximal tubule of the nephron and results in glycosuria, which helps to improve glycaemic control. Also, Dapagliflozin is used to lower the risk of sustained eGFR decline, end-stage renal disease, cardiovascular death, and hospitalization for heart failure in patients with chronic kidney disease who are at risk of progression.</p>

<p>Amiodarone, a class III anti-arrhythmic agent is used to treat and prevent certain types of irregular heartbeats. It is a competitor for natural ligands of alpha and beta adrenergic receptors, muscarinic acetylcholine receptors, histamine H1 receptors, and serotonin 5HT2A/5HT2C receptors. Amiodarone has been shown to reduce the number of atrial and ventricular arrhythmias in patients with structural heart disease, and has been used to treat atrial fibrillation, ventricular tachycardia, and Wolff-Parkinson-White Syndrome. It has also been used in the prevention of myocardial infarcts due to its ability to modify blood pressure and maintain cardiac function. In addition, amiodarone inhibits prostaglandin synthesis by inhibiting cyclooxygenase enzymes. This prevents inflammation in the gastrointestinal tract and reduces bowel disease symptoms such as cramping or diarrhoea.<br>Amiodarone HCl is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.</p>

<p>Palonosetron is a selective serotonin 5-HT3 receptor antagonist. It is an antinauseant and antiemetic agent that has been shown to be effective in preventing nausea and vomiting induced by cancer chemotherapy, radiotherapy, or surgery. By directly inhibiting serotonin activity in the region postrema and the chemoreceptor trigger zone, the inhibition of 5-HT3 receptors also prevents the visceral afferent stimulation of the vomiting center.</p>

<p>(R)-Phenylephrine is a non-selective α1-adrenoceptor agonist that can be used as a bronchodilator or vasopressor. The biological effects of this compound are due to its ability to cause relaxation of smooth muscle cells and increase blood pressure by stimulating alpha-adrenergic receptors in the body. Also, this drug is used to relieve nasal discomfort caused by colds and allergies and is used to relieve sinus congestion and pressure.</p>

<p>Cetilistat is a drug that is used to treat obesity. This drug inhibits the enzyme pancreatic lipase and so it prevents triglycerides from being hydrolyzed into absorbable free fatty acids.</p>

<p>Inhibitor of HIF1-α transcription factor and repressor of HIF1-α-regulated genes in adult and embryonic stem cell models as well as in tumoral cell lines. FM19G11 inhibits the expression of undifferentiating factors Oct4, Sox2, Nanog, and Tgf-α at transcriptional and protein level. FM 19G11 affects also epigenetic events by reducing histone acetylation and leading to repression of p300, a HIF-transcription activation co-factor.</p>

<p>Lodoxamide is a type of ophthalmic medication known as a mast cell stabilizer, which is chemically synthesized from non-steroidal structures. It works by inhibiting the degranulation of sensitized mast cells and subsequent release of inflammatory mediators such as histamine. This action is achieved through the stabilization of the cell membrane of mast cells, thus preventing cellular activation.</p>

<p>Modulator of S1P receptor</p>

<p>Ziprasidone is an atypical antipsychotic drug that is used to manage schizophrenia, bipolar mania, and agitation. This drug binds to serotonin and dopamine receptors. As a result it enhances modulation of mood and improves overall cognition.</p>

<p>Inhibitor of 8-oxoguanine DNA glycosylase OGG1 with IC50 of 0.059 μM and excellent specificity over other DNA repair enzymes. OGG1 and its substrate 8-oxoguanine are involved in mutagenesis, genotoxicity, inflammation and cancer. The compound can cause accumulation of 8-oxoguanine in DNA in vitro and is a potent tool for the study of OGG1 biology.</p>

<p>Lomustine is an alkylating agent that is used as chemotherapy for treating metastatic brain tumors and relapsed Hodgkin’s disease in combination with radiation treatments. This drug causes alkylation and cross-linking of DNA, thus inducing cytotoxicity. Furthermore, this drug inhibits DNA synthesis.</p>

<p>Omeprazole is a proton pump inhibitor (PPI) that inhibits the production of gastric acid in the stomach. This is due to Omeprazole binding through a stable disulphide bond to the H+/K+ ATPase enzyme found on parietal cells, and preventing hydrogen ion transport. Consequently, gastric acid secretion is supressed. As a PPI, Omerprazole can be used to treat disorders where gastric acid is over-secreted. Examples of these disorders are gastroesophageal reflux disease (GERD) and peptic ulcer disease.</p>

