Organometallic Ligands

<p>Inhibitor of the intracellular copper chaperones ATOX1 and CCS</p>

<p>Selective and potent inhibitor of lysine acetyltransferases KAT6A and KAT6B with IC50 values of 8 nM and 28 nM, respectively. The compound is a reversible competitor of acetyl coenzyme A domain of KAT6A/B enzymes. It inhibits MYST-catalysed histone acetylation and potentiates senescence in vitro and in zebrafish model of hepatocellular carcinoma. The compound opened the door to a new class of cancer therapeutics that could potentially direct the cancer cells in senescence or permanent dormancy.</p>

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

<p>Neu5Ac[1Me,4789Ac]a(2-3)Gal[246Bz]-b-MP is a synthetic glycan, which is a complex carbohydrate molecule modeled after naturally occurring glycoconjugates. This product is derived through chemical synthesis in the laboratory, allowing precise control over its structure and functional groups. It consists of sialic acid (Neu5Ac) linked to galactose (Gal), with several protective acetyl (Ac) and benzyl (Bz) groups that confer stability during synthesis and ensure high specificity in its interactions.</p>

<p>Dopamine reuptake inhibitor</p>

<p>Activator of p53; inhibitor of NF-?B</p>

<p>COX-2 inhibitor; anti-inflammatory</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>Halogenated derivative of febrifugine; coccidiostat</p>

<p>Saha Chloroalkane T1 is a specialized chemical compound, typically categorized as a chloroalkane. It emerges from a synthetic process involving the chlorination of hydrocarbons, specifically alkanes, which serves as its primary source. The mode of action for chloroalkanes like Saha Chloroalkane T1 involves the stable incorporation of chlorine atoms, enhancing reactivity and providing versatility in chemical reactions.</p>

<p>Oxaprozin is a non-steroidal anti-inflammatory drug (NSAID) used for the treatment of osteoarthritis and rheumatoid arthritis. This drug relieves swelling and inflammation by inhibiting the enzyme cyclooxygenase which in turn inhibits prostaglandin synthesis.</p>

<p>Oxaliplatin is a platinum-based DNA-cross-linking agent. It is a chemotherapeutic drug, often used in combination with leucovorin, fluorouracil, and capecitabine. Oxaliplatin works by cross-linking DNA thus inhibiting the synthesis of RNA and proteins, which leads to cell death and inhibition of cancer cells growth. It is more effective than cisplatin or irinotecan in treating metastatic cancer. Oxaliplatin also has effects on Toll-like receptor 4 (TLR4) expression levels in vitro and in vivo models. In addition, oxaliplatin's effect on ATP binding cassette transporter proteins may be responsible for its antitumour activity against solid tumours.<br>Oxaliplatin 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>Tolterodine is a muscarinic antagonist drug that is used for the treatment of an overactive bladder and its conditions associated with that such as urine urgency and incontinence. This drug act as an antagonist at muscarinic receptors which results in inhibition of bladder contraction, decrease in detrusor pressure, and an incomplete emptying of the bladder.</p>

<p>A2A adenosine receptor antagonist</p>

<p>Inverse agonist of 5-HT2A serotonin receptor; anti-psychotic</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>Endogenous non-toxic agonist of the aryl hydrocarbon receptor (AhR) with immunosuppressive activity. The compound also inhibits the nuclear translocation of Smad2/3/4 leading to aberrant Transforming Growth Factor-β1 (TGFβ1) signaling. It inhibits myofibroblast differentiation and is a potential anti-scarring agent.</p>

<p>Gastric proton pump inhibitor</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>Inhibitor of AKR1C3 (type 5 17β-hydroxysteroid dehydrogenase)</p>

<p>Inhibitor of ecto-ATPase which blocks the hydrolysis of nucleoside diphosphates and triphosphates in extracellular space. The compound inhibits NTPDase1, NTPDase 3, NTPDase 8 and NPP1and prolongs the effect of ATP on purinergic P2 receptors in environment with physiological concentrations of nucleotides. The compound has variable effectiveness as ecto-ATP inhibitor in mouse, rat, human and guineia pig tissues.</p>

<p>A reversible and selective inhibitor of thrombin that rapidly binds to the catalytic site directly. Inhibits both soluble and bound forms of thrombin. Used for prophylaxis and treatment of heparin-induced thrombocytopenia type II.</p>

<p>Used to treat psoriasis; teratogenic</p>

<p>Inhibits multiple receptor tyrosine kinases (RTKs), including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl. Sitravatinib inhibits proliferation of sarcoma cells and reduced tumor growth in vivo. Promotes immune response in tumor microenvironment and enhances sensitivity to immune checkpoint inhibitors. This compound is undergoing several clinical trials as a potential anti-cancer therapeutic agent.</p>

<p>Phosphodiesterase 5 inhibitor; anti-impotence drug</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>Pheniramine is an antihistamine drug that is used to treat allergic rhinitis and pruritus. This drug is a histamine receptor antagonist and competes with histamine for the H1 receptor. Pheniramine aims to reduce edema, itching and redness. This drug also produces sedation by acting on the central nervous system.</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>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>Tulobuterol is a drug used as a bronchodilator for the treatment and management of asthma and COPD. This drug is a long acting beta-2 adrenergic receptor agonist.</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>Agonist of μ opioid receptor; irritable bowel disease treatment</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>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>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>Cisplatin, also known as cisplatinum, is a platinum-based anti-cancer agent that inhibits the EGFR, which is a receptor tyrosine kinase. It has been shown to have anti-cancer effects in melanoma cells and to inhibit tumor growth in mice. Cisplatin acts by interfering with the mechanism of DNA repairing. It loses one chloride ligand and binds to DNA to inhibit the synthesis, causing DNA damage, and thus inducing apoptosis in cancer cells. In certain studies, the use of cisplatin in combination with other metal chelators has shown improvement in the uptake of the anticancer drug. CisplatiN - Bio-X™ 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>Selective c-Met kinase inhibitor</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>Induces expression of Oct3/4 transcription factor</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>Carbamazepine is an anticonvulsant that is used to treat epilepsy and nerve pain from trigeminal neuralgia. The mechanism of action for Carbamazepine is not well understood but it is theorized that carbamazepine reduces seizure activity by preventing sodium channel activation. This interaction reduces the frequency and duration of sodium channel opening, slowing down nerve impulses and helping to prevent seizures Studies on animals have shown that carbamazepine works by reducing polysynaptic nerve response and preventing post-tetanic potentiation.</p>

<p>Gefitinib is an inhibitor of the epidermal growth factor receptor (EGFR) protein. This inhibition is on the EGFR tyrosine kinase domain, where Gefitinib bindings to the ATP-binding site. As a a tyrosine kinase inhibitor, Gefitinib blocks tumor growth and has led to its use in slowing the progression of non-small cell lung cancer. Gefitinib also inhibits invasion and metastasis through inhibition of macrophage receptor interacting protein kinase 2 (RIPK2), rather than EGFR.</p>

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

<p>BDP 37 is a type of boron-dipyrromethene (BODIPY) dye, which is a class of fluorescent compounds known for their stability and brightness. These dyes are synthetic, designed for optimal photophysical properties, and are synthesized through the condensation of pyrrole derivatives with boron difluoride. BDP 37 operates by absorbing light and emitting fluorescence, a process facilitated by its delocalized electron system, which results in a high quantum yield and exceptional photostability. This makes it particularly well-suited for applications requiring long exposure to light.</p>

<p>Platinum-based anti-tumor drug</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>

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