Organometallic Ligands

<p>Dopamine reuptake inhibitor; ligand of sigma receptors</p>

<p>Glucocorticoid receptor agonist; anti-inflammatory</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>Inhibitor of CDK2, JAK2 and FLT3; anticancer</p>

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

<p>Moracin C is a prenylated flavonoid, which is a type of naturally occurring compound. It is derived from the Morus genus, commonly known as mulberry trees. This compound functions primarily as an antioxidant, showing activity that may protect cells from oxidative stress by neutralizing free radicals.</p>

<p>Aniracetam is a nootropic drug that is used to alleviate memory disturbances caused by cerebrovascular disease and brain disorders. This drug has anti-depressive and anxiolytic properties and is said to target serotonin and dopamine receptors.</p>

<p>Nicotinamide is a form of vitamin B that is found in food and it used to treat many conditions such as pellagra and acne. It replenishes cellular energy and has anti-inflammatory effects. Nicotinamide is an inhibitor of the enzyme SIRT1 in vitro but can be a stimulator in cells.</p>

<p>Hispolon is a naturally occurring polyketide compound, which is derived from the mushroom Phellinus linteus, commonly found in Asia. This compound is known for its diverse biological activities, primarily functioning as an antioxidant, anti-inflammatory, and antitumor agent. The mode of action of hispolon involves the modulation of multiple cellular pathways. It has been shown to induce apoptosis in cancer cells by triggering intrinsic and extrinsic apoptotic pathways. Additionally, hispolon exhibits the ability to inhibit the NF-κB pathway, subsequently decreasing the expression of pro-inflammatory cytokines and leading to an anti-inflammatory effect.</p>

<p>Dopamine D2 receptor antagonist</p>

<p>Inhibitor of dopamine (D2) and serotonin (5HT2) receptors; anti-psychotic</p>

<p>Inhibitor of ErbB2 (IC50 = 3 nM) and EGFR kinase (IC50 = 6.4 nM) with anti-proliferative effects. It inhibits ErbB2 receptor autophosphorylation and induces G1 cell cycle block. The CP 724714 treatment induces reduction of downstream ErbB2 receptor tyrosine kinase signalling, tumor cell apoptosis, release of caspase 3 and regression of tumors in in vivo and in vitro models.</p>

<p>Adefovir is an antiviral acyclic nucleoside phosphonate (ANP) analogue that works by blocking reverse transcriptase. This drug is used to treat infections associated with Hepatitis B.</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>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>SIRT1 activator</p>

<p>Inhibits MEK1 and MEK2 kinases; targeted therapy for melanoma</p>

<p>COX-2 enzyme inhibitor; anti-inflammatory</p>

<p>Inhibitor of fibroblast growth factor receptors (FGFR1, FGFR2 and FGFR3). Demonstrated anti-tumor effects in pre-clinical models of FGFR-driven tumors. AZD 4547 resulted in tumor progression when applied on a patient-derived model of FGFR1-amplified squamous cell lung disease. Antineoplastic effects also observed in FGFR2-amplified gastric cancer.</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>Orally available prodrug of gemcitabine</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>Inhibitor of dopamine-?-hydroxylase</p>

<p>Pomalidomide is an immunomodulatory agent that inhibits transcriptional regulation by interacting with the pomalidomide-binding protein, which prevents its interaction with RNA polymerase II and thereby prevents DNA transcription. The study with U266 cells demonstrated that pomalidomide targets CRBN, part of an E3 ligase complex, and inhibits its autoubiquinitation and supresses a critical gene (IRF4, interferon regulatory factor 4) for myeloma cell growth with concentrations up to 10 μM. In vitro assays have shown that pomalidomide has inhibitory effects on cell signaling pathways, such as the NF-κB pathway. Pomalidomide also decreases the production of proinflammatory cytokines, such as TNFα and IL-1β, by inhibiting their synthesis or their release from activated monocytes. Recently, the promoting effect of pomalidomide, as its analog lenalidomide, on erythropoiesis (production of red blood cells) has been investigated, demonstrating positive results for its use as a potential new therapy agent for β-hemoglobinopathies.<br>Pomalidomide 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>(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>Clebopride is a dopamine antagonist drug that is used in the treatment of symptoms associated with gastrointestinal disorders. This drug is also used to treat nausea and vomiting. Clebopride blocks dopamine to allow an increase in the release of acetylcholine so that muscle movement in the digestive system is increased.</p>

<p>Azathioprine belongs to the group of immunosuppressant drugs that suppress the immune system by inhibiting the production of white blood cells (leukocytes). It is used to treat inflammatory diseases, such as rheumatoid arthritis, lupus, and Crohn's disease. Azathioprine is metabolized in the liver. Additionally, this drug inhibits DNA synthesis by binding to nuclear DNA, preventing RNA transcription and protein synthesis in susceptible cells.</p>