<p>Bruton's tyrosine kinase antagonist; reduces Fcγ receptor signaling</p>

<p>Rabeprazole is a proton pump inhibitor drug that is used to treat symptoms of GERD, heal gastrointestinal ulcers and eradicate Helicobacter pylori. This antiulcer drug suppresses gastric acid by inhibiting the gastric H+/K+ ATPase at the parietal cell.</p>

<p>Eliglustat is an oral medication used as a substrate reduction therapy for Gaucher disease type 1, which is an inherited lysosomal storage disorder. This product is a small-molecule inhibitor derived via chemical synthesis. Its primary mode of action involves the selective inhibition of glucosylceramide synthase, an enzyme responsible for the first committed step in glycosphingolipid biosynthesis. By reducing the production of glucosylceramide, eliglustat decreases the substrate accumulation that contributes to the pathophysiology of Gaucher disease.</p>

<p>Selective c-Met kinase inhibitor</p>

<p>Inhibitor of glucose uptake via GLUT1 and GLUT4 transporters, promoting intracellular glucose deprivation. The compound is a chemical sensitizer to the FAS cell death receptor and is able to break down the resistance of caspase activation. It has potential for anti-cancer therapy as it modulates the Warburg effect in cancer cell lines.</p>

<p>Monoamine oxidase-B inhibitor; anti-parkinsonian; neuroprotective</p>

<p>Prodrug of 5-aminosalicylic acid; anti-inflammatory</p>

<p>Synthetic antineoplastic agent</p>

<p>Solifenacin is a muscarinic antagonist drug that is used to treat symptoms associated with an overactive bladder such as urine urgency and urinary incontinence. This drug has high affinity for M1, M2 and M3 receptors, with its highest being for M3 receptors. Antagonism of these receptors prevent contraction of smooth muscles in the bladder.</p>

<p>AZD 1152 is an Aurora kinase inhibitor, which is a type of small-molecule therapeutic agent. It is derived from the pharmaceutical research conducted by AstraZeneca. Its primary mode of action involves the selective inhibition of Aurora B kinase, an enzyme crucial for the regulation of mitosis. By interfering with this enzyme, AZD 1152 disrupts the normal progression of cell division, leading to the inhibition of proliferation and induction of apoptosis in rapidly dividing cells.</p>

<p>Androgen receptor antagonist; anti-cancer agent</p>

<p>Albuterol is a selective beta-2 adrenergic receptor agonist drug that is used to prevent and treat wheezing, shortness of breath, and other breathing difficulties caused by asthma. It relaxes the muscles in the airways, making them more open. Albuterol also has an anti-inflammatory effect.</p>

<p>An inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase that reduces total cholesterol and low-density lipoprotein (LDL). Cerivastatin is cardioprotective and anti-atherosclerotic. Cerivastatin inhibits the expression of the atherosclerotic genes monocyte chemoattractant protein-1 (MCP-1) and C-C chemokine receptor type 2 (CCR2), whilst inducing the expression of Kruppel-like factor 2 (KLF2).</p>

<p>ÎŽ opioid receptor agonist; anti-nociceptive; anti-depressant</p>

<p>Vasopressin analog; vasoactive agent</p>

<p>MET tyrosine kinase inhibitor; anti-proliferative; pro-apoptotic</p>

<p>Anastrozole is a non-steroidal drug that belongs to the class of aromatase inhibitors. It inhibits the production of estrogen by blocking the conversion of androgens to estrogens in peripheral tissues. The drug has been shown to be effective in treating breast cancer in postmenopausal women. In vitro assays have shown that Anastrozole can inhibit tumor growth as well as induce apoptosis in human serum cells, which suggests that it may be effective against a variety of cancers.</p>

<p>Hyp9 is an advanced biochemical reagent, which is derived from sustainably sourced natural compounds with a proprietary purification process. Its mode of action involves targeted binding to specific molecular sites, enabling the modulation of biochemical pathways with high precision.</p>

<p>Thioglycosyl Naphthalimide is a highly potent human O-GlcNAcase (hOGA) inhibitor with good selectivity against human β-N-acetylhexosaminidase B (HsHexB).</p>

<p>Fingolimod is a sphingosine 1-phosphate receptor modulator that is used in the treatment of relapsing-remitting form of multiple sclerosis. It is also being studies to manage lung complications in patients with COVID-19. This drug binds to various sphingosine 1-phospahte receptors and suppresses the exit of lymphocytes from lymph nodes.</p>

