Organometallic Ligands

<p>Lenalidomide is a thalidomide derivative that is used to treat multiple myeloma and anemia. This drug exerts immunomodulatory effects by altering cytokine production. Lenalidomide also directly inhibits the cullin ring E3 ubiquitin ligase complex.</p>

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

<p>Prasugrel is a thienopyridine prodrug that inhibits the enzyme ADP-dependent P2Y purinergic receptor. Prasugrel inhibits platelet aggregation and the formation of blood clots by blocking the conversion of ADP to ATP on the surface of platelets, thus preventing the release of serotonin from platelets. The reaction products formed by prasugrel are similar to those formed by clopidogrel and include hydrogen sulfate ions and a thiol-containing metabolite. It has also been shown to have potent cytotoxic activity against melanoma cells and anti-inflammatory properties. <br>Prasugrel 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>Leflunomide is a pyrimidine synthesis inhibitor drug that is used to treat rheumatoid arthritis. Although its mechanism of action is not fully determined, this drug has shown to interfere with cell cycle progression by inhibiting dihydroorotate dehydrogenase and has shown antiproliferative activity. As a result of this, it interferes with the expansion of activated autoimmune lymphocytes. Additionally, Leflunomide is a tyrosine kinase inhibitor.</p>

<p>Ipratropium is an ammonium derivative of atropine and acts as an anticholinergic drug that is used for the control of bronchospasms in chronic obstructive pulmonary disease (COPD). This drug is an antagonist of muscarinic acetylcholine receptors and produces an inhibitor of the parasympathetic system. As a result, this leads to bronchodilation and fewer bronchial secretions.</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>Inhibitor of oxidative phosphorylation which acts on the F0F1 ATP synthase in the inner mitochondrial membrane and causes acute increase in mitochondrial membrane potential. Gboxin was shown to accumulate in mitochondria of cancer cells, to cause cellular toxicity and cell growth inhibition in mouse glioblastoma. However, Gboxin did not inhibit growth of mouse embryonic fibroblasts or neonatal astrocytes.</p>

<p>Selective A2 adenosine receptor agonist. Increases cardiac output in rats with acute heart failure, mediated by reduced venous resistance and raised heart rate. Demonstrates neuroprotective properties by lowering blood cell infiltrates and neuroinflammation in ischemic cerebral tissue.</p>

<p>Pioglitazone is a thiazolidinedione drug that is used in combination with diet change and exercise to treat glycemic levels in patients with type 2 diabetes mellitus. This drug is an agonist of peroxisome proliferator-activated receptor-gamma and increases glucose uptake. In animal studies, Pioglitazone has shown to have anti-inflammatory properties.</p>

<p>Toxin; induces pulmonary hypertension</p>

<p>An agonist of 5-HT1A serotonin receptors. Neurotrophic and neuroprotective activities have been demonstrated in neurodegenerative models in vivo. This is mediated by increasing the secretion of nerve growth factor (NGF), when tested in astrocytes in vitro. Anti-nociceptive activity was displayed in a model of acute tonic nociceptive and inflammatory pain.</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>Trkc active human is a bioengineered protein, which is a synthetic derivative of the TRKC (tropomyosin receptor kinase C) receptor. This product is derived from recombinant DNA technology, utilizing expression systems to produce a functionally active protein that mimics the natural receptor found in human cells. Its mode of action involves the specific binding and activation of neurotrophin-3 (NT-3), a critical signaling molecule in the nervous system.</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>Dabigatran is an anticoagulant that is used for the treatment of atrial fibrillation and prevention of venous thromboembolic events. It is a drug that acts as an inhibitor of the enzyme thrombin. Dabigatran inhibits platelet activation and aggregation, which reduces the risk of stroke or other vascular events. Dabigatran is a prodrug and does not have any activity in its active form.</p>

<p>CholecystokininB (CCKB) receptor antagonist</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>NButGT (N-butyryl-glucosamine-1,5-lactone O-(phenylcarbamoyl)oxime) is a selective inhibitor of O-GlcNAcase (OGA), the enzyme responsible for removing O-linked N-acetylglucosamine (O-GlcNAc) modifications from proteins. It effectively increases O-GlcNAc levels in cells and tissues without altering hexosamine biosynthetic pathway enzyme expression. It has also been shown that NButGT rapidly increases O-GlcNAcylation of mitochondrial proteins involved in oxidative phosphorylation and metabolism. While effective, NButGT served as a precursor to more potent OGA inhibitors like Thiamet-G. These findings highlight NButGT's importance as a tool for studying O-GlcNAcylation in various biological contexts, particularly in cardiac and neurological research. For example, in recent cardiac studies, NButGT pretreatment has demonstrated an improvement in cardiac output and mitochondrial respiration when combined with epinephrine.</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>BMH-7 is a small molecule inhibitor used in molecular biology, which is derived from chemical synthesis methods. It interacts with specific protein domains to disrupt protein-protein interactions within cellular pathways. The mode of action involves binding to target proteins, thereby inhibiting essential interactions that are crucial for the stability and function of multiprotein complexes. This targeted approach allows researchers to dissect complex signaling pathways and understand the underlying mechanisms of cellular functions.</p>

<p>Inhibitor of chymotrypsin</p>

<p>Endothelin receptor antagonist</p>

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

<p>4,5,6,7-Tetrabromobenzimidazole is a brominated heterocyclic compound, which is synthesized chemically from benzimidazole. Its bromination at the 4, 5, 6, and 7 positions of the benzimidazole ring enhances its reactivity, making it a highly potent inhibitor in various enzymatic processes. This compound is primarily sourced through methods that involve controlled bromination reactions in laboratory settings.</p>