<p>Febuxostat is a non-purine xanthine oxidase inhibitor that is used for the treatment and management of hyperuricemia and chronic gouty arthritis. Febuxostat inhibits the uptake of uric acid from the blood into cells and thereby reduces its concentration in plasma. Additionally, this drug has been shown to have anti-inflammatory and antioxidant effects.</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>Inhibits aromatic amino acid decarboxylase</p>

<p>Agonist of A3 adenosine receptor; antineoplastic</p>

<p>Inhibitor of DNA topoisomerase I</p>

<p>Spla2-X Inhibitor 31 is a chemical inhibitor specifically targeting the human secreted phospholipase A2 group X (sPLA2-X), which is derived synthetically through chemical synthesis. Its mode of action involves binding to the active site of sPLA2-X, effectively blocking its enzymatic activity. This enzyme catalyzes the hydrolysis of phospholipids, leading to the release of arachidonic acid, a precursor for bioactive lipids involved in inflammation and other cellular processes.</p>

<p>Inhibitor of prolyl 4-hydroxylase PHD</p>

<p>A potent and selective covalent inhibitor of fibroblast growth factor receptor 4 (FGFR4). This receptor tyrosine kinase activates an oncogenic driver in hepatocellular carcinoma, the fibroblast growth factor 19 (FGF19). The FGFR4 inhibitor is therefore a promising candidate for the treatment of advanced liver cancer.</p>

<p>Histamine (H1) receptor antagonist; anti-ulcer agent</p>

<p>Bupropion is an antidepressant drug that has been used in treatment trials for major depressive disorder. It has been shown to be effective in combination therapy with other drugs, such as a serotonin reuptake inhibitor (SSRI) or a tricyclic antidepressant (TCA). The drug's mechanism of action is not well understood but is said to increase the levels of dopamine and norepinephrine by inhibiting their reuptake.</p>

<p>Amlexanox is an antiallergic and anti-inflammatory drug that has been shown to be effective in treating rhinitis and allergic asthma in clinical studies. It prevents the slow-reacting substance of anaphylaxis (SRS-A) from being released chemically as a mediator and may have antagonistic effects on interleukin-3.</p>

<p>Inhibits c-MET tyrosine kinases</p>

<p>WIN 64338 hydrochloride is a bradykinin receptor antagonist that inhibits the action of bradykinin, an inflammatory and pain-causing agent.  It also blocks the binding of bradykinin to its receptors, thereby preventing their activation which causes inflammation and pain.  The affinity values for WIN 64338 hydrochloride at the bradykinin B2 receptor are more than 1000 times greater than those at the bradykinin B1 receptor.</p>

<p>Activates muscarinic GPCR DREADDs, which are unaffected by the endogenous ligand acetycholamine of the parent receptor. Clozapine is metabolized to clozapine N oxide in the liver, mainly by CYP3A4. Has anti-seizure effects, when induced by chemoconvulsants pilocarpine and picrotoxin.</p>

<p>Inhibitor of Factor Xa; anti-thrombotic</p>

<p>Glimepiride is a sulfonylurea drug that is used in the treatment of type 2 diabetes mellitus. This drug works by inhibiting ATP-sensitive potassium channels by binding non-specifically to the B sites of both sulfonylurea receptor-1 (SUR1) and sulfonylurea receptor-2A (SUR2A) subunits. As a result, this promotes insulin secretion from beta cells.</p>

<p>This compound is a novel negative allosteric modulator of glutamate metabotropic receptor mGlu7. It is highly selective for mGlu7 over other receptors of mGlu class with IC50 = 795 nM. Although VU 6010608 showed favourable brain penetration in rats, it has been proposed as an in vitro tool for electrophysiology studies. The mGlu7 is broadly distributed within the mammalian central nervous system and it plays a key role in neuronal function and synaptic plasticity.</p>

<p>Dual IGF-1R and InsR kinase inhibitor; antineoplastic</p>

<p>Inhibitor of isocitrate dehydrogenase 2</p>

<p>Inhibits proto-oncogene Pim kinases (Pim-1, Pim-2 and Pim-3); antineoplastic</p>

<p>Lovastatin is an HMG-CoA reductase inhibitor that is used to lower LDL cholesterol levels and to aid in the management of cardiovascular diseases. Animal studies have demonstrated that this drug has vasculoprotective properties.</p>

<p>Duloxetine is a serotonin and norepinephrine reuptake inhibitor drug that is used to treat anxiety, pain, osteoarthritis and stress incontinence. This drug inhibits the reuptake of the neurotransmitters serotonin and norepinephrine so that there are increased levels of them in the synaptic cleft.</p>