<p>NMDA glutamate receptor antagonist</p>

<p>Androgen receptor antagonist</p>

<p>Atenolol is a beta-blocker that slows the heart rate and decreases the force of contraction, which reduces the workload on the heart. Atenolol has been shown to be effective in lowering blood pressure in people with chronic kidney disease who are not taking angiotensin-converting enzyme inhibitors. It is also used to treat hypertension and chronic angina.</p>

<p>Pemirolast is an antihistamine drug that is used for the treatment of allergies such as hay fever and allergic conjunctivitis. This drug binds to the histamine H1 receptor and blocks the action of histamine which results in the relief of allergic symptoms brought on by histamine. This drug is also a mast cell stabilizer.</p>

<p>Metabotropic glutamate receptor subtype-5 antagonist</p>

<p>Inhibitor of ERK1 and ERK2 kinases</p>

<p>Potent and selective inhibitor of the glycogen synthase kinase GSK-3. Promotes cell renewal in embryonic stem cells by modulating Notch, MAPK and TGF-β signalling pathways, which are involved in pluripotency. It also affects the Wnt/β-catenin pathway and alters expression of genes coding for proteins, epigenetic regulatory elements and non-coding RNAs. The combination of CHIR 99021 and basic fibroblast growth factor (bFGF) allows long-term self-renewal in adult mouse retinal progenitor cells.</p>

<p>5-HT1A serotonin receptor agonist; alleviates symptoms of depression</p>

<p>Camostat is a serine protease inhibitor that is used for the treatment of chronic pancreatitis. This drug has shown to reduce inflammation and pain. Studies have shown that Camostat has also inhibited the entry of SARS-CoV-2 in lung cells by inhibiting the priming process of S-protein, necessary for the viral entry into host cells.</p>

<p>Inhibits type III tyrosine kinases (PDGFRα, PDGFRβ, FLT3)</p>

<p>Retinoic acid receptor alpha agonist; antineoplastic</p>

<p>Ramelteon is a synthetic drug, which is a melatonin receptor agonist with high affinity for MT1 and MT2 receptors. These receptors are primarily located in the suprachiasmatic nucleus of the brain, an area responsible for regulating circadian rhythms. By binding to these receptors, Ramelteon mimics the effects of the endogenous hormone melatonin, promoting the onset of sleep.</p>

<p>Rivastigmine is a cholinergic agent that is used in the treatment of dementia in Parkinson’s and Alzheimer’s disease. This drug is a carbamate derivative that binds to and inactivates cholinesterase such as acetylcholinesterase and butyrylcholinesterase. This leads to an increase concentration of acetylcholine at cholinergic synapse.</p>

<p>A cytidine analogue and inhibitor of DNA methyl transferases (DNMTs) with anti-cancer activity. This stable, hydrophilic compound forms covalent complexes between DNMT and zebularine-substrate DNA. It causes DNA lesions that block replication and cause replication fork collapse, leading to the formation of DNA double-strand breaks. It was also shown that zebularine-induced DNA methylation decrease in the IL-1β promoter region and disrupts molecular mechanisms of neuroinflammation. Moreover, this molecule down-regulates the DNA-methylation profile in the pluripotency genes’ promoters, which leads to improved development of somatic cell nuclear transfer (SCNT) embryos.</p>

<p>Long-acting β2-agonist; bronchodilator</p>

<p>Acecelofenac is a non-steroidal anti-inflammatory drug that is used in the treatment of osteoarthritis, arthritis, and ankylosing spondylitis. This drug is also a cyclooxygenase inhibitor and works by inhibiting this enzyme so that pain and inflammation is reduced.</p>

<p>Imiquimod maleate is an immune response modifier, which is a synthetic compound sourced from chemical synthesis. Its mode of action involves the activation of the immune system through the stimulation of toll-like receptor 7 (TLR7), leading to the induction of various cytokines, such as interferon-alpha, that initiate an antiviral and anti-tumor response.</p>

<p>γ-secretase inhibitor; reduces amyloid-β in brainÂ</p>

<p>An irreversible GSK-3β inhibitor that reduces phosphorylation of tau proteins, protects from neuronal loss and has cognitive and behavioural benefits in murine models. Studied for its potential as a therapeutic agent in Alzheimer’s disease and other neurodegenerative diseases. Tideglusib was also shown to inhibit the main protease Mpro from the SARS-CoV-2 virus with IC50 of 1.55 μM.</p>