<p>2-adrenoceptor agonist; bronchodilator</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>Sunitinib is a tyrosine kinase inhibitor drug. It is a drug that is used as a treatment for renal cell carcinoma, gastrointestinal stromal tumor, and other solid tumors. This drug inhibits tyrosine kinases such as VEGFRs, this prevents tumour growth and pathologic angiogenesis.</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.</p>

<p>Smoothened receptor agonist; induces mesenchymal progenitor cell differentiation</p>

<p>S6821 is a synthetic compound classified as a selective inhibitor, which is derived through chemical synthesis processes. The compound functions by targeting specific molecular pathways involved in cellular processes, primarily through inhibition of particular enzymes or signaling proteins. This selective inhibition allows for precise modulation of biochemical pathways, providing insight into cellular mechanisms and disease pathology.</p>

<p>Azocasein is a chromogenic substrate, which is derived from casein, with azo dye linkages. It functions by undergoing hydrolysis in the presence of proteolytic enzymes, resulting in the release of soluble azo dye fragments that can be quantified spectrophotometrically. This mode of action allows for the measurement of protease activity by evaluating the intensity of the color change, typically at an absorbance wavelength of around 350-440 nm.</p>

<p>Forskolin is a compound derived from the medicinal plant Coleus forskohlii. As an activator of adenylate cyclase, Forskolin causes increases cellular levels of cAMP, and can be used in cell physiology research. It also has antihypertensive, platelet aggregation inhibitory and smooth muscle relaxant effects.</p>

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

<p>HS-1371 is a selective chemical inhibitor targeting specific enzymes, which is derived from synthetic organic compounds with a high affinity for its target proteins. It functions by selectively binding to the active site of the enzyme, inhibiting its activity and subsequently influencing downstream signaling pathways within the cell. This mode of action allows researchers to dissect complex biochemical pathways and assess the impact of enzyme inhibition on cellular functions.</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>Inhibitor of serotonin reuptake</p>

<p>Microtubule disrupter; anti-mitotic drug; anti-cancer alkaloid</p>

<p>Temozolomide is an imidazotetrazine alkylating agent. It has anti-tumor activity against a broad spectrum of tumors, such as leukemias, lymphomas and solid tumors. Temozolomide induces G2/M arrest, preventing cells from entering mitosis and, therefore, apoptosis. As a drug resistance-modifying agent it is used for studying drug resistance mechanisms in glioblastoma cell lines.</p>

<p>AP 1903 is a synthetic small molecule, which acts as a dimerizer ligand. It is derived from the modification of the macrolide antibiotic rapamycin to remove its immunosuppressive effects, thus enabling targeted control of cellular processes. The mode of action involves binding to engineered receptors on the cell surface that contain drug-dependent domains. This binding triggers the dimerization of these receptors, leading to downstream signaling and subsequent cellular responses.</p>

<p>A highly potent antagonist of group II metabotropic glutamate receptors (IC50 values = 21 nM and 14 nM at human mGluR2 and mGluR3 respectively). LY 341495 also inhibits group I and III mGluRs with lower potencies (IC50 values = 0.17, 7.8 and 8.2 µM at mGluR8, mGluR1a and mGluR5a respectively). There has been contradicting findings on the antidepressant and anxiolytic activities of this compound. Enhanced cognitive function and locomotor activity have also been described for LY 341495.</p>

<p>Inhibits FGFR family of kinases; antineoplastic; anti-angiogenic</p>

<p>Nisoldipine is a calcium channel blocker that is used to treat hypertension. It acts on vascular smooth muscle cells by blocking voltage-gated L-type calcium channels. By inhibiting the influx of calcium in smooth muscle cells, Nisoldipine prevents calcium-dependent smooth muscle contraction and subsequent vasoconstriction.</p>

<p>Pravastatin is an HMG-CoA reductase inhibitor that is used to lower lipid levels and manage cardiovascular events such as strokes and myocardial infarction. This drug inhibits HMG-CoA reductase allowing for a reduction in the level of cholesterol.</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>Promotes binding of vWf to glycoproteins on platelets, inducing aggregation</p>

<p>Fenpiverinium is an anticholinergic and antispasmodic agent that is used to treat muscle spasms and pain. Fenpiverinium inhibits the production of acetylcholine at muscarinic receptors by inhibiting cholinesterase enzymes. Also it has an effect on autoimmune diseases and non-immune-related diseases such as lupus erythematosus, rheumatoid arthritis, psoriasis, and Crohn's disease. It is also effective against pain caused by diabetes mellitus.</p>

<p>Clopidogrel is a potent inhibitor of the platelet aggregation. It reduces blood clotting by inhibiting the ADP receptor on the surface of platelets, thereby inhibiting the aggregation and adhesion of platelets. Clopidogrel has been shown to be effective in preventing thrombosis, myocardial infarction (heart attack), and stroke. Clopidogrel inhibits the activity of cytochrome P450 3A4 (CYP3A4) and p2Y 12 receptors. Clopidogrel has been shown to have synergic effects with nonsteroidal anti-inflammatory drugs (NSAIDs). The polymorphic nature of Clopidogrel can be monitored using a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for quantification in biological samples such as human serum and plasma.</p>