<p>Belinostat is a histone deacetylase (HDAC) inhibitor, which is a synthetic compound with a targeted mechanism of action. It is derived from the hydroxamic acid class and functions by inhibiting the activity of HDAC enzymes. These enzymes are responsible for removing acetyl groups from lysine residues on histone and non-histone proteins, altering chromatin structure and affecting gene expression. By inhibiting HDACs, Belinostat leads to an accumulation of acetylated histones, promoting an open chromatin structure and reactivation of silenced genes that can suppress tumor growth.</p>

<p>Ractopamine hydrochloride is a beta-agonist that stimulates the release of fatty acids from adipose tissue, increasing food intake and weight gain in pigs. It has been shown to have significant interactions with other drugs used for bowel disease, as well as with sodium carbonate, which can be used for control analysis. Ractopamine hydrochloride is an effective drug to stimulate the release of estradiol benzoate in rats during pregnancy. The matrix effect observed when analyzing samples containing ractopamine hydrochloride may be due to its ability to bind to serum proteins or lipids. This drug has been shown to have molecular docking properties that are similar to those found in other molecules.</p>

<p>S1RA hydrochloride is a selective antagonist targeting the sigma-1 receptor, which is a type of small molecule ligand. It is synthesized chemically, enabling precise modulation of its properties for experimental use. S1RA functions by selectively inhibiting the sigma-1 receptor, a chaperone protein involved in modulating ion channels and other receptors within the endoplasmic reticulum. This modulation plays a critical role in various cellular processes, including calcium signaling and cellular stress responses.</p>

<p>Used to treat multiple sclerosis; anti-inflammatory</p>

<p>Pantoprazole is a proton pump inhibitor drug that is used to treat erosive esophagitis and promotes healing of tissue damage caused by gastric acid. It is used for the management of GERD. Through the proton pump inhibition, the formation of hydrochloric acid is inhibited thus inhibiting gastric secretion.</p>

<p>Bromocriptine is a dopamine D2 receptor agonist that is used for the treatment of galactorrhoea which is due to hyperprolactinemia and other prolactin-related conditions. This drug is an ergot alkaloid derivative that inhibits prolactin secretion. Additionally, it can be used to management signs and symptoms of Parkinsonian syndrome. Research has indicated this drug for pulmonary fibrosis as well.</p>

<p>Inhibitor of chymotrypsin</p>

<p>Histamine (H2) receptor antagonist</p>

<p>A selective and potent inhibitor of phosphodiesterase 2 (PDE2). Raises cAMP and cGMP levels in neurons, improves social recognition and object memory in murine animals. Reverses anxiolytic effects induced by oxidative stress in mice by blocking cGMP-PKG signaling.</p>

<p>Inhibitor of immunophilin FKBP12 and mTOR signalling with immunosuppressant activity. Zotarolimus inhibits proliferation of endothelial cells and smooth muscle cells and is employed in vascular interventional therapies.</p>

<p>A serotonin reuptake inhibitor with anticholinergic activity and mild inhibitory activity on noradrenaline reuptake. Paroxetine has been used for the treatment of depression, anxiety disorders, post-traumatic stress disorder, premenstrual dysphoric disorder and obsessive-compulsive disorder.  Also inhibits nitric oxide synthase and cytochrome isoenzyme P450 2D6.</p>

<p>VEGFR tyrosine kinase inhibitor</p>

<p>Estrogen receptor degrader; therapeutic use in breast cancer</p>

<p>A potent inhibitor of STING protein (stimulator of interferon genes), a protein that partakes in intracellular DNA sensing pathway.  H 151 blocks palmitoylation of STING, which is required for the formation of multimeric complexes for recruiting downstream signalling molecules. Inhibition of STING by H 151 reduces pro-inflammatory cytokine synthesis.</p>

<p>Rebamipide is a gastroprotective agent that is used to treat various gastrointestinal disorders such as gastric ulcers and GERD. This drug’s mechanism of action is not fully understood however, it is thought to exert its effects by promoting the secretion of protective mucus in the stomach and intestine, which helps to create a barrier against stomach acid and other irritants. Additionally, it has antioxidant and anti-inflammatory properties that can help reduce tissue damage.</p>

<p>Inhibits isocitrate dehydrogenase 1 (IDH-1) harbouring a gain of function mutation at R132, which causes impaired cellular differentiation via epigenetic modulation. By inhibiting mutant IDH1, synthesis of oncometabolite 2-hydroxyglutarate is reduced. This compound therefore has therapeutic potential in solid and haematological malignancies, such as acute myeloid leukemia (AML).</p>

<p>Sphingosine-1-phosphate receptor modulator</p>

<p>Inhibitor of 5-lipoxygenase activating protein_x000D_</p>

<p>KBU2046 is an antimicrobial peptide, which is derived from natural or synthetic peptide sequences with potential therapeutic properties. It exerts its effects by disrupting the structure and integrity of bacterial cell membranes through the formation of pores or micelles. This action alters membrane permeability, ultimately leading to cell lysis and death.</p>

<p>GSK-lsd1 dihydrochloride is a potent chemical inhibitor, which is derived synthetically to target LSD1, a histone demethylase involved in epigenetic regulation. It functions by inhibiting the enzymatic activity of LSD1, thereby affecting the methylation status of histones, a critical process in regulating gene expression. This inhibition leads to alterations in the transcriptional programs of cells, particularly those in oncogenic pathways.</p>

<p>Inhibitor of FLT3 and AXL tyrosine kinases</p>

<p>17:0-20:4 Pi (4,5) P2 is a synthetic phosphoinositide, which is a chemically defined lipid derived from laboratory synthesis. It features a specific acyl chain composition with a heptadecanoic acid (17:0) at the sn-1 position and an arachidonic acid (20:4) at the sn-2 position. This phosphoinositide mimics naturally occurring phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2), an essential component of cellular membranes.</p>

<p>Inhibits MET, VEGFR1-3, Tie and Ron tyrosine kinases; antineoplastic</p>

<p>Galloylpaeoniflorin is a bioactive compound derived from the roots of Paeonia lactiflora, a plant traditionally used in various herbal medicines. This compound plays a significant role in the realm of natural products, offering intriguing possibilities for research due to its complex chemical structure and biological activities.</p>

<p>Dopamine D2 receptor antagonist</p>

<p>Nicardipine is calcium channel blocker drug that is used for the treatment of hypertension and angina. This drug can also be used in the treatment of asthma and is said to enhance the action of various antineoplastic agents.</p>

<p>Selective and potent inhibitor of glucose transporter GLUT1 with IC50 of 2 nM. The compound limits glucose uptake and is able to block basal as well as stress-regulated glycolysis in ovarian cancer cells. It supresses proliferation, viability and tumorigenicity of ovarian cancer cells.</p>

<p>Gardos channel inhibitor</p>

<p>SIRT1 activator</p>

<p>Bremelanotide is a 7 amino acid peptide that is used to treat hypoactive sexual desire disorder in premenopausal women. This drug is an agonist of many melanocortin receptors. Although, its mechanism is unknown, it is said to increase melanin expression which aids in the regulation of sexual arousal.</p>

<p>Potent and selective inhibitor of polycomb repressive complex 2 (PRC2), by binding to the K27me3-pocket of the regulatory EED subunit. Inhibits H3K27 methylation in histone 3. Has anti-tumor activity in murine xenograft models. Synergistic with EZH2 inhibitor against cancer cell growth.</p>

<p>SHP099 is an allosteric inhibitor of the SHP2 protein, which is derived from targeted small-molecule drug development. Its mode of action involves binding to SHP2 in a region distinct from the catalytic site, thereby stabilizing the protein in its auto-inhibited conformation and preventing activation. This disrupts downstream signaling pathways mediated by SHP2, a protein-tyrosine phosphatase essential in promoting oncogenic signaling through the RAS/MAPK pathway.</p>

<p>Icilin is a transient receptor potential M8 (TRPM8) agonist drug that is used for the treatment of pruritis. This drug has shown to be effective in producing an extreme cold sensation in both human and animal models. It is used in research for studying TRP channels.</p>

<p>Inhibitor of Rho-kinases</p>

<p>13:0 Lyso PS is a lysophosphatidylserine, which is a synthetic lipid derivative that serves as a crucial component in biochemical research. It is synthesized from naturally occurring phospholipids, offering a structurally simplified molecule that retains the functional headgroup critical for biological activity. As a single fatty acid chain molecule, its mode of action includes the modulation of cellular processes through interactions with lysophospholipid receptors and participation in signaling pathways. These interactions can influence cell proliferation, apoptosis, or differentiation, depending on the biological context.</p>

<p>Aripiprazole is an antipsychotic drug that is used in the treatment for various mood and psychotic disorders such as schizophrenia, depression and bipolar disorder. Although, its mechanism is not fully understood, the antipsychotic action of aripiprazole is likely due to its partial agonist activity on D2 and 5-HT1A receptors as well as its antagonist activity at 5-HT2A receptors.</p>

<p>BRK tyrosine kinase (PTK6) inhibitor; anti-proliferative in breast cancer cells</p>